Binding Site Information of Target
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T77548 | Target Info | |||
| Target Name | Metabotropic glutamate receptor 8 (mGluR8) | ||||
| Synonyms | MGluR8a; MGLUR8; Glutamate receptor mGLU8; GRM8 | ||||
| Target Type | Literature-reported Target | ||||
| Gene Name | GRM8 | ||||
| Biochemical Class | GPCR glutamate | ||||
| UniProt ID | |||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| Ligand Name: (S)-3,4-DCPG | Ligand Info | |||||
| Structure Description | human mGlu8 receptor amino terminal domain in complex with (S)-3,4-Dicarboxyphenylglycine (DCPG) | PDB:6E5V | ||||
| Method | X-ray diffraction | Resolution | 2.95 Å | Mutation | Yes | [1] |
| PDB Sequence |
HSIRVDGDII
47 LGGLFPVHAK57 GERGVPCGEL67 KKEKGIHRLE77 AMLYAIDQIN87 KDPDLLSNIT 97 LGVRILDTCS107 RDTYALEQSL117 TFVQALIPDK146 ISGVIGAAAS156 SVSIMVANIL 166 RLFKIPQISY176 ASTAPELSDN186 TRYDFFSRVV196 PPDSYQAQAM206 VDIVTALGWN 216 YVSTLASEGN226 YGESGVEAFT236 QISREIGGVS246 IAQSQKIPRE256 PRPGEFEKII 266 KRLLETPNAR276 AVIMFANEDD286 IRRILEAAKK296 LNQSGHFLWI306 GSDSWGSKIA 316 PVYQQEEIAE326 GAVTILPKRA336 SIDGFDRYFR346 SRTLANNRRN356 VWFAEFWEEN 366 FGCKLCTGLE388 RIARDSSYEQ398 EGKVQFVIDA408 VYSMAYALHN418 MHKDLCPGYI 428 GLCPRMSTID438 GKELLGYIRA448 VNFNGSAGTP458 VTFNENGDAP468 GRYDIFQYQI 478 TSTEYKVIGH490 WTNQLHLKVE500 DMQWA
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| Ligand Name: L-AP4 | Ligand Info | |||||
| Structure Description | Human mGlu8 Receptor complexed with L-AP4 | PDB:6BT5 | ||||
| Method | X-ray diffraction | Resolution | 2.92 Å | Mutation | No | [2] |
| PDB Sequence |
AHSIRVDGDI
46 ILGGLFPVHA56 KGERGVPCGE66 LKKEKGIHRL76 EAMLYAIDQI86 NKDPDLLSNI 96 TLGVRILDTC106 SRDTYALEQS116 LTFVQKISGV150 IGAAASSVSI160 MVANILRLFK 170 IPQISYASTA180 PELSDNTRYD190 FFSRVVPPDS200 YQAQAMVDIV210 TALGWNYVST 220 LASEGNYGES230 GVEAFTQISR240 EIGGVSIAQS250 QKIPREPRPG260 EFEKIIKRLL 270 ETPNARAVIM280 FANEDDIRRI290 LEAAKKLNQS300 GHFLWIGSDS310 WGSKIAPVYQ 320 QEEIAEGAVT330 ILPKRASIDG340 FDRYFRSRTL350 ANNRRNVWFA360 EFWEENFGCK 370 LKCTGLERIA391 RDSSYEQEGK401 VQFVIDAVYS411 MAYALHNMHK421 DLCPGYIGLC 431 PRMSTIDGKE441 LLGYIRAVNF451 NGSAGTPVTF461 NENGDAPGRY471 DIFQYQITNK 481 STEYKVIGHW491 TNQLHLKVED501 MQWAHRTHPA513 SE
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| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Structural Basis for ( S)-3,4-Dicarboxyphenylglycine (DCPG) As a Potent and Subtype Selective Agonist of the mGlu(8) Receptor. J Med Chem. 2018 Nov 21;61(22):10040-10052. | ||||
| REF 2 | Determination of L-AP4-bound human mGlu8 receptor amino terminal domain structure and the molecular basis for L-AP4's group III mGlu receptor functional potency and selectivity. Bioorg Med Chem Lett. 2018 Feb 15;28(4):612-617. | ||||
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