Structure of PDB 3f81 Chain A

Receptor sequence
>3f81A (length=179) Species: 9606 (Homo sapiens) [Search protein sequence]
LSVQDLNDLLSDGSGCYSLPSQPCNEVTPRIYVGNASVAQDIPKLQKLGI
THVLNAAEGRSFMHVNTNANFYKDSGITYLGIKANDTQEFNLSAYFERAA
DFIDQALAQKNGRVLVHCREGYSRSPTLVIAYLMMRQKMDVKSALSIVRQ
NREIGPNDGFLAQLCQLNDRLAKEGKLKP
3D structure
PDB3f81 Multidentate small-molecule inhibitors of vaccinia H1-related (VHR) phosphatase decrease proliferation of cervix cancer cells.
ChainA
Resolution1.9 Å
3D
structure
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Enzymatic activity
Enzyme Commision number 3.1.3.16: protein-serine/threonine phosphatase.
3.1.3.48: protein-tyrosine-phosphatase.
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 STT A M69 D92 C124 R125 E126 Y128 S129 R130 M63 D86 C118 R119 E120 Y122 S123 R124 MOAD: ic50=0.074uM
PDBbind-CN: -logKd/Ki=7.13,IC50=74nM
Gene Ontology
Molecular Function
GO:0004721 phosphoprotein phosphatase activity
GO:0004722 protein serine/threonine phosphatase activity
GO:0004725 protein tyrosine phosphatase activity
GO:0005515 protein binding
GO:0008092 cytoskeletal protein binding
GO:0008138 protein tyrosine/serine/threonine phosphatase activity
GO:0016791 phosphatase activity
GO:0017018 myosin phosphatase activity
GO:0019901 protein kinase binding
GO:0030971 receptor tyrosine kinase binding
GO:0033549 MAP kinase phosphatase activity
GO:1990782 protein tyrosine kinase binding
Biological Process
GO:0006470 protein dephosphorylation
GO:0016311 dephosphorylation
GO:0030336 negative regulation of cell migration
GO:0035335 peptidyl-tyrosine dephosphorylation
GO:0042059 negative regulation of epidermal growth factor receptor signaling pathway
GO:0043409 negative regulation of MAPK cascade
GO:0045931 positive regulation of mitotic cell cycle
GO:0046329 negative regulation of JNK cascade
GO:0050860 negative regulation of T cell receptor signaling pathway
GO:0050868 negative regulation of T cell activation
GO:0050922 negative regulation of chemotaxis
GO:0051893 regulation of focal adhesion assembly
GO:0070373 negative regulation of ERK1 and ERK2 cascade
GO:0071364 cellular response to epidermal growth factor stimulus
GO:0120183 positive regulation of focal adhesion disassembly
GO:1990264 peptidyl-tyrosine dephosphorylation involved in inactivation of protein kinase activity
Cellular Component
GO:0001772 immunological synapse
GO:0005634 nucleus
GO:0005654 nucleoplasm
GO:0005737 cytoplasm
GO:0005829 cytosol
GO:0005856 cytoskeleton
GO:0031514 motile cilium

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Molecular Function

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Biological Process

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Cellular Component
External links
PDB RCSB:3f81, PDBe:3f81, PDBj:3f81
PDBsum3f81
PubMed19888758
UniProtP51452|DUS3_HUMAN Dual specificity protein phosphatase 3 (Gene Name=DUSP3)

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