Binding Site Information of Target
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T08910 | Target Info | |||
| Target Name | GABA(A) receptor gamma-2 (GABRG2) | ||||
| Synonyms | Gamma-aminobutyric acid receptor subunit gamma-2; GABA(A) receptor subunit gamma-2 | ||||
| Target Type | Successful Target | ||||
| Gene Name | GABRG2 | ||||
| Biochemical Class | Neurotransmitter receptor | ||||
| UniProt ID | |||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| Ligand Name: Diazepam | Ligand Info | |||||
| Structure Description | Human GABAA receptor alpha1-beta2-gamma2 subtype in complex with GABA plus diazepam | PDB:6X3X | ||||
| Method | Electron microscopy | Resolution | 2.92 Å | Mutation | No | [1] |
| PDB Sequence |
GDVTVILNNL
34 LEGYDNKLRP44 DIGVKPTLIH54 TDMYVNSIGP64 VNAINMEYTI74 DIFFAQTWYD 84 RRLKFNSTIK94 VLRLNSNMVG104 KIWIPDTFFR114 NSKKADAHWI124 TTPNRMLRIW 134 NDGRVLYTLR144 LTIDAECQLQ154 LHNFPMDEHS164 CPLEFSSYGY174 PREEIVYQWK 184 RSSVEVGDTR194 SWRLYQFSFV204 GLRNTTEVVK214 TTSGDYVVMS224 VYFDLSRRMG 234 YFTIQTYIPC244 TLIVVLSWVS254 FWINKDAVPA264 RTSLGITTVL274 TMTTLSTIAR 284 KSLPKVSYVT294 AMDLFVSVCF304 IFVFSALVEY314 GTLHYFVSSQ324 PARAAKMDSY 334 ARIFFPTAFC344 LFNLVYWVSY354 LYL
|
|||||
|
|
||||||
| Ligand Name: Phenobarbital | Ligand Info | |||||
| Structure Description | Human GABAA receptor alpha1-beta2-gamma2 subtype in complex with GABA plus phenobarbital | PDB:6X3W | ||||
| Method | Electron microscopy | Resolution | 3.30 Å | Mutation | No | [1] |
| PDB Sequence |
GDVTVILNNL
34 LEGYDNKLRP44 DIGVKPTLIH54 TDMYVNSIGP64 VNAINMEYTI74 DIFFAQTWYD 84 RRLKFNSTIK94 VLRLNSNMVG104 KIWIPDTFFR114 NSKKADAHWI124 TTPNRMLRIW 134 NDGRVLYTLR144 LTIDAECQLQ154 LHNFPMDEHS164 CPLEFSSYGY174 PREEIVYQWK 184 RSSVEVGDTR194 SWRLYQFSFV204 GLRNTTEVVK214 TTSGDYVVMS224 VYFDLSRRMG 234 YFTIQTYIPC244 TLIVVLSWVS254 FWINKDAVPA264 RTSLGITTVL274 TMTTLSTIAR 284 KSLPKVSYVT294 AMDLFVSVCF304 IFVFSALVEY314 GTLHYFVSSQ324 PARAAKMDSY 334 ARIFFPTAFC344 LFNLVYWVSY354 LYL
|
|||||
|
|
||||||
| Ligand Name: Picrotoxinin | Ligand Info | |||||
| Structure Description | CryoEM structure of human full-length heteromeric alpha1beta3gamma2L GABA(A)R in complex with picrotoxin, GABA and megabody Mb38. | PDB:6HUJ | ||||
| Method | Electron microscopy | Resolution | 3.04 Å | Mutation | No | [2] |
| PDB Sequence |
DVTVILNNLL
35 EGYDNKLRPD45 IGVKPTLIHT55 DMYVNSIGPV65 NAINMEYTID75 IFFAQTWYDR 85 RLKFNSTIKV95 LRLNSNMVGK105 IWIPDTFFRN115 SKKADAHWIT125 TPNRMLRIWN 135 DGRVLYTLRL145 TIDAECQLQL155 HNFPMDEHSC165 PLEFSSYGYP175 REEIVYQWKR 185 SSVEVGDTRS195 WRLYQFSFVG205 LRNTTEVVKT215 TSGDYVVMSV225 YFDLSRRMGY 235 FTIQTYIPCT245 LIVVLSWVSF255 WINKDAVPAR265 TSLGITTVLT275 MTTLSTIARK 285 SLPKVSYVTA295 MDLFVSVCFI305 FVFSALVEYG315 TLHYFVSNRR406 IAKMDSYARI 416 FFPTAFCLFN426 LVYWVSYLYL436
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .RI5 or .RI52 or .RI53 or :3RI5;style chemicals stick;color identity;select .C:267 or .C:270 or .C:271 or .C:274; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
||||||
| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| Ligand Name: Alpha-D-Mannose | Ligand Info | |||||
| Structure Description | Human GABAA receptor alpha1-beta2-gamma2 subtype in complex with bicuculline methbromide | PDB:6X3S | ||||
| Method | Electron microscopy | Resolution | 3.12 Å | Mutation | No | [1] |
| PDB Sequence |
GDVTVILNNL
34 LEGYDNKLRP44 DIGVKPTLIH54 TDMYVNSIGP64 VNAINMEYTI74 DIFFAQTWYD 84 RRLKFNSTIK94 VLRLNSNMVG104 KIWIPDTFFR114 NSKKADAHWI124 TTPNRMLRIW 134 NDGRVLYTLR144 LTIDAECQLQ154 LHNFPMDEHS164 CPLEFSSYGY174 PREEIVYQWK 184 RSSVEVGDTR194 SWRLYQFSFV204 GLRNTTEVVK214 TTSGDYVVMS224 VYFDLSRRMG 234 YFTIQTYIPC244 TLIVVLSWVS254 FWINKDAVPA264 RTSLGITTVL274 TMTTLSTIAR 284 KSLPKVSYVT294 AMDLFVSVCF304 IFVFSALVEY314 GTLHYFVSSQ324 PARAAKMDSY 334 ARIFFPTAFC344 LFNLVYWVSY354 LYL
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .MAN or .MAN2 or .MAN3 or :3MAN;style chemicals stick;color identity;select .E:118 or .E:119 or .E:120; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
||||||
| Ligand Name: Cholesterol hemisuccinate | Ligand Info | |||||
| Structure Description | Human GABA-A receptor alpha1-beta2-gamma2 subtype in complex with GABA and flumazenil, conformation B | PDB:6D6T | ||||
| Method | Electron microscopy | Resolution | 3.86 Å | Mutation | No | [3] |
| PDB Sequence |
.
|
|||||
|
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 .E:263 or .E:264 or .E:266; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
||||||
| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Shared structural mechanisms of general anaesthetics and benzodiazepines. Nature. 2020 Sep;585(7824):303-308. | ||||
| REF 2 | GABA(A) receptor signalling mechanisms revealed by structural pharmacology. Nature. 2019 Jan;565(7740):454-459. | ||||
| REF 3 | Structure of a human synaptic GABA(A) receptor. Nature. 2018 Jul;559(7712):67-72. | ||||
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.