Binding Site Information of Target
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T04980 | Target Info | |||
| Target Name | EZH2 Y641N mutant (EZH2 Y641N) | ||||
| Synonyms | Lysine Nmethyltransferase 6 Y641N mutant; Lysine N-methyltransferase 6 Y641N mutant; KMT6 Y641N mutant; Histonelysine Nmethyltransferase EZH2 Y641N mutant; Histone-lysine N-methyltransferase EZH2 Y641N mutant; EZH2 Y641N mutations; ENX1 Y641N mutant; ENX-1 Y641N mutant | ||||
| Target Type | Patented-recorded Target | ||||
| Gene Name | EZH2 | ||||
| UniProt ID | |||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| Ligand Name: 5,8-Dichloro-2-[(4-Ethyl-6-Methyl-2-Oxo-1,2-Dihydropyridin-3-Yl)methyl]-7-({1-[(2r)-2-Hydroxypropanoyl]piperidin-4-Yl}oxy)-3,4-Dihydroisoquinolin-1(2h)-One | Ligand Info | |||||
| Structure Description | Structure of the primary oncogenic mutant Y641N Hs/AcPRC2 in complex with a pyridone inhibitor | PDB:5IJ8 | ||||
| Method | X-ray diffraction | Resolution | 2.99 Å | Mutation | Yes | [1] |
| PDB Sequence |
EKGPICWRKR
18 VKSEYMRLRQ28 LKRFRRADEV38 KSMFNSNRQK48 IQERTEILNQ58 EWKQRRIQPV 68 HIMRECSVTS87 DLDFPKQVIP97 LKTLNAVASV107 PIMYSWSPLQ117 QNFMVEDIND 168 EIFVELVNAL178 GQLDRRDEKP219 SDKIFEAISS229 MFPDKGTAEE239 LKEKYKECTP 262 NIDGPNAKSV272 QREQSLHSFH282 TLFCRRCFKY292 DCFLHPFHAT302 PNTYKRWSGA 435 EASMFRVLIG445 TYYDNFCAIA455 RLIGTKTCRQ465 VYEFRVKVYN519 YQPCDHPRQP 529 CDNSCPCVIA539 QNFCEKFCQC549 SSECQNRFPG559 CRCKAQCNTK569 QCPCYLAVRE 579 CDPDLCLTCG589 AADHWDSKNV599 SCKNCSIQRG609 SKKHLLLAPS619 DVAGWGIFIK 629 DPVQKNEFIS639 ENCGEIISQD649 EADRRGKVYD659 KYMCSFLFNL669 NNDFVVDATR 679 KGNKIRFANH689 SVNPNCYAKV699 MMVNGDHRIG709 IFAKRAIQTG719 EELFFDYRYS 729 QADA
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| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Polycomb repressive complex 2 structure with inhibitor reveals a mechanism of activation and drug resistance. Nat Commun. 2016 Apr 28;7:11384. | ||||
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