Binding Site Information of Target
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T71374 | Target Info | |||
| Target Name | Polo-like kinase 4 (PLK4) | ||||
| Synonyms | Serine/threonine-protein kinase Sak; Serine/threonine-protein kinase PLK4; Serine/threonine-protein kinase 18; STK18; SAK; PLK-4 | ||||
| Target Type | Literature-reported Target | ||||
| Gene Name | PLK4 | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| Ligand Name: AMP-PNP | Ligand Info | |||||
| Structure Description | Crystal structure of PLK4 kinase | PDB:3COK | ||||
| Method | X-ray diffraction | Resolution | 2.25 Å | Mutation | No | [1] |
| PDB Sequence |
SLATCIGEKI
8 EDFKVGNLLG18 KGSFAGVYRA28 ESIHTGLEVA38 IKMIDKKAMY48 KAGMVQRVQN 58 EVKIHCQLKH68 PSILELYNYF78 EDSNYVYLVL88 EMCHNGEMNR98 YLKNRVKPFS 108 ENEARHFMHQ118 IITGMLYLHS128 HGILHRDLTL138 SNLLLTRNMN148 IKIADFGLAT 158 QLKESDVWSL196 GCMFYTLLIG206 RPPFDTDTVK216 VVLADYEMPS231 FLSIEAKDLI 241 HQLLRRNPAD251 RLSLSSVLDH261 PFMS
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| Ligand Name: Centrinone | Ligand Info | |||||
| Structure Description | Crystal Structure of Plk4 Kinase Domain Bound to Centrinone | PDB:4YUR | ||||
| Method | X-ray diffraction | Resolution | 2.65 Å | Mutation | No | [2] |
| PDB Sequence |
IGEKIEDFKV
14 GNLLGKGSFA24 GVYRAESIHT34 GLEVAIKMID44 KKAMYKAGMV54 QRVQNEVKIH 64 CQLKHPSILE74 LYNYFEDSNY84 VYLVLEMCHN94 GEMNRYLKNR104 VKPFSENEAR 114 HFMHQIITGM124 LYLHSHGILH134 RDLTLSNLLL144 TRNMNIKIAD154 FGLESDVWSL 197 GCMFYTLLIG207 RPPFTVKNTL220 NKVVLADYEM230 PSFLSIEAKD240 LIHQLLRRNP 250 ADRLSLSSVL260 DHPFMS
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| Ligand Name: (1r,2s)-2-{3-[(E)-2-{4-[(Dimethylamino)methyl]phenyl}ethenyl]-2h-Indazol-6-Yl}-5'-Methoxyspiro[cyclopropane-1,3'-Indol]-2'(1'h)-One | Ligand Info | |||||
| Structure Description | Crystal Structure of PLK4 Kinase with an inhibitor: 400631 ((1R,2S)-2-{3-[(E)-2-{4-[(DIMETHYLAMINO)METHYL]PHENYL}ETHENYL]-2H-INDAZOL-6-YL}-5'-METHOXYSPIRO[CYCLOPROPANE-1,3'-INDOL]-2'(1'H)-ONE) | PDB:4JXF | ||||
| Method | X-ray diffraction | Resolution | 2.40 Å | Mutation | No | [3] |
| PDB Sequence |
CIGEKIEDFK
13 VGNLLGKGSF23 AGVYRAESIH33 TGLEVAIKMI43 DKKAMYKAGM53 VQRVQNEVKI 63 HCQLKHPSIL73 ELYNYFEDSN83 YVYLVLEMCH93 NGEMNRYLKN103 RVKPFSENEA 113 RHFMHQIITG123 MLYLHSHGIL133 HRDLTLSNLL143 LTRNMNIKIA153 DFGLATQLKM 163 PHESDVWSLG198 CMFYTLLIGR208 PPFVKNTLNK222 VVLADYEMPS232 FLSIEAKDLI 242 HQLLRRNPAD252 RLSLSSVLDH262 PFMSR
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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 .631 or .6312 or .6313 or :3631;style chemicals stick;color identity;select .A:18 or .A:19 or .A:23 or .A:26 or .A:28 or .A:39 or .A:41 or .A:73 or .A:89 or .A:90 or .A:91 or .A:92 or .A:93 or .A:94 or .A:95 or .A:96 or .A:140 or .A:141 or .A:142 or .A:143 or .A:153 or .A:154 or .A:159 or .A:160 or .A:161; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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LEU18
3.694
GLY19
3.413
PHE23
3.605
VAL26
3.675
ARG28
4.093
ALA39
3.352
LYS41
2.752
LEU73
3.848
LEU89
3.823
GLU90
2.788
MET91
3.656
CYS92
3.075
HIS93
3.324
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| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Crystal structure of PLK4 kinase. | ||||
| REF 2 | Cell biology. Reversible centriole depletion with an inhibitor of Polo-like kinase 4. Science. 2015 Jun 5;348(6239):1155-60. | ||||
| REF 3 | Crystal Structure of PLK4 Kinase with an inhibitor: 400631 | ||||
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