Binding Site Information of Target
Target General Information | Top | ||||
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Target ID | T05661 | Target Info | |||
Target Name | Lecithin-cholesterol acyltransferase (LCAT) | ||||
Synonyms | Phospholipidcholesterolacyltransferase; Phospholipid-cholesterol acyltransferase; Phosphatidylcholinesterol acyltransferase; Phosphatidylcholine-sterol acyltransferase | ||||
Target Type | Clinical trial Target | ||||
Gene Name | LCAT | ||||
Biochemical Class | Acyltransferase | ||||
UniProt ID |
Drug Binding Sites of Target | Top | |||||
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Ligand Name: 6-{4-[(4R)-4-hydroxy-6-oxo-4-(trifluoromethyl)-4,5,6,7-tetrahydro-2H-pyrazolo[3,4-b]pyridin-3-yl]piperidin-1-yl}-4-(trifluoromethyl)pyridine-3-carbonitrile | Ligand Info | |||||
Structure Description | Crystal structure of Lecithin:cholesterol acyltransferase (LCAT) in complex with isopropyl dodec-11-enylfluorophosphonate (IDFP) and a small molecule activator | PDB:6MVD | ||||
Method | X-ray diffraction | Resolution | 3.10 Å | Mutation | No | [1] |
PDB Sequence |
HTRPVILVPG
30 CLGNQLEAKL40 DKPDVVNWMC50 YRKTEDFFTI60 WLDLNMFLPL70 GVDCWIDNTR 80 VVYNRSSGLV90 SNAPGVQIRV100 PGFGKTYSVE110 YLDSSKLAGY120 LHTLVQNLVN 130 NGYVRDETVR140 AAPYDWRLEP150 GQQEEYYRKL160 AGLVEEMHAA170 YGKPVFLIGH 180 SLGCLHLLYF190 LLRQPQAWKD200 RFIDGFISLG210 APWGGSIKPM220 LVLASGDNQG 230 IPIMSSIKEE242 QRITTTSPWM252 FPSRMAWPED262 HVFISTPSFN272 YTGRDFQRFF 282 ADLHFEEGWY292 MWLQSRDLLA302 GLPAPGVEVY312 CLYGVGLPTP322 RTYIYDHGFP 332 YTDPVGVLYE342 DGDDTVATRS352 TELCGLWQGR362 QPQPVHLLPL372 HGIQHLNMVF 382 SNLTLEHINA392 ILLGAH
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Ligand Name: propan-2-yl hydrogen (R)-ethylphosphonate | Ligand Info | |||||
Structure Description | Crystal structure of Lecithin:cholesterol acyltransferase (LCAT) in complex with isopropyl dodec-11-enylfluorophosphonate (IDFP) and a small molecule activator | PDB:6MVD | ||||
Method | X-ray diffraction | Resolution | 3.10 Å | Mutation | No | [1] |
PDB Sequence |
HTRPVILVPG
30 CLGNQLEAKL40 DKPDVVNWMC50 YRKTEDFFTI60 WLDLNMFLPL70 GVDCWIDNTR 80 VVYNRSSGLV90 SNAPGVQIRV100 PGFGKTYSVE110 YLDSSKLAGY120 LHTLVQNLVN 130 NGYVRDETVR140 AAPYDWRLEP150 GQQEEYYRKL160 AGLVEEMHAA170 YGKPVFLIGH 180 SLGCLHLLYF190 LLRQPQAWKD200 RFIDGFISLG210 APWGGSIKPM220 LVLASGDNQG 230 IPIMSSIKEE242 QRITTTSPWM252 FPSRMAWPED262 HVFISTPSFN272 YTGRDFQRFF 282 ADLHFEEGWY292 MWLQSRDLLA302 GLPAPGVEVY312 CLYGVGLPTP322 RTYIYDHGFP 332 YTDPVGVLYE342 DGDDTVATRS352 TELCGLWQGR362 QPQPVHLLPL372 HGIQHLNMVF 382 SNLTLEHINA392 ILLGAH
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References | Top | ||||
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REF 1 | Molecular basis for activation of lecithin:cholesterol acyltransferase by a compound that increases HDL cholesterol. Elife. 2018 Nov 27;7:e41604. |
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