Target Binding Site Detail
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T25861 | Target Info | |||
| Target Name | Short transient receptor potential channel 3 (TRPC3) | ||||
| Synonyms | TrpC3; Htrp3; Htrp-3 | ||||
| Target Type | Literature-reported Target | ||||
| Gene Name | TRPC3 | ||||
| Biochemical Class | Transient receptor potential catioin channel | ||||
| UniProt ID | |||||
| Ligand General Information | Top | ||||
|---|---|---|---|---|---|
| Ligand Name | Cholesterol hemisuccinate | Ligand Info | |||
| Canonical SMILES | CC(C)CCCC(C)C1CCC2C1(CCC3C2CC=C4C3(CCC(C4)OC(=O)CCC(=O)O)C)C | ||||
| InChI | 1S/C31H50O4/c1-20(2)7-6-8-21(3)25-11-12-26-24-10-9-22-19-23(35-29(34)14-13-28(32)33)15-17-30(22,4)27(24)16-18-31(25,26)5/h9,20-21,23-27H,6-8,10-19H2,1-5H3,(H,32,33)/t21-,23+,24+,25-,26+,27+,30+,31-/m1/s1 | ||||
| InChIKey | WLNARFZDISHUGS-MIXBDBMTSA-N | ||||
| PubChem Compound ID | 65082 | ||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| PDB ID: 7DXB Structure of TRPC3 at 2.7 angstrom in high calcium state | ||||||
| Method | Electron microscopy | Resolution | 2.70 Å | Mutation | No | [1] |
| PDB Sequence |
GPAFMFNTSL
24 TAEEERFLDA34 AEYGNIPVVR44 KMLEESKTLN54 VNCVDYMGQN64 ALQLAVGNEH 74 LEVTELLLKK84 ENLARIGDAL94 LLAISKGYVR104 IVEAILNHPG114 FAASKRLTLS 124 PCEQELQDDD134 FYAYDEDGTR144 FSPDITPIIL154 AAHCQKYEVV164 HMLLMKGARI 174 ERPHDYFCKC184 GDCMEKQRHD194 SFSHSRSRIN204 AYKGLASPAY214 LSLSSEDPVL 224 TALELSNELA234 KLANIEKEFK244 NDYRKLSMQC254 KDFVVGVLDL264 CRDSEEVEAI 274 LNGDASLSRV297 KLAIKYEVKK307 FVAHPNCQQQ317 LLTIWYENLS327 GLREQTIAIK 337 CLVVLVVALG347 LPFLAIGYWI357 APCSRLGKIL367 RSPFMKFVAH377 AASFIIFLGL 387 LVFNASDRFE397 GITTLPNITV407 TDYPKQIFRV417 KTTQFTWTEM427 LIMVWVLGMM 437 WSECKELWLE447 GPREYILQLW457 NVLDFGMLSI467 FIAAFTARFL477 AFLQATKAQQ 487 YVDSYVQESD497 LSEVTLPPEI507 QYFTYARDKW517 LPSDPQIISE527 GLYAIAVVLS 537 FSRIAYILPA547 NESFGPLQIS557 LGRTVKDIFK567 FMVLFIMVFF577 AFMIGMFILY 587 SYYLGAKVNA597 AFTTVEESFK607 TLFWSIFGLS617 EVTSVVLKYD627 HKFIENIGYV 637 LYGIYNVTMV647 VVLLNMLIAM657 INSSYQEIED667 DSDVEWKFAR677 SKLWLSYFDD 687 GKTLPPPFSL697 VPQPTRYQQI766 MKRLIKRYVL776 KAQVDKENDE786 VNEGELKEIK 796 QDISSLRYEL806 LEDKSQATEE816 LAILIHKL
|
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|
TRP322
3.952
TYR323
2.864
ILE334
4.771
LYS337
3.493
CYS338
4.952
VAL341
3.647
PHE371
3.225
PHE374
3.983
ALA378
4.703
ILE382
3.543
MET437
3.713
PHE462
4.438
SER466
4.844
ILE469
4.007
ALA470
3.599
|
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| PDB ID: 7DXC Structure of TRPC3 at 3.06 angstrom in low calcium state | ||||||
| Method | Electron microscopy | Resolution | 3.06 Å | Mutation | No | [1] |
| PDB Sequence |
TSLTAEEERF
31 LDAAEYGNIP41 VVRKMLEESK51 TLNVNCVDYM61 GQNALQLAVG71 NEHLEVTELL 81 LKKENLARIG91 DALLLAISKG101 YVRIVEAILN111 HPGFAASKRL121 TLSPCEQELQ 131 DDDFYAYDED141 GTRFSPDITP151 IILAAHCQKY161 EVVHMLLMKG171 ARIERPHDYF 181 CKCGDCMEKQ191 RHDSFSHSRS201 RINAYKGLAS211 PAYLSLSSED221 PVLTALELSN 231 ELAKLANIEK241 EFKNDYRKLS251 MQCKDFVVGV261 LDLCRDSEEV271 EAILNGDSLS 295 RVKLAIKYEV305 KKFVAHPNCQ315 QQLLTIWYEN325 LSGLREQTIA335 IKCLVVLVVA 345 LGLPFLAIGY355 WIAPCSRLGK365 ILRSPFMKFV375 AHAASFIIFL385 GLLVFNASDR 395 FEGITTLPNI405 TVTDYPKQIF415 RVKTTQFTWT425 EMLIMVWVLG435 MMWSECKELW 445 LEGPREYILQ455 LWNVLDFGML465 SIFIAAFTAR475 FLAFLQATKA485 QQYVDSYVQE 495 SDLSEVTLPP505 EIQYFTYARD515 KWLPSDPQII525 SEGLYAIAVV535 LSFSRIAYIL 545 PANESFGPLQ555 ISLGRTVKDI565 FKFMVLFIMV575 FFAFMIGMFI585 LYSYYLGAKV 595 NAAFTTVEES605 FKTLFWSIFG615 LSEVTSVVLK625 YDHKFIENIG635 YVLYGIYNVT 645 MVVVLLNMLI655 AMINSSYDDS669 DVEWKFARSK679 LWLSYFDKTL691 PPPFSLVPQP 760 TRYQQIMKRL770 IKRYVLKAQV780 DKENDEVNEG790 ELKEIKQDIS800 SL |
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|
|
TYR323
3.467
ILE334
3.343
LYS337
3.629
CYS338
4.199
VAL341
4.512
PHE371
3.351
PHE374
4.329
ILE382
3.698
MET437
3.633
PHE462
4.062
SER466
4.131
ILE469
4.406
ALA470
3.596
THR473
3.619
ALA474
3.808
|
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| PDB ID: 7DXE Structure of TRPC3 gain of function mutation R803C at 3.2 angstrom in 1340nM free calcium state | ||||||
| Method | Electron microscopy | Resolution | 3.20 Å | Mutation | No | [1] |
| PDB Sequence |
TSLTAEEERF
31 LDAAEYGNIP41 VVRKMLEESK51 TLNVNCVDYM61 GQNALQLAVG71 NEHLEVTELL 81 LKKENLARIG91 DALLLAISKG101 YVRIVEAILN111 HPGFAASKRL121 TLSPCEQELQ 131 DDDFYAYDED141 GTRFSPDITP151 IILAAHCQKY161 EVVHMLLMKG171 ARIERPHDYF 181 CKCGDCMEKQ191 RHDSFSHSRS201 RINAYKGLAS211 PAYLSLSSED221 PVLTALELSN 231 ELAKLANIEK241 EFKNDYRKLS251 MQCKDFVVGV261 LDLCRDSEEV271 EAILNGDSLS 295 RVKLAIKYEV305 KKFVAHPNCQ315 QQLLTIWYEN325 LSGLREQTIA335 IKCLVVLVVA 345 LGLPFLAIGY355 WIAPCSRLGK365 ILRSPFMKFV375 AHAASFIIFL385 GLLVFNASDR 395 FEGITTLPNI405 TVTDYPKQIF415 RVKTTQFTWT425 EMLIMVWVLG435 MMWSECKELW 445 LEGPREYILQ455 LWNVLDFGML465 SIFIAAFTAR475 FLAFLQATKA485 QQYVDSYVQE 495 SDLSEVTLPP505 EIQYFTYARD515 KWLPSDPQII525 SEGLYAIAVV535 LSFSRIAYIL 545 PANESFGPLQ555 ISLGRTVKDI565 FKFMVLFIMV575 FFAFMIGMFI585 LYSYYLGAKV 595 NAAFTTVEES605 FKTLFWSIFG615 LSEVTSVVLK625 YDHKFIENIG635 YVLYGIYNVT 645 MVVVLLNMLI655 AMINSSYDDS669 DVEWKFARSK679 LWLSYFDKTL691 PPPFSLVPQP 760 TRYQQIMKRL770 IKRYVLKAQV780 DKEND
|
|||||
|
|
TYR323
3.514
ILE334
4.615
LYS337
3.627
CYS338
4.517
VAL341
4.220
PHE371
3.263
PHE374
4.664
ILE382
3.576
LEU385
3.729
MET437
4.874
PHE462
3.860
SER466
3.879
ILE469
3.805
ALA470
3.446
|
|||||
| PDB ID: 7DXD Structure of TRPC3 at 3.9 angstrom in 1340 nM free calcium state | ||||||
| Method | Electron microscopy | Resolution | 3.90 Å | Mutation | No | [1] |
| PDB Sequence |
GPAFMFNTSL
24 TAEEERFLDA34 AEYGNIPVVR44 KMLEESKTLN54 VNCVDYMGQN64 ALQLAVGNEH 74 LEVTELLLKK84 ENLARIGDAL94 LLAISKGYVR104 IVEAILNHPG114 FAASKRLTLS 124 PCEQELQDDD134 FYAYDEDGTR144 FSPDITPIIL154 AAHCQKYEVV164 HMLLMKGARI 174 ERPHDYFCKC184 GDCMEKQRHD194 SFSHSRSRIN204 AYKGLASPAY214 LSLSSEDPVL 224 TALELSNELA234 KLANIEKEFK244 NDYRKLSMQC254 KDFVVGVLDL264 CRDSEEVEAI 274 LNGDASLSRV297 KLAIKYEVKK307 FVAHPNCQQQ317 LLTIWYENLS327 GLREQTIAIK 337 CLVVLVVALG347 LPFLAIGYWI357 APCSRLGKIL367 RSPFMKFVAH377 AASFIIFLGL 387 LVFNASDRFE397 GITTLPNITV407 TDYPKQIFRV417 KTTQFTWTEM427 LIMVWVLGMM 437 WSECKELWLE447 GPREYILQLW457 NVLDFGMLSI467 FIAAFTARFL477 AFLQATKAQQ 487 YVDSYVQESD497 LSEVTLPPEI507 QYFTYARDKW517 LPSDPQIISE527 GLYAIAVVLS 537 FSRIAYILPA547 NESFGPLQIS557 LGRTVKDIFK567 FMVLFIMVFF577 AFMIGMFILY 587 SYYLGAKVNA597 AFTTVEESFK607 TLFWSIFGLS617 EVTSVVLKYD627 HKFIENIGYV 637 LYGIYNVTMV647 VVLLNMLIAM657 INSSYQEDSD670 VEWKFARSKL680 WLSYFDDLPP 693 PFSLVPQPTR762 YQQIMKRLIK772 RYVLKAQVDK782 ENDEVNEGEL792 KEIKQDISSL 802 RYELLEDKSQ812 ATEELAILIH822 KL
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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 .Y01 or .Y012 or .Y013 or :3Y01;style chemicals stick;color identity;select .A:322 or .A:323 or .A:334 or .A:337 or .A:338 or .A:341 or .A:371 or .A:374 or .A:378 or .A:382 or .A:541 or .A:544 or .A:545 or .A:547 or .A:548 or .A:549 or .A:681; 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 | Structural mechanism of human TRPC3 and TRPC6 channel regulation by their intracellular calcium-binding sites. Neuron. 2022 Mar 16;110(6):1023-1035.e5. | ||||
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