Structure of PDB 2hfp Chain A

Receptor sequence
>2hfpA (length=272) Species: 9606 (Homo sapiens) [Search protein sequence]
PESADLRALAKHLYDSYIKSFPLTKAKARAILTGKTTDKSPFVIYDMNSL
MMGEDKIKFKHITPLQEQSKEVAIRIFQGCQFRSVEAVQEITEYAKSIPG
FVNLDLNDQVTLLKYGVHEIIYTMLASLMNKDGVLISEGQGFMTREFLKS
LRKPFGDFMEPKFEFAVKFNALELDDSDLAIFIAVIILSGDRPGLLNVKP
IEDIQDNLLQALELQLKLNHPESSQLFAKLLQKMTDLRQIVTEHVQLLQV
IKKTETDMSLHPLLQEIYKDLY
3D structure
PDB2hfp Design and synthesis of novel N-sulfonyl-2-indole carboxamides as potent PPAR-gamma binding agents with potential application to the treatment of osteoporosis.
ChainA
Resolution2.0 Å
3D
structure
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Enzymatic activity
Enzyme Commision number ?
Interaction with ligand
Site
#
Ligand Ligand
chain
Binding residues on receptor
(original residue number in PDB)
Binding residues on receptor
(residue number reindexed from 1)
Binding affinity
BS01 peptide A K301 V315 L318 K319 L468 E471 K96 V110 L113 K114 L263 E266
BS02 NSI A E259 K265 H266 I281 G284 C285 R288 L330 I341 S342 E54 K60 H61 I76 G79 C80 R83 L125 I136 S137 MOAD: ic50=3nM
PDBbind-CN: -logKd/Ki=8.52,IC50=3nM
BindingDB: IC50=3nM
BS03 NSI A C285 Q286 S289 H323 Y327 F360 F363 M364 K367 H449 L452 L453 Y473 C80 Q81 S84 H118 Y122 F155 F158 M159 K162 H244 L247 L248 Y268 MOAD: ic50=3nM
PDBbind-CN: -logKd/Ki=8.52,IC50=3nM
BindingDB: IC50=3nM
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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Molecular Function

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Biological Process

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Cellular Component
External links
PDB RCSB:2hfp, PDBe:2hfp, PDBj:2hfp
PDBsum2hfp
PubMed16919947
UniProtP37231|PPARG_HUMAN Peroxisome proliferator-activated receptor gamma (Gene Name=PPARG)

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