Target Binding Site Detail
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T80165 | Target Info | |||
| Target Name | Short transient receptor potential channel 6 (TRPC6) | ||||
| Synonyms | TRPC6; TRP6; STrpC6 | ||||
| Target Type | Literature-reported Target | ||||
| Gene Name | TRPC6 | ||||
| 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: 7DXF Structure of BTDM-bound human TRPC6 nanodisc at 2.9 angstrom in high calcium state | ||||||
| Method | Electron microscopy | Resolution | 2.90 Å | Mutation | No | [1] |
| PDB Sequence |
LSIEEERFLD
104 AAEYGNIPVV114 RKMLEECHSL124 NVNCVDYMGQ134 NALQLAVANE144 HLEITELLLK 154 KENLSRVGDA164 LLLAISKGYV174 RIVEAILSHP184 AFAEGKRLDD205 FYAYDEDGTR 215 FSHDVTPIIL225 AAHCQEYEIV235 HTLLRKGARI245 ERPHDYFCKC255 NDCNQKQKHD 265 SFSHSRSRIN275 AYKGLASPAY285 LSLSSEDPVM295 TALELSNELA305 VLANIEKEFK 315 NDYKKLSMQC325 KDFVVGLLDL335 CRNTEEVEAI345 LNGDVETLQS355 GDHGRPNLSR 365 LKLAIKYEVK375 KFVAHPNCQQ385 QLLSIWYENL395 SGLRQQTMAV405 KFLVVLAVAI 415 GLPFLALIYW425 FAPCSKMGKI435 MRGPFMKFVA445 HAASFTIFLG455 LLVMNAADRF 465 EGTFRMKTSC490 FSWMEMLIIS500 WVIGMIWAEC510 KEIWTQGPKE520 YLFELWNMLD 530 FGMLAIFAAS540 FIARFMAFWH550 ASKAQSIIDN575 VKYYNLARIK585 WDPSDPQIIS 595 EGLYAIAVVL605 SFSRIAYILP615 ANESFGPLQI625 SLGRTVKDIF635 KFMVIFIMVF 645 VAFMIGMFNL655 YSYYIGAKQN665 EAFTTVEESF675 KTLFWAIFGL685 SEVKSVVINY 695 NHKFIENIGY705 VLYGVYNVTM715 VIVLLNMLIA725 MINSSFQEIE735 DDADVEWKFA 745 RAKLWFSYFE755 EGRTLPVPFN765 LVPRQYQKIM859 KRLIKRYVLQ869 AQIDKESDEV 879 NEGELKEIKQ889 DISSLRYELL899 EEKSQ
|
|||||
|
|
TRP391
4.055
TYR392
3.233
MET403
3.728
LYS406
3.555
PHE407
3.520
VAL410
3.692
PHE440
3.079
PHE443
4.321
ALA447
3.614
THR451
3.520
ILE506
4.721
PHE531
3.617
LEU534
4.910
ALA535
4.018
ALA538
4.403
ALA539
3.539
ILE542
3.641
|
|||||
| PDB ID: 7DXG Structure of SAR7334-bound TRPC6 at 2.9 angstrom | ||||||
| Method | Electron microscopy | Resolution | 2.90 Å | Mutation | No | [1] |
| PDB Sequence |
LSIEEERFLD
104 AAEYGNIPVV114 RKMLEECHSL124 NVNCVDYMGQ134 NALQLAVANE144 HLEITELLLK 154 KENLSRVGDA164 LLLAISKGYV174 RIVEAILSHP184 AFAEGKRLDD205 FYAYDEDGTR 215 FSHDVTPIIL225 AAHCQEYEIV235 HTLLRKGARI245 ERPHDYFCKC255 NDCNQKQKHD 265 SFSHSRSRIN275 AYKGLASPAY285 LSLSSEDPVM295 TALELSNELA305 VLANIEKEFK 315 NDYKKLSMQC325 KDFVVGLLDL335 CRNTEEVEAI345 LNGDVETLQS355 GDHGRPNLSR 365 LKLAIKYEVK375 KFVAHPNCQQ385 QLLSIWYENL395 SGLRQQTMAV405 KFLVVLAVAI 415 GLPFLALIYW425 FAPCSKMGKI435 MRGPFMKFVA445 HAASFTIFLG455 LLVMNAADRF 465 EGTLFRMKTS489 CFSWMEMLII499 SWVIGMIWAE509 CKEIWTQGPK519 EYLFELWNML 529 DFGMLAIFAA539 SFIARFMAFW549 HASKAQSIID574 NVKYYNLARI584 KWDPSDPQII 594 SEGLYAIAVV604 LSFSRIAYIL614 PANESFGPLQ624 ISLGRTVKDI634 FKFMVIFIMV 644 FVAFMIGMFN654 LYSYYIGAKQ664 NEAFTTVEES674 FKTLFWAIFG684 LSEVKSVVIN 694 YNHKFIENIG704 YVLYGVYNVT714 MVIVLLNMLI724 AMINSSFQDA738 DVEWKFARAK 748 LWFSYFEEGR758 TLPVPFNLVP768 RQYQKIMKRL862 IKRYVLQAQI872 DKESDEVNEG 882 ELKEIKQDIS892 SLRYELLEEK902 SQNTEDLAEL912 IRELGEKL
|
|||||
|
|
TRP391
3.869
TYR392
2.533
MET403
3.638
LYS406
3.673
PHE407
3.750
VAL410
3.496
PHE440
2.730
PHE443
3.783
ALA447
3.991
PHE450
4.183
THR451
2.990
LEU454
3.679
VAL458
3.532
ILE506
4.596
MET528
3.968
PHE531
3.542
GLY532
3.884
ALA535
3.811
ILE536
4.257
ALA538
4.381
ALA539
3.498
|
|||||
| PDB ID: 6UZ8 Cryo-EM structure of human TRPC6 in complex with agonist AM-0883 | ||||||
| Method | Electron microscopy | Resolution | 2.84 Å | Mutation | No | [2] |
| PDB Sequence |
AYMFSDRSTS
94 LSIEEERFLD104 AAEYGNIPVV114 RKMLEECHSL124 NVNCVDYMGQ134 NALQLAVANE 144 HLEITELLLK154 KENLSRVGDA164 LLLAISKGYV174 RIVEAILSHP184 AFAEGKRLAT 194 QDDFYAYDED212 GTRFSHDVTP222 IILAAHCQEY232 EIVHTLLRKG242 ARIERPHDYF 252 CKCNDCNQKQ262 KHDSFSHSRS272 RINAYKGLAS282 PAYLSLSSED292 PVMTALELSN 302 ELAVLANIEK312 EFKNDYKKLS322 MQCKDFVVGL332 LDLCRNTEEV342 EAILNGDVET 352 LQSGDHGRPN362 LSRLKLAIKY372 EVKKFVAHPN382 CQQQLLSIWY392 ENLSGLRQQT 402 MAVKFLVVLA412 VAIGLPFLAL422 IYWFAPCSKM432 GKIMRGPFMK442 FVAHAASFTI 452 FLGLLVMNAA462 DRFEGTKLLP472 NETSTDNAKQ482 LFRMKTSCFS492 WMEMLIISWV 502 IGMIWAECKE512 IWTQGPKEYL522 FELWNMLDFG532 MLAIFAASFI542 ARFMAFWHAS 552 KAQSIIDKVT571 LGDNVKYYNL581 ARIKWDPSDP591 QIISEGLYAI601 AVVLSFSRIA 611 YILPANESFG621 PLQISLGRTV631 KDIFKFMVIF641 IMVFVAFMIG651 MFNLYSYYIG 661 AKQNEAFTTV671 EESFKTLFWA681 IFGLSEVKSV691 VINYNHKFIE701 NIGYVLYGVY 711 NVTMVIVLLN721 MLIAMINSSF731 QEIEDDADVE741 WKFARAKLWF751 SYFEEGRTLP 761 VPFNLVRQYQ856 KIMKRLIKRY866 TTQAQIDKES876 DEVNEGELKE886 IKQDISSLRY 896 ELLEEKSQNT906 EDLAELIREL916 GEKL
|
|||||
|
|
TRP391
2.898
TYR392
2.360
MET403
3.304
LYS406
3.364
PHE407
3.624
VAL410
4.158
PHE440
3.697
PHE443
4.116
ALA447
3.815
PHE450
4.831
THR451
3.406
LEU454
3.807
PHE607
3.729
|
|||||
| PDB ID: 6UZA Cryo-EM structure of human TRPC6 in complex with antagonist AM-1473 | ||||||
| Method | Electron microscopy | Resolution | 3.08 Å | Mutation | No | [2] |
| PDB Sequence |
AYMFSDRSTS
94 LSIEEERFLD104 AAEYGNIPVV114 RKMLEECHSL124 NVNCVDYMGQ134 NALQLAVANE 144 HLEITELLLK154 KENLSRVGDA164 LLLAISKGYV174 RIVEAILSHP184 AFAEGKRLAT 194 QDDFYAYDED212 GTRFSHDVTP222 IILAAHCQEY232 EIVHTLLRKG242 ARIERPHDYF 252 CKCNDCNQKQ262 KHDSFSHSRS272 RINAYKGLAS282 PAYLSLSSED292 PVMTALELSN 302 ELAVLANIEK312 EFKNDYKKLS322 MQCKDFVVGL332 LDLCRNTEEV342 EAILNGDVET 352 LQSGDHGRPN362 LSRLKLAIKY372 EVKKFVAHPN382 CQQQLLSIWY392 ENLSGLRQQT 402 MAVKFLVVLA412 VAIGLPFLAL422 IYWFAPCSKM432 GKIMRGPFMK442 FVAHAASFTI 452 FLGLLVMNAA462 DRFEGTKLLP472 NETSTDNAKQ482 LFRMKTSCFS492 WMEMLIISWV 502 IGMIWAECKE512 IWTQGPKEYL522 FELWNMLDFG532 MLAIFAASFI542 ARFMAFWHAS 552 KAQSIIDKVT571 LGDNVKYYNL581 ARIKWDPSDP591 QIISEGLYAI601 AVVLSFSRIA 611 YILPANESFG621 PLQISLGRTV631 KDIFKFMVIF641 IMVFVAFMIG651 MFNLYSYYIG 661 AKQNEAFTTV671 EESFKTLFWA681 IFGLSEVKSV691 VINYNHKFIE701 NIGYVLYGVY 711 NVTMVIVLLN721 MLIAMINSSF731 QEIEDDADVE741 WKFARAKLWF751 SYFEEGRTLP 761 VPFNLVRQYQ856 KIMKRLIKRY866 VLQAQIDKES876 DEVNEGELKE886 IKQDISSLRY 896 ELLEEKSQNT906 EDLAELIREL916 GEKL
|
|||||
|
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:388 or .A:391 or .A:392 or .A:403 or .A:406 or .A:407 or .A:410 or .A:440 or .A:443 or .A:447 or .A:451 or .A:454 or .A:455 or .A:458 or .A:607 or .A:610 or .A:613 or .A:614 or .A:616 or .A:617 or .A:698 or .A:699 or .A:702 or .A:703 or .A:706 or .A:750; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
LEU388
4.958
TRP391
2.995
TYR392
2.362
MET403
3.948
LYS406
4.048
PHE407
3.655
VAL410
4.074
PHE440
3.613
PHE443
4.344
ALA447
4.116
THR451
3.522
LEU454
3.897
GLY455
4.288
|
|||||
| 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. | ||||
| REF 2 | Structural basis for pharmacological modulation of the TRPC6 channel. Elife. 2020 Mar 9;9:e53311. | ||||
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.