Binding Site Information of Target
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T75596 | Target Info | |||
| Target Name | Methionine aminopeptidase 2 (METAP2) | ||||
| Synonyms | Peptidase M 2; P67eIF2; P67; MetAP 2; METAP2; Initiation factor 2 associated 67 kDa glycoprotein; (MetAP)-2 | ||||
| Target Type | Clinical trial Target | ||||
| Gene Name | METAP2 | ||||
| Biochemical Class | Peptidase | ||||
| UniProt ID | |||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| Ligand Name: D-methionine | Ligand Info | |||||
| Structure Description | Human methionine aminopeptidase type II in complex with D-methionine | PDB:1KQ0 | ||||
| Method | X-ray diffraction | Resolution | 2.00 Å | Mutation | No | [1] |
| PDB Sequence |
VQTDPPSVPI
120 CDLYPNGVFP130 KGQECEYPEE154 KKALDQASEE164 IWNDFREAAE174 AHRQVRKYVM 184 SWIKPGMTMI194 EICEKLEDCS204 RKLIKENGLN214 AGLAFPTGCS224 LNNCAAHYTP 234 NAGDTTVLQY244 DDICKIDFGT254 HISGRIIDCA264 FTVTFNPKYD274 TLLKAVKDAT 284 NTGIKCAGID294 VRLCDVGEAI304 QEVMESYEVE314 IDGKTYQVKP324 IRNLNGHSIG 334 QYRIHAGKTV344 PIIKGGEATR354 MEEGEVYAIE364 TFGSTGKGVV374 HDDMECSHYM 384 KNFDVGHVPI394 RLPRTKHLLN404 VINENFGTLA414 FCRRWLDRLG424 ESKYLMALKN 434 LCDLGIVDPY444 PPLCDIKGSY454 TAQFEHTILL464 RPTCKEVVSR474 GDDY |
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| Ligand Name: Fumagillin | Ligand Info | |||||
| Structure Description | HUMAN METHIONINE AMINOPEPTIDASE 2 COMPLEXED WITH ANGIOGENESIS INHIBITOR FUMAGILLIN | PDB:1BOA | ||||
| Method | X-ray diffraction | Resolution | 1.80 Å | Mutation | No | [2] |
| PDB Sequence |
KVQTDPPSVP
119 ICDLYPNGVF129 PKGQECEYPE154 KKALDQASEE164 IWNDFREAAE174 AHRQVRKYVM 184 SWIKPGMTMI194 EICEKLEDCS204 RKLIKENGLN214 AGLAFPTGCS224 LNNCAAHYTP 234 NAGDTTVLQY244 DDICKIDFGT254 HISGRIIDCA264 FTVTFNPKYD274 TLLKAVKDAT 284 NTGIKCAGID294 VRLCDVGEAI304 QEVMESYEVE314 IDGKTYQVKP324 IRNLNGHSIG 334 QYRIHAGKTV344 PIIKGGEATR354 MEEGEVYAIE364 TFGSTGKGVV374 HDDMECSHYM 384 KNFDVGHVPI394 RLPRTKHLLN404 VINENFGTLA414 FCRRWLDRLG424 ESKYLMALKN 434 LCDLGIVDPY444 PPLCDIKGSY454 TAQFEHTILL464 RPTCKEVVSR474 GDDY |
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PHE219
3.802
PRO220
4.746
ALA230
4.150
HIS231
1.484
ASP262
4.326
ASN327
3.273
LEU328
3.596
ASN329
3.245
GLY330
4.031
HIS331
3.566
ILE338
3.704
HIS339
3.620
|
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| Ligand Name: L-methionine | Ligand Info | |||||
| Structure Description | Human methionine aminopeptidase type II in complex with L-methionine | PDB:1KQ9 | ||||
| Method | X-ray diffraction | Resolution | 1.90 Å | Mutation | No | [1] |
| PDB Sequence |
QTPSVPICDL
123 YPNGVFPKGQ133 ECEYPKKALD159 QASEEIWNDF169 REAAEAHRQV179 RKYVMSWIKP 189 GMTMIEICEK199 LEDCSRKLIK209 ENGLNAGLAF219 PTGCSLNNCA229 AHYTPNAGDT 239 TVLQYDDICK249 IDFGTHISGR259 IIDCAFTVTF269 NPKYDTLLKA279 VKDATNTGIK 289 CAGIDVRLCD299 VGEAIQEVME309 SYEVEIDGKT319 YQVKPIRNLN329 GHSIGQYRIH 339 AGKTVPIIKG349 GEATRMEEGE359 VYAIETFGST369 GKGVVHDDME379 CSHYMKNFDV 389 GHVPIRLPRT399 KHLLNVINEN409 FGTLAFCRRW419 LDRLGESKYL429 MALKNLCDLG 439 IVDPYPPLCD449 IKGSYTAQFE459 HTILLRPTCK469 EVVSRGDDY
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .MET or .MET2 or .MET3 or :3MET;style chemicals stick;color identity;select .A:219 or .A:220 or .A:231 or .A:251 or .A:262 or .A:331 or .A:338 or .A:339 or .A:364 or .A:382 or .A:414 or .A:444 or .A:457 or .A:459; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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| Ligand Name: 2-Methyl-2-Propanol | Ligand Info | |||||
| Structure Description | Structure of human methionine aminopeptidase 2 with covalent spiroepoxytriazole inhibitor (-)-31b | PDB:5D6E | ||||
| Method | X-ray diffraction | Resolution | 1.49 Å | Mutation | No | [3] |
| PDB Sequence |
PKVQTDPPSV
118 PICDLYPNGV128 FPKGQECEYP138 PTQDGRTAAW148 RTTSEEKKAL158 DQASEEIWND 168 FREAAEAHRQ178 VRKYVMSWIK188 PGMTMIEICE198 KLEDCSRKLI208 KENGLNAGLA 218 FPTGCSLNNC228 AAHYTPNAGD238 TTVLQYDDIC248 KIDFGTHISG258 RIIDCAFTVT 268 FNPKYDTLLK278 AVKDATNTGI288 KCAGIDVRLC298 DVGEAIQEVM308 ESYEVEIDGK 318 TYQVKPIRNL328 NGHSIGQYRI338 HAGKTVPIVK348 GGEATRMEEG358 EVYAIETFGS 368 TGKGVVHDDM378 ECSHYMKNFD388 VGHVPIRLPR398 TKHLLNVINE408 NFGTLAFCRR 418 WLDRLGESKY428 LMALKNLCDL438 GIVDPYPPLC448 DIKGSYTAQF458 EHTILLRPTC 468 KEVVSRGDDY478
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .TBU or .TBU2 or .TBU3 or :3TBU;style chemicals stick;color identity;select .A:188 or .A:189 or .A:244 or .A:268 or .A:269 or .A:270 or .A:271 or .A:274; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| Ligand Name: 5-methyl-2-(phenylsulfonamido)benzoic acid | Ligand Info | |||||
| Structure Description | h-MetAP2 complexed with A444148 | PDB:1YW7 | ||||
| Method | X-ray diffraction | Resolution | 1.85 Å | Mutation | No | [4] |
| PDB Sequence |
KVQTDPPSVP
119 ICDLYPNGVF129 PKGQECEYPP139 TQDGRTAAWR149 TTSEEKKALD159 QASEEIWNDF 169 REAAEAHRQV179 RKYVMSWIKP189 GMTMIEICEK199 LEDCSRKLIK209 ENGLNAGLAF 219 PTGCSLNNCA229 AHYTPNAGDT239 TVLQYDDICK249 IDFGTHISGR259 IIDCAFTVTF 269 NPKYDTLLKA279 VKDATNTGIK289 CAGIDVRLCD299 VGEAIQEVME309 SYEVEIDGKT 319 YQVKPIRNLN329 GHSIGQYRIH339 AGKTVPIIKG349 GEATRMEEGE359 VYAIETFGST 369 GKGVVHDDME379 CSHYMKNFDV389 GHVPIRLPRT399 KHLLNVINEN409 FGTLAFCRRW 419 LDRLGESKYL429 MALKNLCDLG439 IVDPYPPLCD449 IKGSYTAQFE459 HTILLRPTCK 469 EVVSRGDDY
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .A41 or .A412 or .A413 or :3A41;style chemicals stick;color identity;select .A:230 or .A:231 or .A:251 or .A:262 or .A:328 or .A:329 or .A:330 or .A:331 or .A:338 or .A:339 or .A:364 or .A:366 or .A:384 or .A:414 or .A:444 or .A:447 or .A:459; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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| Ligand Name: A-357300 | Ligand Info | |||||
| Structure Description | Crystal Structure of MetAP2 complexed with A357300 | PDB:1R58 | ||||
| Method | X-ray diffraction | Resolution | 1.90 Å | Mutation | No | [5] |
| PDB Sequence |
KVQTDPPSVP
119 ICDLYPNGVF129 PKGQECEYPP139 TQDGRTAAWR149 TTSEEKKALD159 QASEEIWNDF 169 REAAEAHRQV179 RKYVMSWIKP189 GMTMIEICEK199 LEDCSRKLIK209 ENGLNAGLAF 219 PTGCSLNNCA229 AHYTPNAGDT239 TVLQYDDICK249 IDFGTHISGR259 IIDCAFTVTF 269 NPKYDTLLKA279 VKDATNTGIK289 CAGIDVRLCD299 VGEAIQEVME309 SYEVEIDGKT 319 YQVKPIRNLN329 GHSIGQYRIH339 AGKTVPIIKG349 GEATRMEEGE359 VYAIETFGST 369 GKGVVHDDME379 CSHYMKNFDV389 GHVPIRLPRT399 KHLLNVINEN409 FGTLAFCRRW 419 LDRLGESKYL429 MALKNLCDLG439 IVDPYPPLCD449 IKGSYTAQFE459 HTILLRPTCK 469 EVVSRGDDY
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .AO5 or .AO52 or .AO53 or :3AO5;style chemicals stick;color identity;select .A:219 or .A:220 or .A:231 or .A:251 or .A:262 or .A:331 or .A:338 or .A:339 or .A:364 or .A:382 or .A:384 or .A:414 or .A:444 or .A:457 or .A:459; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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| Ligand Name: 5-bromo-2-(4-chlorophenylsulfonamido)benzoic acid | Ligand Info | |||||
| Structure Description | h-MetAP2 complexed with A193400 | PDB:2GA2 | ||||
| Method | X-ray diffraction | Resolution | 1.95 Å | Mutation | No | [6] |
| PDB Sequence |
KVQTDPPSVP
119 ICDLYPNGVF129 PKGQECEYPP139 TQDGRTAAWR149 TTSEEKKALD159 QASEEIWNDF 169 REAAEAHRQV179 RKYVMSWIKP189 GMTMIEICEK199 LEDCSRKLIK209 ENGLNAGLAF 219 PTGCSLNNCA229 AHYTPNAGDT239 TVLQYDDICK249 IDFGTHISGR259 IIDCAFTVTF 269 NPKYDTLLKA279 VKDATNTGIK289 CAGIDVRLCD299 VGEAIQEVME309 SYEVEIDGKT 319 YQVKPIRNLN329 GHSIGQYRIH339 AGKTVPIIKG349 GEATRMEEGE359 VYAIETFGST 369 GKGVVHDDME379 CSHYMKNFDV389 GHVPIRLPRT399 KHLLNVINEN409 FGTLAFCRRW 419 LDRLGESKYL429 MALKNLCDLG439 IVDPYPPLCD449 IKGSYTAQFE459 HTILLRPTCK 469 EVVSRGDDY
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .A19 or .A192 or .A193 or :3A19;style chemicals stick;color identity;select .A:230 or .A:231 or .A:251 or .A:262 or .A:328 or .A:329 or .A:330 or .A:331 or .A:338 or .A:339 or .A:364 or .A:366 or .A:382 or .A:384 or .A:414 or .A:444 or .A:447 or .A:459; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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| Ligand Name: (1r,2s,3s,4r)-4-Hydroxy-2-Methoxy-4-Methyl-3-[(2r,3r)-2-Methyl-3-(3-Methylbut-2-En-1-Yl)oxiran-2-Yl]cyclohexyl (Chloroacetyl)carbamate | Ligand Info | |||||
| Structure Description | HUMAN METHIONINE AMINOPEPTIDASE 2 COMPLEXED WITH TNP-470 | PDB:1B6A | ||||
| Method | X-ray diffraction | Resolution | 1.60 Å | Mutation | No | [2] |
| PDB Sequence |
KVQTDPPSVP
119 ICDLYPNGVF129 PKGQECEYPE153 EKKALDQASE163 EIWNDFREAA173 EAHRQVRKYV 183 MSWIKPGMTM193 IEICEKLEDC203 SRKLIKENGL213 NAGLAFPTGC223 SLNNCAAHYT 233 PNAGDTTVLQ243 YDDICKIDFG253 THISGRIIDC263 AFTVTFNPKY273 DTLLKAVKDA 283 TNTGIKCAGI293 DVRLCDVGEA303 IQEVMESYEV313 EIDGKTYQVK323 PIRNLNGHSI 333 GQYRIHAGKT343 VPIVKGGEAT353 RMEEGEVYAI363 ETFGSTGKGV373 VHDDMECSHY 383 MKNFDVGHVP393 IRLPRTKHLL403 NVINENFGTL413 AFCRRWLDRL423 GESKYLMALK 433 NLCDLGIVDP443 YPPLCDIKGS453 YTAQFEHTIL463 LRPTCKEVVS473 RGDDY |
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .TN4 or .TN42 or .TN43 or :3TN4;style chemicals stick;color identity;select .A:219 or .A:220 or .A:230 or .A:231 or .A:251 or .A:262 or .A:327 or .A:328 or .A:329 or .A:330 or .A:331 or .A:338 or .A:339 or .A:343 or .A:364 or .A:366 or .A:382 or .A:384 or .A:414 or .A:444 or .A:447; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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PHE219
3.713
PRO220
4.625
ALA230
4.052
HIS231
1.500
ASP251
4.993
ASP262
4.297
ASN327
3.103
LEU328
3.532
ASN329
3.096
GLY330
4.005
HIS331
3.632
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| Ligand Name: (E)-(2R,3R,4S,5R)-3,4,5-Trihydroxy-2-methoxy-8,8-dimethyl-non-6-enoic acid ((3S,6R)-6-hydroxy-2-oxo-azepan-3-YL)-amide | Ligand Info | |||||
| Structure Description | Human Methionine Aminopeptidase in complex with bengamide inhibitor LAF153 and cobalt | PDB:1QZY | ||||
| Method | X-ray diffraction | Resolution | 1.60 Å | Mutation | No | [7] |
| PDB Sequence |
KVQTDPPSVP
119 ICDLYPNGVF129 PKGQECEYPE153 EKKALDQASE163 EIWNDFREAA173 EAHRQVRKYV 183 MSWIKPGMTM193 IEICEKLEDC203 SRKLIKENGL213 NAGLAFPTGC223 SLNNCAAHYT 233 PNAGDTTVLQ243 YDDICKIDFG253 THISGRIIDC263 AFTVTFNPKY273 DTLLKAVKDA 283 TNTGIKCAGI293 DVRLCDVGEA303 IQEVMESYEV313 EIDGKTYQVK323 PIRNLNGHSI 333 GQYRIHAGKT343 VPIIKGGEAT353 RMEEGEVYAI363 ETFGSTGKGV373 VHDDMECSHY 383 MKNFDVGHVP393 IRLPRTKHLL403 NVINENFGTL413 AFCRRWLDRL423 GESKYLMALK 433 NLCDLGIVDP443 YPPLCDIKGS453 YTAQFEHTIL463 LRPTCKEVVS473 RGDDY |
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .TDE or .TDE2 or .TDE3 or :3TDE;style chemicals stick;color identity;select .A:219 or .A:220 or .A:230 or .A:231 or .A:251 or .A:262 or .A:327 or .A:328 or .A:329 or .A:330 or .A:331 or .A:338 or .A:339 or .A:343 or .A:364 or .A:366 or .A:382 or .A:384 or .A:414 or .A:444 or .A:447 or .A:457 or .A:459; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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PHE219
3.112
PRO220
4.295
ALA230
3.989
HIS231
2.956
ASP251
3.010
ASP262
3.131
ASN327
4.104
LEU328
3.536
ASN329
2.855
GLY330
3.777
HIS331
2.982
ILE338
4.318
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| Ligand Name: N-[(4-fluorophenyl)methyl]-N-(1H-1,2,4-triazol-5-ylmethyl)thiophene-2-sulfonamide | Ligand Info | |||||
| Structure Description | CRYSTAL STRUCTURE OF HUMAN METHIONINE AMINOPEPTIDASE-2 IN COMPLEX WITH AN INHIBITOR Thiophene-2-sulfonic acid (4-fluoro-benzyl)-(4H-[1,2,4]triazol-3-ylmethyl)-amide | PDB:6QEJ | ||||
| Method | X-ray diffraction | Resolution | 1.62 Å | Mutation | No | [8] |
| PDB Sequence |
KVQTDPPSVP
119 ICDLYPNGVF129 PKGQECEYPP139 WRTSEEKKAL158 DQASEEIWND168 FREAAEAHRQ 178 VRKYVMSWIK188 PGMTMIEICE198 KLEDCSRKLI208 KENGLNAGLA218 FPTGCSLNNC 228 AAHYTPNAGD238 TTVLQYDDIC248 KIDFGTHISG258 RIIDCAFTVT268 FNPKYDTLLK 278 AVKDATNTGI288 KCAGIDVRLC298 DVGEAIQEVM308 ESYEVEIDGK318 TYQVKPIRNL 328 NGHSIGQYRI338 HAGKTVPIVK348 GGEATRMEEG358 EVYAIETFGS368 TGKGVVHDDM 378 ECSHYMKNFD388 VGHVPIRLPR398 TKHLLNVINE408 NFGTLAFCRR418 WLDRLGESKY 428 LMALKNLCDL438 GIVDPYPPLC448 DIKGSYTAQF458 EHTILLRPTC468 KEVVSRGDDY 478
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .HZT or .HZT2 or .HZT3 or :3HZT;style chemicals stick;color identity;select .A:219 or .A:220 or .A:231 or .A:251 or .A:262 or .A:328 or .A:329 or .A:330 or .A:331 or .A:338 or .A:339 or .A:343 or .A:364 or .A:382 or .A:383 or .A:384 or .A:414 or .A:444 or .A:447 or .A:457 or .A:459; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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PHE219
3.856
PRO220
3.995
HIS231
2.755
ASP251
3.025
ASP262
3.173
LEU328
4.982
ASN329
3.664
GLY330
3.751
HIS331
3.593
ILE338
3.899
HIS339
3.524
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| Ligand Name: 6-[(2~{r})-2-[(2-Methylphenoxy)methyl]pyrrolidin-1-Yl]-7~{h}-Purine | Ligand Info | |||||
| Structure Description | CRYSTAL STRUCTURE OF HUMAN METHIONINE AMINOPEPTIDASE-2 IN COMPLEX; WITH AN INHIBITOR 6-((R)-2-o-Tolyloxymethyl-pyrrolidin-1-yl)-9H-purine | PDB:5LYW | ||||
| Method | X-ray diffraction | Resolution | 1.69 Å | Mutation | No | [9] |
| PDB Sequence |
KVQTDPPSVP
119 ICDLYPNGVF129 PKGQECEYPT145 AAWRTTSEEK155 KALDQASEEI165 WNDFREAAEA 175 HRQVRKYVMS185 WIKPGMTMIE195 ICEKLEDCSR205 KLIKENGLNA215 GLAFPTGCSL 225 NNCAAHYTPN235 AGDTTVLQYD245 DICKIDFGTH255 ISGRIIDCAF265 TVTFNPKYDT 275 LLKAVKDATN285 TGIKCAGIDV295 RLCDVGEAIQ305 EVMESYEVEI315 DGKTYQVKPI 325 RNLNGHSIGQ335 YRIHAGKTVP345 IVKGATRMEE357 GEVYAIETFG367 STGKGVVHDD 377 MECSHYMKNF387 DVGHVPIRLP397 RTKHLLNVIN407 ENFGTLAFCR417 RWLDRLGESK 427 YLMALKNLCD437 LGIVDPYPPL447 CDIKGSYTAQ457 FEHTILLRPT467 CKEVVSRGD |
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .7BH or .7BH2 or .7BH3 or :37BH;style chemicals stick;color identity;select .A:219 or .A:231 or .A:251 or .A:262 or .A:331 or .A:338 or .A:339 or .A:364 or .A:382 or .A:384 or .A:414 or .A:444 or .A:459; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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| Ligand Name: (3~{S})-~{N}-[(3-chloranyl-5-fluoranyl-phenyl)methyl]-3-oxidanyl-2-oxidanylidene-1-phenyl-pyrrolidine-3-carboxamide | Ligand Info | |||||
| Structure Description | CRYSTAL STRUCTURE OF HUMAN METHIONINE AMINOPEPTIDASE-2 IN COMPLEX WITH AN INHIBITOR (S)-3-Hydroxy-2-oxo-1-phenyl-pyrrolidine-3-carboxylic acid 3-chloro-5-fluoro-benzylamide | PDB:6QEF | ||||
| Method | X-ray diffraction | Resolution | 1.79 Å | Mutation | No | [8] |
| PDB Sequence |
VQTDPPSVPI
120 CDLYPNGVFP130 KGQECEYPPT140 QDGRTAAWRT150 TSEEKKALDQ160 ASEEIWNDFR 170 EAAEAHRQVR180 KYVMSWIKPG190 MTMIEICEKL200 EDCSRKLIKE210 NGLNAGLAFP 220 TGCSLNNCAA230 HYTPNAGDTT240 VLQYDDICKI250 DFGTHISGRI260 IDCAFTVTFN 270 PKYDTLLKAV280 KDATNTGIKC290 AGIDVRLCDV300 GEAIQEVMES310 YEVEIDGKTY 320 QVKPIRNLNG330 HSIGQYRIHA340 GKTVPIVKGG350 EATRMEEGEV360 YAIETFGSTG 370 KGVVHDDMEC380 SHYMKNFDVG390 HVPIRLPRTK400 HLLNVINENF410 GTLAFCRRWL 420 DRLGESKYLM430 ALKNLCDLGI440 VDPYPPLCDI450 KGSYTAQFEH460 TILLRPTCKE 470 VVSRG
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .HZW or .HZW2 or .HZW3 or :3HZW;style chemicals stick;color identity;select .A:219 or .A:220 or .A:230 or .A:231 or .A:251 or .A:262 or .A:327 or .A:328 or .A:329 or .A:331 or .A:338 or .A:339 or .A:364 or .A:366 or .A:382 or .A:383 or .A:384 or .A:414 or .A:444 or .A:447 or .A:457 or .A:459; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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PHE219
3.216
PRO220
4.769
ALA230
3.517
HIS231
3.253
ASP251
3.037
ASP262
3.107
ASN327
4.712
LEU328
3.667
ASN329
3.318
HIS331
3.026
ILE338
3.627
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| Ligand Name: (3~{S})-~{N}-[(3-chloranyl-5-fluoranyl-phenyl)methyl]-3-oxidanyl-2-oxidanylidene-1-(2-oxidanylidene-3,4-dihydro-1~{H}-quinolin-6-yl)pyrrolidine-3-carboxamide | Ligand Info | |||||
| Structure Description | CRYSTAL STRUCTURE OF HUMAN METHIONINE AMINOPEPTIDASE-2 IN COMPLEX; WITH AN INHIBITOR (S)-3-Hydroxy-2-oxo-1-(2-oxo-1,2,3,4-tetrahydro-quinolin-6-yl)-pyrrolidine-3-carboxylic acid 3-chloro-5-fluoro-benzylamide | PDB:6QED | ||||
| Method | X-ray diffraction | Resolution | 1.80 Å | Mutation | No | [8] |
| PDB Sequence |
VQTDPPSVPI
120 CDLYPNGVFP130 KGQECEYPPT140 QDGRTAAWRT150 TSEEKKALDQ160 ASEEIWNDFR 170 EAAEAHRQVR180 KYVMSWIKPG190 MTMIEICEKL200 EDCSRKLIKE210 NGLNAGLAFP 220 TGCSLNNCAA230 HYTPNAGDTT240 VLQYDDICKI250 DFGTHISGRI260 IDCAFTVTFN 270 PKYDTLLKAV280 KDATNTGIKC290 AGIDVRLCDV300 GEAIQEVMES310 YEVEIDGKTY 320 QVKPIRNLNG330 HSIGQYRIHA340 GKTVPIVKGG350 EATRMEEGEV360 YAIETFGSTG 370 KGVVHDDMEC380 SHYMKNFDVG390 HVPIRLPRTK400 HLLNVINENF410 GTLAFCRRWL 420 DRLGESKYLM430 ALKNLCDLGI440 VDPYPPLCDI450 KGSYTAQFEH460 TILLRPTCKE 470 VVSRG
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .HZK or .HZK2 or .HZK3 or :3HZK;style chemicals stick;color identity;select .A:219 or .A:220 or .A:230 or .A:231 or .A:251 or .A:262 or .A:327 or .A:328 or .A:329 or .A:331 or .A:338 or .A:339 or .A:364 or .A:366 or .A:382 or .A:383 or .A:384 or .A:414 or .A:415 or .A:444 or .A:447 or .A:457 or .A:459; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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PHE219
3.265
PRO220
4.785
ALA230
3.557
HIS231
3.118
ASP251
2.920
ASP262
3.404
ASN327
3.909
LEU328
3.550
ASN329
2.890
HIS331
3.181
ILE338
3.628
HIS339
2.700
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|||||
| Ligand Name: 5,6-bis(fluoranyl)-3-(4-piperazin-1-yl-2-propan-2-yloxy-phenyl)-1~{H}-indole-2-carboxamide | Ligand Info | |||||
| Structure Description | CRYSTAL STRUCTURE OF HUMAN METHIONINE AMINOPEPTIDASE-2 IN COMPLEX WITH AN INHIBITOR 5,6-Difluoro-3-(2-isopropoxy-4-piperazin-1-yl-phenyl)-1H-indole-2-carboxylic acid amide | PDB:6QEI | ||||
| Method | X-ray diffraction | Resolution | 1.80 Å | Mutation | No | [8] |
| PDB Sequence |
VQTDPPSVPI
120 CDLYPNGVFP130 KGQECEYPPT140 QDGRTAAWRT150 TSEEKKALDQ160 ASEEIWNDFR 170 EAAEAHRQVR180 KYVMSWIKPG190 MTMIEICEKL200 EDCSRKLIKE210 NGLNAGLAFP 220 TGCSLNNCAA230 HYTPNAGDTT240 VLQYDDICKI250 DFGTHISGRI260 IDCAFTVTFN 270 PKYDTLLKAV280 KDATNTGIKC290 AGIDVRLCDV300 GEAIQEVMES310 YEVEIDGKTY 320 QVKPIRNLNG330 HSIGQYRIHA340 GKTVPIVKAT353 RMEEGEVYAI363 ETFGSTGKGV 373 VHDDMECSHY383 MKNFDVGHVP393 IRLPRTKHLL403 NVINENFGTL413 AFCRRWLDRL 423 GESKYLMALK433 NLCDLGIVDP443 YPPLCDIKGS453 YTAQFEHTIL463 LRPTCKEVVS 473 RG
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .HZE or .HZE2 or .HZE3 or :3HZE;style chemicals stick;color identity;select .A:219 or .A:220 or .A:231 or .A:262 or .A:328 or .A:331 or .A:338 or .A:339 or .A:364 or .A:382 or .A:383 or .A:384 or .A:414 or .A:415 or .A:444 or .A:447 or .A:459; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
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| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| Ligand Name: 5-[[(2R)-1-([1,2,4]triazolo[1,5-a]pyrimidin-7-yl)pyrrolidin-2-yl]methoxy]isoquinoline | Ligand Info | |||||
| Structure Description | CRYSTAL STRUCTURE OF HUMAN METHIONINE AMINOPEPTIDASE-2 IN COMPLEX; WITH AN INHIBITOR 5-((R)-1-[1,2,4]Triazolo[1,5-a]pyrimidin-7-yl-pyrrolidin-2-ylmethoxy)-isoquinoline | PDB:5LYX | ||||
| Method | X-ray diffraction | Resolution | 1.90 Å | Mutation | No | [9] |
| PDB Sequence |
KVQTDPPSVP
119 ICDLYPNGVF129 PKGQECEYPP139 TQDGRTAAWR149 TTSKKALDQA161 SEEIWNDFRE 171 AAEAHRQVRK181 YVMSWIKPGM191 TMIEICEKLE201 DCSRKLIKEN211 GLNAGLAFPT 221 GCSLNNCAAH231 YTPNAGDTTV241 LQYDDICKID251 FGTHISGRII261 DCAFTVTFNP 271 KYDTLLKAVK281 DATNTGIKCA291 GIDVRLCDVG301 EAIQEVMESY311 EVEIDGKTYQ 321 VKPIRNLNGH331 SIGQYRIHAG341 KTVPIVKGGE351 ATRMEEGEVY361 AIETFGSTGK 371 GVVHDDMECS381 HYMKNFDVGH391 VPIRLPRTKH401 LLNVINENFG411 TLAFCRRWLD 421 RLGESKYLMA431 LKNLCDLGIV441 DPYPPLCDIK451 GSYTAQFEHT461 ILLRPTCKEV 471 VSR
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .7BF or .7BF2 or .7BF3 or :37BF;style chemicals stick;color identity;select .A:219 or .A:231 or .A:251 or .A:262 or .A:331 or .A:338 or .A:339 or .A:364 or .A:382 or .A:384 or .A:414 or .A:444 or .A:459; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
||||||
| Ligand Name: (3~{S})-3-oxidanyl-2-oxidanylidene-1-phenyl-~{N}-(2-thiophen-2-ylethyl)pyrrolidine-3-carboxamide | Ligand Info | |||||
| Structure Description | CRYSTAL STRUCTURE OF HUMAN METHIONINE AMINOPEPTIDASE-2 IN COMPLEX WITH AN INHIBITOR 2-Oxo-1-phenyl-pyrrolidine-3-carboxylic acid (2-thiophen-2-yl-ethyl)-amide | PDB:6QEG | ||||
| Method | X-ray diffraction | Resolution | 2.08 Å | Mutation | No | [8] |
| PDB Sequence |
VQTDPPSVPI
120 CDLYPNGVFP130 KGQECEYPPT140 QDGRTAAWRT150 TSEEKKALDQ160 ASEEIWNDFR 170 EAAEAHRQVR180 KYVMSWIKPG190 MTMIEICEKL200 EDCSRKLIKE210 NGLNAGLAFP 220 TGCSLNNCAA230 HYTPNAGDTT240 VLQYDDICKI250 DFGTHISGRI260 IDCAFTVTFN 270 PKYDTLLKAV280 KDATNTGIKC290 AGIDVRLCDV300 GEAIQEVMES310 YEVEIDGKTY 320 QVKPIRNLNG330 HSIGQYRIHA340 GKTVPIVKGG350 EATRMEEGEV360 YAIETFGSTG 370 KGVVHDDMEC380 SHYMKNFDVG390 HVPIRLPRTK400 HLLNVINENF410 GTLAFCRRWL 420 DRLGESKYLM430 ALKNLCDLGI440 VDPYPPLCDI450 KGSYTAQFEH460 TILLRPTCKE 470 VVSR
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .K4K or .K4K2 or .K4K3 or :3K4K;style chemicals stick;color identity;select .A:219 or .A:230 or .A:231 or .A:251 or .A:262 or .A:327 or .A:328 or .A:329 or .A:331 or .A:338 or .A:339 or .A:364 or .A:366 or .A:382 or .A:384 or .A:414 or .A:444 or .A:447 or .A:457 or .A:459; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
PHE219
3.283
ALA230
3.498
HIS231
2.866
ASP251
3.103
ASP262
3.261
ASN327
4.731
LEU328
3.759
ASN329
3.439
HIS331
3.114
ILE338
3.503
|
|||||
| Ligand Name: 5-Chloro-8-hydroxyquinoline | Ligand Info | |||||
| Structure Description | CRYSTAL STRUCTURE OF HUMAN METHIONINE AMINOPEPTIDASE-2 IN COMPLEX WITH AN INHIBITOR 5-Chloro-quinolin-8-ol | PDB:6QEH | ||||
| Method | X-ray diffraction | Resolution | 2.17 Å | Mutation | No | [8] |
| PDB Sequence |
VQTDPPSVPI
120 CDLYPNGVFP130 KGQECEYPPT140 QDGRTAAWRT150 TSEEKKALDQ160 ASEEIWNDFR 170 EAAEAHRQVR180 KYVMSWIKPG190 MTMIEICEKL200 EDCSRKLIKE210 NGLNAGLAFP 220 TGCSLNNCAA230 HYTPNAGDTT240 VLQYDDICKI250 DFGTHISGRI260 IDCAFTVTFN 270 PKYDTLLKAV280 KDATNTGIKC290 AGIDVRLCDV300 GEAIQEVMES310 YEVEIDGKTY 320 QVKPIRNLNG330 HSIGQYRIHA340 GKTVPIVKGG350 EATRMEEGEV360 YAIETFGSTG 370 KGVVHDDMEC380 SHYMKNFDVG390 HVPIRLPRTK400 HLLNVINENF410 GTLAFCRRWL 420 DRLGESKYLM430 ALKNLCDLGI440 VDPYPPLCDI450 KGSYTAQFEH460 TILLRPTCKE 470 VVSRG
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .HZQ or .HZQ2 or .HZQ3 or :3HZQ;style chemicals stick;color identity;select .A:219 or .A:231 or .A:251 or .A:262 or .A:331 or .A:338 or .A:339 or .A:364 or .A:382 or .A:414 or .A:444 or .A:457 or .A:459; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
||||||
| Ligand Name: [(4R,7S)-7-hydroxy-1-[(4-methoxyphenyl)methyl]-7-methyl-5,6-dihydro-4H-benzotriazol-4-yl] N-propan-2-ylcarbamate | Ligand Info | |||||
| Structure Description | Structure of human methionine aminopeptidase 2 with covalent spiroepoxytriazole inhibitor (-)-31b | PDB:5D6E | ||||
| Method | X-ray diffraction | Resolution | 1.49 Å | Mutation | No | [3] |
| PDB Sequence |
PKVQTDPPSV
118 PICDLYPNGV128 FPKGQECEYP138 PTQDGRTAAW148 RTTSEEKKAL158 DQASEEIWND 168 FREAAEAHRQ178 VRKYVMSWIK188 PGMTMIEICE198 KLEDCSRKLI208 KENGLNAGLA 218 FPTGCSLNNC228 AAHYTPNAGD238 TTVLQYDDIC248 KIDFGTHISG258 RIIDCAFTVT 268 FNPKYDTLLK278 AVKDATNTGI288 KCAGIDVRLC298 DVGEAIQEVM308 ESYEVEIDGK 318 TYQVKPIRNL328 NGHSIGQYRI338 HAGKTVPIVK348 GGEATRMEEG358 EVYAIETFGS 368 TGKGVVHDDM378 ECSHYMKNFD388 VGHVPIRLPR398 TKHLLNVINE408 NFGTLAFCRR 418 WLDRLGESKY428 LMALKNLCDL438 GIVDPYPPLC448 DIKGSYTAQF458 EHTILLRPTC 468 KEVVSRGDDY478
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .94A or .94A2 or .94A3 or :394A;style chemicals stick;color identity;select .A:219 or .A:220 or .A:230 or .A:231 or .A:251 or .A:262 or .A:327 or .A:328 or .A:329 or .A:331 or .A:338 or .A:339 or .A:364 or .A:366 or .A:374 or .A:382 or .A:383 or .A:384 or .A:414 or .A:444 or .A:447 or .A:457 or .A:459; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
PHE219
3.781
PRO220
4.478
ALA230
4.309
HIS231
2.794
ASP251
3.847
ASP262
3.475
ASN327
3.257
LEU328
3.489
ASN329
3.117
HIS331
3.296
ILE338
3.664
HIS339
3.470
|
|||||
| Ligand Name: (4s,7r)-7-Hydroxy-1-(4-Methoxybenzyl)-7-Methyl-4,5,6,7-Tetrahydro-1h-Benzotriazol-4-Yl Propan-2-Ylcarbamate | Ligand Info | |||||
| Structure Description | Structure of human methionine aminopeptidase-2 complexed with spiroepoxytriazole inhibitor (+)-31b | PDB:5D6F | ||||
| Method | X-ray diffraction | Resolution | 1.55 Å | Mutation | No | [3] |
| PDB Sequence |
KVQTDPPSVP
119 ICDLYPNGVF129 PKGQECEYPP139 TQDGRTAAWR149 TTSEEKKALD159 QASEEIWNDF 169 REAAEAHRQV179 RKYVMSWIKP189 GMTMIEICEK199 LEDCSRKLIK209 ENGLNAGLAF 219 PTGCSLNNCA229 AHYTPNAGDT239 TVLQYDDICK249 IDFGTHISGR259 IIDCAFTVTF 269 NPKYDTLLKA279 VKDATNTGIK289 CAGIDVRLCD299 VGEAIQEVME309 SYEVEIDGKT 319 YQVKPIRNLN329 GHSIGQYRIH339 AGKTVPIVKG349 GEATRMEEGE359 VYAIETFGST 369 GKGVVHDDME379 CSHYMKNFDV389 GHVPIRLPRT399 KHLLNVINEN409 FGTLAFCRRW 419 LDRLGESKYL429 MALKNLCDLG439 IVDPYPPLCD449 IKGSYTAQFE459 HTILLRPTCK 469 EVVSRGDDY
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .57R or .57R2 or .57R3 or :357R;style chemicals stick;color identity;select .A:219 or .A:220 or .A:230 or .A:231 or .A:251 or .A:262 or .A:327 or .A:328 or .A:329 or .A:331 or .A:338 or .A:339 or .A:364 or .A:366 or .A:382 or .A:383 or .A:384 or .A:414 or .A:415 or .A:444 or .A:447 or .A:459; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
PHE219
4.105
PRO220
4.409
ALA230
4.114
HIS231
1.421
ASP251
4.817
ASP262
4.379
ASN327
3.285
LEU328
3.677
ASN329
2.822
HIS331
3.884
ILE338
3.728
|
|||||
| Ligand Name: (4r,7r)-7-Hydroxy-1-(4-Methoxybenzyl)-7-Methyl-4,5,6,7-Tetrahydro-1h-Benzotriazol-4-Yl Propan-2-Ylcarbamate | Ligand Info | |||||
| Structure Description | Structure of human methionine aminopeptidase-2 complexed with spiroepoxytriazole inhibitor (+)-31a | PDB:5CLS | ||||
| Method | X-ray diffraction | Resolution | 1.75 Å | Mutation | No | [3] |
| PDB Sequence |
KVQTDPPSVP
119 ICDLYPNGVF129 PKGQECEYPP139 TQDGRTAAWR149 TTSEEKKALD159 QASEEIWNDF 169 REAAEAHRQV179 RKYVMSWIKP189 GMTMIEICEK199 LEDCSRKLIK209 ENGLNAGLAF 219 PTGCSLNNCA229 AHYTPNAGDT239 TVLQYDDICK249 IDFGTHISGR259 IIDCAFTVTF 269 NPKYDTLLKA279 VKDATNTGIK289 CAGIDVRLCD299 VGEAIQEVME309 SYEVEIDGKT 319 YQVKPIRNLN329 GHSIGQYRIH339 AGKTVPIVKG349 GEATRMEEGE359 VYAIETFGST 369 GKGVVHDDME379 CSHYMKNFDV389 GHVPIRLPRT399 KHLLNVINEN409 FGTLAFCRRW 419 LDRLGESKYL429 MALKNLCDLG439 IVDPYPPLCD449 IKGSYTAQFE459 HTILLRPTCK 469 EVVSRGDDY
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .52T or .52T2 or .52T3 or :352T;style chemicals stick;color identity;select .A:219 or .A:220 or .A:230 or .A:231 or .A:251 or .A:262 or .A:327 or .A:328 or .A:329 or .A:331 or .A:338 or .A:339 or .A:343 or .A:364 or .A:382 or .A:383 or .A:384 or .A:414 or .A:444 or .A:447; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
PHE219
3.523
PRO220
4.332
ALA230
3.964
HIS231
1.516
ASP251
3.999
ASP262
3.182
ASN327
3.810
LEU328
3.595
ASN329
2.857
HIS331
2.873
|
|||||
| Ligand Name: 5-chloro-3-phenyl-1H-indole-2-carboxamide | Ligand Info | |||||
| Structure Description | CRYSTAL STRUCTURE OF HUMAN METHIONINE AMINOPEPTIDASE-2 IN COMPLEX WITH AN INHIBITOR GW557358X (COMPOUND 9) | PDB:7A12 | ||||
| Method | X-ray diffraction | Resolution | 2.00 Å | Mutation | No | [10] |
| PDB Sequence |
KVQTDPPSVP
119 ICDLYPNGVF129 PKGQECEYPP139 TQDGRTAAWR149 TTSEEKKALD159 QASEEIWNDF 169 REAAEAHRQV179 RKYVMSWIKP189 GMTMIEICEK199 LEDCSRKLIK209 ENGLNAGLAF 219 PTGCSLNNCA229 AHYTPNAGDT239 TVLQYDDICK249 IDFGTHISGR259 IIDCAFTVTF 269 NPKYDTLLKA279 VKDATNTGIK289 CAGIDVRLCD299 VGEAIQEVME309 SYEVEIDGKT 319 YQVKPIRNLN329 GHSIGQYRIH339 AGKTVPIVKA352 TRMEEGEVYA362 IETFGSTGKG 372 VVHDDMECSH382 YMKNFDVGHV392 PIRLPRTKHL402 LNVINENFGT412 LAFCRRWLDR 422 LGESKYLMAL432 KNLCDLGIVD442 PYPPLCDIKG452 SYTAQFEHTI462 LLRPTCKEVV 472 SRGDDY
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .QVK or .QVK2 or .QVK3 or :3QVK;style chemicals stick;color identity;select .A:219 or .A:220 or .A:231 or .A:262 or .A:331 or .A:338 or .A:339 or .A:364 or .A:382 or .A:383 or .A:384 or .A:414 or .A:415 or .A:444 or .A:459; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
||||||
| Ligand Name: 5-chloranyl-3-(3-methoxyphenyl)-1~{H}-indole-2-carboxamide | Ligand Info | |||||
| Structure Description | CRYSTAL STRUCTURE OF HUMAN METHIONINE AMINOPEPTIDASE-2 IN COMPLEX WITH AN INHIBITOR GSK1978537A (COMPOUND 27) | PDB:7A13 | ||||
| Method | X-ray diffraction | Resolution | 2.04 Å | Mutation | No | [10] |
| PDB Sequence |
KVQTDPPSVP
119 ICDLYPNGVF129 PKGQECEYPP139 TQDGRTAAWR149 TTSEEKKALD159 QASEEIWNDF 169 REAAEAHRQV179 RKYVMSWIKP189 GMTMIEICEK199 LEDCSRKLIK209 ENGLNAGLAF 219 PTGCSLNNCA229 AHYTPNAGDT239 TVLQYDDICK249 IDFGTHISGR259 IIDCAFTVTF 269 NPKYDTLLKA279 VKDATNTGIK289 CAGIDVRLCD299 VGEAIQEVME309 SYEVEIDGKT 319 YQVKPIRNLN329 GHSIGQYRIH339 AGKTVPIVKA352 TRMEEGEVYA362 IETFGSTGKG 372 VVHDDMECSH382 YMKNFDVGHV392 PIRLPRTKHL402 LNVINENFGT412 LAFCRRWLDR 422 LGESKYLMAL432 KNLCDLGIVD442 PYPPLCDIKG452 SYTAQFEHTI462 LLRPTCKEVV 472 SRGDDY
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .QW5 or .QW52 or .QW53 or :3QW5;style chemicals stick;color identity;select .A:219 or .A:220 or .A:231 or .A:262 or .A:331 or .A:338 or .A:339 or .A:364 or .A:382 or .A:383 or .A:384 or .A:414 or .A:415 or .A:444 or .A:459; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
||||||
| Ligand Name: 5-chloranyl-6-fluoranyl-3-(2-propan-2-yloxyphenyl)-1~{H}-indole-2-carboxamide | Ligand Info | |||||
| Structure Description | CRYSTAL STRUCTURE OF HUMAN METHIONINE AMINOPEPTIDASE-2 IN COMPLEX WITH AN INHIBITOR GSK2218325A (COMPOUND 32) | PDB:7A14 | ||||
| Method | X-ray diffraction | Resolution | 2.14 Å | Mutation | No | [10] |
| PDB Sequence |
KVQTDPPSVP
119 ICDLYPNGVF129 PKGQECEYPP139 TQDGRTAAWR149 TTSEEKKALD159 QASEEIWNDF 169 REAAEAHRQV179 RKYVMSWIKP189 GMTMIEICEK199 LEDCSRKLIK209 ENGLNAGLAF 219 PTGCSLNNCA229 AHYTPNAGDT239 TVLQYDDICK249 IDFGTHISGR259 IIDCAFTVTF 269 NPKYDTLLKA279 VKDATNTGIK289 CAGIDVRLCD299 VGEAIQEVME309 SYEVEIDGKT 319 YQVKPIRNLN329 GHSIGQYRIH339 AGKTVPIVKA352 TRMEEGEVYA362 IETFGSTGKG 372 VVHDDMECSH382 YMKNFDVGHV392 PIRLPRTKHL402 LNVINENFGT412 LAFCRRWLDR 422 LGESKYLMAL432 KNLCDLGIVD442 PYPPLCDIKG452 SYTAQFEHTI462 LLRPTCKEVV 472 SRGDDY
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .QVB or .QVB2 or .QVB3 or :3QVB;style chemicals stick;color identity;select .A:219 or .A:220 or .A:231 or .A:262 or .A:328 or .A:331 or .A:338 or .A:339 or .A:364 or .A:382 or .A:383 or .A:384 or .A:414 or .A:415 or .A:444 or .A:447 or .A:459; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
||||||
| Ligand Name: 5-chloranyl-6-fluoranyl-3-(4-piperazin-1-yl-2-propan-2-yloxy-phenyl)-1~{H}-indole-2-carboxamide | Ligand Info | |||||
| Structure Description | CRYSTAL STRUCTURE OF HUMAN METHIONINE AMINOPEPTIDASE-2 IN COMPLEX WITH AN INHIBITOR GSK2224863A (COMPOUND 42) | PDB:7A15 | ||||
| Method | X-ray diffraction | Resolution | 2.15 Å | Mutation | No | [10] |
| PDB Sequence |
KVQTDPPSVP
119 ICDLYPNGVF129 PKGQECEYPP139 TQDGRTAAWR149 TTSEEKKALD159 QASEEIWNDF 169 REAAEAHRQV179 RKYVMSWIKP189 GMTMIEICEK199 LEDCSRKLIK209 ENGLNAGLAF 219 PTGCSLNNCA229 AHYTPNAGDT239 TVLQYDDICK249 IDFGTHISGR259 IIDCAFTVTF 269 NPKYDTLLKA279 VKDATNTGIK289 CAGIDVRLCD299 VGEAIQEVME309 SYEVEIDGKT 319 YQVKPIRNLN329 GHSIGQYRIH339 AGKTVPIVAT353 RMEEGEVYAI363 ETFGSTGKGV 373 VHDDMECSHY383 MKNFDVGHVP393 IRLPRTKHLL403 NVINENFGTL413 AFCRRWLDRL 423 GESKYLMALK433 NLCDLGIVDP443 YPPLCDIKGS453 YTAQFEHTIL463 LRPTCKEVVS 473 RGDDY
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .QV5 or .QV52 or .QV53 or :3QV5;style chemicals stick;color identity;select .A:219 or .A:220 or .A:231 or .A:262 or .A:328 or .A:329 or .A:331 or .A:338 or .A:339 or .A:364 or .A:382 or .A:383 or .A:384 or .A:414 or .A:415 or .A:444 or .A:447 or .A:459; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
||||||
| Ligand Name: 3,4-Dihydroxy-2-methoxy-4-methyl-3-[2-methyl-3-(3-methyl-but-2-enyl)-oxiranyl]-cyclohexanone | Ligand Info | |||||
| Structure Description | COMPLEX OF HUMAN METHIONINE AMINOPEPTIDASE-2 COMPLEXED WITH OVALICIN | PDB:1B59 | ||||
| Method | X-ray diffraction | Resolution | 1.80 Å | Mutation | No | [2] |
| PDB Sequence |
KVQTDPPSVP
119 ICDLYPNGVF129 PKGQECEYPE153 EKKALDQASE163 EIWNDFREAA173 EAHRQVRKYV 183 MSWIKPGMTM193 IEICEKLEDC203 SRKLIKENGL213 NAGLAFPTGC223 SLNNCAAHYT 233 PNAGDTTVLQ243 YDDICKIDFG253 THISGRIIDC263 AFTVTFNPKY273 DTLLKAVKDA 283 TNTGIKCAGI293 DVRLCDVGEA303 IQEVMESYEV313 EIDGKTYQVK323 PIRNLNGHSI 333 GQYRIHAGKT343 VPIVKGGEAT353 RMEEGEVYAI363 ETFGSTGKGV373 VHDDMECSHY 383 MKNFDVGHVP393 IRLPRTKHLL403 NVINENFGTL413 AFCRRWLDRL423 GESKYLMALK 433 NLCDLGIVDP443 YPPLCDIKGS453 YTAQFEHTIL463 LRPTCKEVVS473 RGDDY |
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .OVA or .OVA2 or .OVA3 or :3OVA;style chemicals stick;color identity;select .A:219 or .A:220 or .A:230 or .A:231 or .A:262 or .A:327 or .A:328 or .A:329 or .A:330 or .A:331 or .A:338 or .A:339 or .A:343 or .A:364 or .A:366 or .A:382 or .A:384 or .A:414 or .A:444 or .A:447; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
PHE219
3.897
PRO220
4.846
ALA230
4.065
HIS231
1.489
ASP262
4.478
ASN327
4.802
LEU328
3.677
ASN329
3.079
GLY330
3.893
HIS331
3.618
|
|||||
| Ligand Name: 7-Fluoro-4-(5-Methyl-3h-Imidazo[4,5-B]pyridin-6-Yl)-2,4-Dihydropyrazolo[4,3-B]indole | Ligand Info | |||||
| Structure Description | Potent, Reversible MetAP2 Inhibitors via Fragment Based Drug Discovery | PDB:5JFR | ||||
| Method | X-ray diffraction | Resolution | 1.60 Å | Mutation | No | [11] |
| PDB Sequence |
KVQTDPPSVP
119 ICDLYPNGVF129 PKGQECEYPP139 TQDGRTAAWR149 TTSEEKKALD159 QASEEIWNDF 169 REAAEAHRQV179 RKYVMSWIKP189 GMTMIEICEK199 LEDCSRKLIK209 ENGLNAGLAF 219 PTGCSLNNCA229 AHYTPNAGDT239 TVLQYDDICK249 IDFGTHISGR259 IIDCAFTVTF 269 NPKYDTLLKA279 VKDATNTGIK289 CAGIDVRLCD299 VGEAIQEVME309 SYEVEIDGKT 319 YQVKPIRNLN329 GHSIGQYRIH339 AGKTVPIVKG349 TRMEEGEVYA362 IETFGSTGKG 372 VVHDDMECSH382 YMKNFDVGHV392 PIRLPRTKHL402 LNVINENFGT412 LAFCRRWLDR 422 LGESKYLMAL432 KNLCDLGIVD442 PYPPLCDIKG452 SYTAQFEHTI462 LLRPTCKEVV 472 SRGDDY
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .6KP or .6KP2 or .6KP3 or :36KP;style chemicals stick;color identity;select .A:219 or .A:220 or .A:231 or .A:262 or .A:331 or .A:338 or .A:339 or .A:364 or .A:382 or .A:383 or .A:384 or .A:414 or .A:444 or .A:459; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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| Ligand Name: 2-[({2-[(1Z)-3-(Dimethylamino)prop-1-enyl]-4-fluorophenyl}sulfonyl)amino]-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid | Ligand Info | |||||
| Structure Description | h-MetAP2 complexed with A849519 | PDB:1YW9 | ||||
| Method | X-ray diffraction | Resolution | 1.64 Å | Mutation | No | [4] |
| PDB Sequence |
KVQTDPPSVP
119 ICDLYPNGVF129 PKGQECEYPP139 TQDGRTAAWR149 TTSEEKKALD159 QASEEIWNDF 169 REAAEAHRQV179 RKYVMSWIKP189 GMTMIEICEK199 LEDCSRKLIK209 ENGLNAGLAF 219 PTGCSLNNCA229 AHYTPNAGDT239 TVLQYDDICK249 IDFGTHISGR259 IIDCAFTVTF 269 NPKYDTLLKA279 VKDATNTGIK289 CAGIDVRLCD299 VGEAIQEVME309 SYEVEIDGKT 319 YQVKPIRNLN329 GHSIGQYRIH339 AGKTVPIIKG349 GEATRMEEGE359 VYAIETFGST 369 GKGVVHDDME379 CSHYMKNFDV389 GHVPIRLPRT399 KHLLNVINEN409 FGTLAFCRRW 419 LDRLGESKYL429 MALKNLCDLG439 IVDPYPPLCD449 IKGSYTAQFE459 HTILLRPTCK 469 EVVSRGDDY
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .A84 or .A842 or .A843 or :3A84;style chemicals stick;color identity;select .A:219 or .A:220 or .A:230 or .A:231 or .A:251 or .A:262 or .A:327 or .A:328 or .A:329 or .A:330 or .A:331 or .A:338 or .A:339 or .A:364 or .A:366 or .A:382 or .A:384 or .A:414 or .A:444 or .A:447 or .A:459; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
PHE219
3.887
PRO220
4.730
ALA230
3.076
HIS231
2.942
ASP251
4.756
ASP262
3.114
ASN327
4.340
LEU328
3.395
ASN329
3.126
GLY330
4.009
HIS331
2.766
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| Ligand Name: [(2R)-1-([1,2,4]triazolo[1,5-a]pyrimidin-7-yl)pyrrolidin-2-yl]methyl 2-methoxybenzoate | Ligand Info | |||||
| Structure Description | Potent, Reversible MetAP2 Inhibitors via FBDD | PDB:5JHU | ||||
| Method | X-ray diffraction | Resolution | 1.80 Å | Mutation | No | [12] |
| PDB Sequence |
KVQTDPPSVP
119 ICDLYPNGVF129 PKGQECEYPP139 TQDGRTAAWR149 TTSEEKKALD159 QASEEIWNDF 169 REAAEAHRQV179 RKYVMSWIKP189 GMTMIEICEK199 LEDCSRKLIK209 ENGLNAGLAF 219 PTGCSLNNCA229 AHYTPNAGDT239 TVLQYDDICK249 IDFGTHISGR259 IIDCAFTVTF 269 NPKYDTLLKA279 VKDATNTGIK289 CAGIDVRLCD299 VGEAIQEVME309 SYEVEIDGKT 319 YQVKPIRNLN329 GHSIGQYRIH339 AGKTVPTRME356 EGEVYAIETF366 GSTGKGVVHD 376 DMECSHYMKN386 FDVGHVPIRL396 PRTKHLLNVI406 NENFGTLAFC416 RRWLDRLGES 426 KYLMALKNLC436 DLGIVDPYPP446 LCDIKGSYTA456 QFEHTILLRP466 TCKEVVSRGD 476 DY
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .6KO or .6KO2 or .6KO3 or :36KO;style chemicals stick;color identity;select .A:219 or .A:220 or .A:231 or .A:251 or .A:262 or .A:331 or .A:338 or .A:339 or .A:364 or .A:382 or .A:384 or .A:414 or .A:444 or .A:459; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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| Ligand Name: 4-(3-Methylphenyl)-1H-1,2,3-triazole | Ligand Info | |||||
| Structure Description | Human Methionine Aminopeptidase Complex with 4-Aryl-1,2,3-triazole Inhibitor | PDB:2ADU | ||||
| Method | X-ray diffraction | Resolution | 1.90 Å | Mutation | No | [13] |
| PDB Sequence |
KVQTDPPSVP
119 ICDLYPNGVF129 PKGQECEYPE153 EKKALDQASE163 EIWNDFREAA173 EAHRQVRKYV 183 MSWIKPGMTM193 IEICEKLEDC203 SRKLIKENGL213 NAGLAFPTGC223 SLNNCAAHYT 233 PNAGDTTVLQ243 YDDICKIDFG253 THISGRIIDC263 AFTVTFNPKY273 DTLLKAVKDA 283 TNTGIKCAGI293 DVRLCDVGEA303 IQEVMESYEV313 EIDGKTYQVK323 PIRNLNGHSI 333 GQYRIHAGKT343 VPIIKGGEAT353 RMEEGEVYAI363 ETFGSTGKGV373 VHDDMECSHY 383 MKNFDVGHVP393 IRLPRTKHLL403 NVINENFGTL413 AFCRRWLDRL423 GESKYLMALK 433 NLCDLGIVDP443 YPPLCDIKGS453 YTAQFEHTIL463 LRPTCKEVVS473 RGDDY |
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|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .R20 or .R202 or .R203 or :3R20;style chemicals stick;color identity;select .A:219 or .A:231 or .A:251 or .A:262 or .A:331 or .A:338 or .A:339 or .A:364 or .A:382 or .A:384 or .A:414 or .A:444 or .A:459; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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| Ligand Name: N-(2-Isopropylphenyl)-3-[(2-Thienylmethyl)thio]-1h-1,2,4-Triazol-5-Amine | Ligand Info | |||||
| Structure Description | Human Methionine Aminopeptidase-2 Complexed with SB-587094 | PDB:2OAZ | ||||
| Method | X-ray diffraction | Resolution | 1.90 Å | Mutation | Yes | [14] |
| PDB Sequence |
KVQTDPPSVP
10 ICDLYPNGVF20 PKGQECEYPE153 EKKALDQASE163 EIWNDFREAA173 EAHRQVRKYV 183 MSWIKPGMTM193 IEICEKLEDC203 SRKLIKENGL213 NAGLAFPTGC223 SLNNCAAHYT 233 PNAGDTTVLQ243 YDDICKIDFG253 THISGRIIDC263 AFTVTFNPKY273 DTLLKAVKDA 283 TNTGIKCAGI293 DVRLCDVGEA303 IQEVMESYEV313 EIDGKTYQVK323 PIRNLNGHSI 333 GQYRIHAGKT343 VPIIKGGEAT353 RMEEGEVYAI363 ETFGSTGKGV373 VHDDMECSHY 383 MKNFDVGHVP393 IRLPRTKHLL403 NVINENFGTL413 AFCRRWLDRL423 GESKYLMALK 433 NLCDLGIVDP443 YPPLCDIKGS453 YTAQFEHTIL463 LRPTCKEVVS473 RGDDY |
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .I96 or .I962 or .I963 or :3I96;style chemicals stick;color identity;select .A:219 or .A:220 or .A:230 or .A:231 or .A:251 or .A:262 or .A:328 or .A:329 or .A:331 or .A:338 or .A:339 or .A:364 or .A:382 or .A:384 or .A:414 or .A:444 or .A:447 or .A:457 or .A:459; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
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| Ligand Name: (2S,3R)-3-Amino-2-hydroxy-5-(ethylsulfanyl)pentanoyl-((S)-(-)-(1-naphthyl)ethyl)amide | Ligand Info | |||||
| Structure Description | Crystal Structure of MetAP2 complexed with A311263 | PDB:1R5G | ||||
| Method | X-ray diffraction | Resolution | 2.00 Å | Mutation | No | [5] |
| PDB Sequence |
KVQTDPPSVP
119 ICDLYPNGVF129 PKGQECEYPP139 TQDGRTAAWR149 TTSEEKKALD159 QASEEIWNDF 169 REAAEAHRQV179 RKYVMSWIKP189 GMTMIEICEK199 LEDCSRKLIK209 ENGLNAGLAF 219 PTGCSLNNCA229 AHYTPNAGDT239 TVLQYDDICK249 IDFGTHISGR259 IIDCAFTVTF 269 NPKYDTLLKA279 VKDATNTGIK289 CAGIDVRLCD299 VGEAIQEVME309 SYEVEIDGKT 319 YQVKPIRNLN329 GHSIGQYRIH339 AGKTVPIIKG349 GEATRMEEGE359 VYAIETFGST 369 GKGVVHDDME379 CSHYMKNFDV389 GHVPIRLPRT399 KHLLNVINEN409 FGTLAFCRRW 419 LDRLGESKYL429 MALKNLCDLG439 IVDPYPPLCD449 IKGSYTAQFE459 HTILLRPTCK 469 EVVSRGDDY
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|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .AO1 or .AO12 or .AO13 or :3AO1;style chemicals stick;color identity;select .A:219 or .A:231 or .A:251 or .A:262 or .A:328 or .A:329 or .A:330 or .A:331 or .A:338 or .A:339 or .A:343 or .A:364 or .A:366 or .A:382 or .A:384 or .A:414 or .A:444 or .A:457 or .A:459; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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| Ligand Name: 4-(3-methylpyridin-4-yl)-6-(trifluoromethyl)-1H-indazole | Ligand Info | |||||
| Structure Description | Potent, Reversible MetAP2 Inhibitors via FBDD | PDB:5JI6 | ||||
| Method | X-ray diffraction | Resolution | 2.15 Å | Mutation | No | [12] |
| PDB Sequence |
KVQTDPPSVP
119 ICDLYPNGVF129 PKGQECEYPP139 TQDGRTAAWR149 TTSEEKKALD159 QASEEIWNDF 169 REAAEAHRQV179 RKYVMSWIKP189 GMTMIEICEK199 LEDCSRKLIK209 ENGLNAGLAF 219 PTGCSLNNCA229 AHYTPNAGDT239 TVLQYDDICK249 IDFGTHISGR259 IIDCAFTVTF 269 NPKYDTLLKA279 VKDATNTGIK289 CAGIDVRLCD299 VGEAIQEVME309 SYEVEIDGKT 319 YQVKPIRNLN329 GHSIGQYRIH339 AGKTVPIVKG350 EATRMEEGEV360 YAIETFGSTG 370 KGVVHDDMEC380 SHYMKNFDVG390 HVPIRLPRTK400 HLLNVINENF410 GTLAFCRRWL 420 DRLGESKYLM430 ALKNLCDLGI440 VDPYPPLCDI450 KGSYTAQFEH460 TILLRPTCKE 470 VVSRGDDY
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .6KN or .6KN2 or .6KN3 or :36KN;style chemicals stick;color identity;select .A:219 or .A:220 or .A:231 or .A:251 or .A:262 or .A:331 or .A:338 or .A:339 or .A:364 or .A:382 or .A:384 or .A:414 or .A:444 or .A:459; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
||||||
| Ligand Name: 2-(2-Aminoethoxy)-3-Ethyl-6-{[(4-Fluorophenyl)sulfonyl]amino}benzoic Acid | Ligand Info | |||||
| Structure Description | h-MetAP2 complexed with A797859 | PDB:2EA4 | ||||
| Method | X-ray diffraction | Resolution | 2.35 Å | Mutation | No | [15] |
| PDB Sequence |
KVQTDPPSVP
119 ICDLYPNGVF129 PKGQECEYPP139 TQDGRTAAWR149 TTSEEKKALD159 QASEEIWNDF 169 REAAEAHRQV179 RKYVMSWIKP189 GMTMIEICEK199 LEDCSRKLIK209 ENGLNAGLAF 219 PTGCSLNNCA229 AHYTPNAGDT239 TVLQYDDICK249 IDFGTHISGR259 IIDCAFTVTF 269 NPKYDTLLKA279 VKDATNTGIK289 CAGIDVRLCD299 VGEAIQEVME309 SYEVEIDGKT 319 YQVKPIRNLN329 GHSIGQYRIH339 AGKTVPIIKG349 GEATRMEEGE359 VYAIETFGST 369 GKGVVHDDME379 CSHYMKNFDV389 GHVPIRLPRT399 KHLLNVINEN409 FGTLAFCRRW 419 LDRLGESKYL429 MALKNLCDLG439 IVDPYPPLCD449 IKGSYTAQFE459 HTILLRPTCK 469 EVVSRGDDY
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|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .F79 or .F792 or .F793 or :3F79;style chemicals stick;color identity;select .A:219 or .A:230 or .A:231 or .A:251 or .A:262 or .A:328 or .A:329 or .A:330 or .A:331 or .A:338 or .A:339 or .A:364 or .A:366 or .A:382 or .A:384 or .A:414 or .A:444 or .A:447 or .A:459; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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| Ligand Name: N'-(2S,3R)-3-Amino-4-cyclohexyl-2-hydroxy-butano-N-(4-methylphenyl)hydrazide | Ligand Info | |||||
| Structure Description | Crystal Structure of MetAP2 complexed with A320282 | PDB:1R5H | ||||
| Method | X-ray diffraction | Resolution | 2.40 Å | Mutation | No | [5] |
| PDB Sequence |
KVQTDPPSVP
119 ICDLYPNGVF129 PKGQECEYPP139 TQDGRTAAWR149 TTSEEKKALD159 QASEEIWNDF 169 REAAEAHRQV179 RKYVMSWIKP189 GMTMIEICEK199 LEDCSRKLIK209 ENGLNAGLAF 219 PTGCSLNNCA229 AHYTPNAGDT239 TVLQYDDICK249 IDFGTHISGR259 IIDCAFTVTF 269 NPKYDTLLKA279 VKDATNTGIK289 CAGIDVRLCD299 VGEAIQEVME309 SYEVEIDGKT 319 YQVKPIRNLN329 GHSIGQYRIH339 AGKTVPIIKG349 GEATRMEEGE359 VYAIETFGST 369 GKGVVHDDME379 CSHYMKNFDV389 GHVPIRLPRT399 KHLLNVINEN409 FGTLAFCRRW 419 LDRLGESKYL429 MALKNLCDLG439 IVDPYPPLCD449 IKGSYTAQFE459 HTILLRPTCK 469 EVVSRGDDY
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|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .AO2 or .AO22 or .AO23 or :3AO2;style chemicals stick;color identity;select .A:219 or .A:231 or .A:251 or .A:262 or .A:327 or .A:328 or .A:329 or .A:330 or .A:331 or .A:338 or .A:339 or .A:364 or .A:382 or .A:384 or .A:414 or .A:444 or .A:457 or .A:459; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
||||||
| Ligand Name: 3-Ethyl-6-{[(4-Fluorophenyl)sulfonyl]amino}-2-Methylbenzoic Acid | Ligand Info | |||||
| Structure Description | h-MetAP2 complexed with A773812 | PDB:2EA2 | ||||
| Method | X-ray diffraction | Resolution | 2.50 Å | Mutation | No | [15] |
| PDB Sequence |
KVQTDPPSVP
119 ICDLYPNGVF129 PKGQECEYPP139 TQDGRTAAWR149 TTSEEKKALD159 QASEEIWNDF 169 REAAEAHRQV179 RKYVMSWIKP189 GMTMIEICEK199 LEDCSRKLIK209 ENGLNAGLAF 219 PTGCSLNNCA229 AHYTPNAGDT239 TVLQYDDICK249 IDFGTHISGR259 IIDCAFTVTF 269 NPKYDTLLKA279 VKDATNTGIK289 CAGIDVRLCD299 VGEAIQEVME309 SYEVEIDGKT 319 YQVKPIRNLN329 GHSIGQYRIH339 AGKTVPIIKG349 GEATRMEEGE359 VYAIETFGST 369 GKGVVHDDME379 CSHYMKNFDV389 GHVPIRLPRT399 KHLLNVINEN409 FGTLAFCRRW 419 LDRLGESKYL429 MALKNLCDLG439 IVDPYPPLCD449 IKGSYTAQFE459 HTILLRPTCK 469 EVVSRGDDY
|
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|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .F77 or .F772 or .F773 or :3F77;style chemicals stick;color identity;select .A:219 or .A:230 or .A:231 or .A:251 or .A:262 or .A:328 or .A:329 or .A:330 or .A:331 or .A:338 or .A:339 or .A:364 or .A:366 or .A:382 or .A:384 or .A:414 or .A:444 or .A:447 or .A:459; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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||||||
| Ligand Name: 2-[(Phenylsulfonyl)amino]-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid | Ligand Info | |||||
| Structure Description | h-MetAP2 complexed with A751277 | PDB:1YW8 | ||||
| Method | X-ray diffraction | Resolution | 2.65 Å | Mutation | No | [4] |
| PDB Sequence |
KVQTDPPSVP
119 ICDLYPNGVF129 PKGQECEYPP139 TQDGRTAAWR149 TTSEEKKALD159 QASEEIWNDF 169 REAAEAHRQV179 RKYVMSWIKP189 GMTMIEICEK199 LEDCSRKLIK209 ENGLNAGLAF 219 PTGCSLNNCA229 AHYTPNAGDT239 TVLQYDDICK249 IDFGTHISGR259 IIDCAFTVTF 269 NPKYDTLLKA279 VKDATNTGIK289 CAGIDVRLCD299 VGEAIQEVME309 SYEVEIDGKT 319 YQVKPIRNLN329 GHSIGQYRIH339 AGKTVPIIKG349 GEATRMEEGE359 VYAIETFGST 369 GKGVVHDDME379 CSHYMKNFDV389 GHVPIRLPRT399 KHLLNVINEN409 FGTLAFCRRW 419 LDRLGESKYL429 MALKNLCDLG439 IVDPYPPLCD449 IKGSYTAQFE459 HTILLRPTCK 469 EVVSRGDDY
|
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|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .A75 or .A752 or .A753 or :3A75;style chemicals stick;color identity;select .A:219 or .A:220 or .A:230 or .A:231 or .A:262 or .A:328 or .A:329 or .A:330 or .A:331 or .A:338 or .A:339 or .A:364 or .A:366 or .A:382 or .A:384 or .A:414 or .A:444 or .A:447 or .A:459; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Human methionine aminopeptidase type 2 in complex with L- and D-methionine. Bioorg Med Chem Lett. 2006 May 15;16(10):2580-3. | ||||
| REF 2 | Structure of human methionine aminopeptidase-2 complexed with fumagillin. Science. 1998 Nov 13;282(5392):1324-7. | ||||
| REF 3 | Spiroepoxytriazoles Are Fumagillin-like Irreversible Inhibitors of MetAP2 with Potent Cellular Activity. ACS Chem Biol. 2016 Apr 15;11(4):1001-11. | ||||
| REF 4 | Discovery and optimization of anthranilic acid sulfonamides as inhibitors of methionine aminopeptidase-2: a structural basis for the reduction of a... J Med Chem. 2006 Jun 29;49(13):3832-49. | ||||
| REF 5 | 3-Amino-2-hydroxyamides and related compounds as inhibitors of methionine aminopeptidase-2. Bioorg Med Chem Lett. 2004 Feb 23;14(4):865-8. | ||||
| REF 6 | Development of sulfonamide compounds as potent methionine aminopeptidase type II inhibitors with antiproliferative properties. Bioorg Med Chem Lett. 2006 Jul 1;16(13):3574-7. | ||||
| REF 7 | Proteomics-based target identification: bengamides as a new class of methionine aminopeptidase inhibitors. J Biol Chem. 2003 Dec 26;278(52):52964-71. | ||||
| REF 8 | Discovery and Structure-Based Optimization of Next-Generation Reversible Methionine Aminopeptidase-2 (MetAP-2) Inhibitors. J Med Chem. 2019 May 23;62(10):5025-5039. | ||||
| REF 9 | Novel reversible methionine aminopeptidase-2 (MetAP-2) inhibitors based on purine and related bicyclic templates. Bioorg Med Chem Lett. 2017 Feb 1;27(3):551-556. | ||||
| REF 10 | Structure-based optimisation of orally active & reversible MetAP-2 inhibitors maintaining a tight 'molecular budget'. Bioorg Med Chem Lett. 2020 Nov 1;30(21):127533. | ||||
| REF 11 | Discovery of potent, reversible MetAP2 inhibitors via fragment based drug discovery and structure based drug design-Part 2. Bioorg Med Chem Lett. 2016 Jun 15;26(12):2779-2783. | ||||
| REF 12 | Discovery of potent, reversible MetAP2 inhibitors via fragment based drug discovery and structure based drug design-Part 1. Bioorg Med Chem Lett. 2016 Jun 15;26(12):2774-2778. | ||||
| REF 13 | 4-Aryl-1,2,3-triazole: a novel template for a reversible methionine aminopeptidase 2 inhibitor, optimized to inhibit angiogenesis in vivo. J Med Chem. 2005 Sep 8;48(18):5644-7. | ||||
| REF 14 | Highly potent inhibitors of methionine aminopeptidase-2 based on a 1,2,4-triazole pharmacophore. J Med Chem. 2007 Aug 9;50(16):3777-85. | ||||
| REF 15 | Lead optimization of methionine aminopeptidase-2 (MetAP2) inhibitors containing sulfonamides of 5,6-disubstituted anthranilic acids. Bioorg Med Chem Lett. 2007 May 15;17(10):2817-22. | ||||
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