Structure of PDB 8b8x Chain A Binding Site BS01

Receptor Information

>8b8x Chain A (length=268) Species: 9606 (Homo sapiens) [Search protein sequence] [Download receptor structure] [Download structure with residue number starting from 1] [View receptor structure]

HMQLNPESADLRALAKHLYDSYIKSFPLTKAKARAILTGKTTDKSPFVIY
DMNSLMMGEDKIKFKHEQSKEVAIRIFQGCQFRSVEAVQEITEYAKSIPG
FVNLDLNDQVTLLKYGVHEIIYTMLASLMNKDGVLISEGQGFMTREFLKS
LRKPFGDFMEPKFEFAVKFNALELDDSDLAIFIAVIILSGDRPGLLNVKP
IEDIQDNLLQALELQLKLNHPESSQLFAKLLQKMTDLRQIVTEHVQLLQV
IKKTETDMSLHPLLQEIY

Ligand information

>8b8x Chain C (length=12) Species: 9606 (Homo sapiens) [Search peptide sequence] [Download ligand structure] [Download structure with residue number starting from 1] [View ligand structure]

MGLEAIIRKALM

Receptor-Ligand Complex Structure

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Structure summary

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PDB	8b8x Discovery and characterization of orally bioavailable 4-chloro-6-fluoroisophthalamides as covalent PPARG inverse-agonists.
Resolution	1.78 Å
Binding residue (original residue number in PDB)	V293 T297 K301 V315 L318 K319 L468 I472
Binding residue (residue number reindexed from 1)	V88 T92 K96 V110 L113 K114 L263 I267

Enzymatic activity

Enzyme Commision number

Gene Ontology

	Molecular Function
GO:0003677	DNA binding
GO:0004879	nuclear receptor activity

	Biological Process
GO:0006355	regulation of DNA-templated transcription

	Cellular Component
GO:0005634	nucleus

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Cellular Component

External links

PDB	RCSB:8b8x, PDBe:8b8x, PDBj:8b8x
PDBsum	8b8x
PubMed	36542958
UniProt	P37231\|PPARG_HUMAN Peroxisome proliferator-activated receptor gamma (Gene Name=PPARG)

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