Structure of PDB 3rqd Chain A Binding Site BS01

Receptor Information
>3rqd Chain A (length=354) Species: 9606 (Homo sapiens) [Search protein sequence] [Download receptor structure] [Download structure with residue number starting from 1] [View receptor structure]
LVPVYIYSPEYVSMCDSLAKIPKRASMVHSLIEAYALHKQMRIVKPKVAS
MEEMATFHTDAYLQHLQKVSQEYGLGYDCPATEGIFDYAAAIGGATITAA
QCLIDGMCKVAINWSGGWHHAKKDEASGFCYLNDAVLGILRLRRKFERIL
YVDLDLHHGDGVEDAFSFTSKVMTVSLHKFSPGFFPGTGDVSDVGLGKGR
YYSVNVPIQDGIQDEKYYQICESVLKEVYQAFNPKAVVLQLGADTIAGDP
MCSFNMTPVGIGKCLKYILQWQLATLILGGGGYNLANTARCWTYLTGVIL
GKTLSSEIPDHEFFTAYGPDYVLEITPSCRPDRNEPHRIQQILNYIKGNL
KHVV
Ligand information
Receptor-Ligand Complex Structure
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PDB3rqd Structural basis of the antiproliferative activity of largazole, a depsipeptide inhibitor of the histone deacetylases.
Resolution2.143 Å
Binding residue
(original residue number in PDB)		D101 H143 G151 F152 H180 F208 M274 Y306
Binding residue
(residue number reindexed from 1)		D78 H120 G128 F129 H157 F185 M251 Y283
Enzymatic activity
Enzyme Commision number 3.5.1.-
3.5.1.98: histone deacetylase.
Gene Ontology
Molecular Function
GO:0004407 histone deacetylase activity
GO:0005515 protein binding
GO:0016787 hydrolase activity
GO:0030544 Hsp70 protein binding
GO:0033558 protein lysine deacetylase activity
GO:0046872 metal ion binding
GO:0051879 Hsp90 protein binding
GO:0140297 DNA-binding transcription factor binding
GO:0160008 protein decrotonylase activity
GO:0160009 histone decrotonylase activity
Biological Process
GO:0000122 negative regulation of transcription by RNA polymerase II
GO:0006325 chromatin organization
GO:0007064 mitotic sister chromatid cohesion
GO:0031397 negative regulation of protein ubiquitination
GO:0031647 regulation of protein stability
GO:0032204 regulation of telomere maintenance
GO:0040029 epigenetic regulation of gene expression
Cellular Component
GO:0000118 histone deacetylase complex
GO:0000228 nuclear chromosome
GO:0005634 nucleus
GO:0005654 nucleoplasm
GO:0005694 chromosome
GO:0005737 cytoplasm

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Molecular Function
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Biological Process
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Cellular Component
External links
PDB RCSB:3rqd, PDBe:3rqd, PDBj:3rqd
PDBsum3rqd
PubMed21790156
UniProtQ9BY41|HDAC8_HUMAN Histone deacetylase 8 (Gene Name=HDAC8)

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