Structure of PDB 5vp1 Chain C

Receptor sequence
>5vp1C (length=313) Species: 9606 (Homo sapiens) [Search protein sequence]
IQPVAAIDSNFASFTYTPRSLPEDDTSMAILSMLQDMNFINNYKIDCPTL
ARFCLMVKKGYRDPPYHNWMHAFSVSHFCYLLYKNLELTNYLEDIEIFAL
FISCMCHDLDHRGTNNSFQGSVMERHHFAQAIAILNTHGCNIFDHFSRKD
YQRMLDLMRDIILATDLAHHLRIFKDLQKMAEVGYDRNNKQHHRLLLCLL
MTSCDLSDQTKGWKTTRKIAELIYKEFFSQGDLEKAMGNRPMEMMDREKA
YIPELQISFMEHIAMPIYKLLQDLFPKAAELYERVASNREHWTKVSHKFT
IRGLPSNNSLDFL
3D structure
PDB5vp1 Discovery of a Novel Series of Pyrazolo[1,5-a]pyrimidine-Based Phosphodiesterase 2A Inhibitors Structurally Different from N-((1S)-1-(3-Fluoro-4-(trifluoromethoxy)phenyl)-2-methoxyethyl)-7-methoxy-2-oxo-2,3-dihydropyrido[2,3-b]pyrazine-4(1H)-carboxamide (TAK-915), for the Treatment of Cognitive Disorders.
ChainC
Resolution1.86 Å
3D
structure
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Enzymatic activity
Enzyme Commision number 3.1.4.17: 3',5'-cyclic-nucleotide phosphodiesterase.
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 ZN C H660 H696 D697 D808 H71 H107 D108 D205
BS02 9GA C L770 H773 T805 D808 L809 I826 Y827 M847 L858 F862 L167 H170 T202 D205 L206 I223 Y224 M244 L255 F259 MOAD: ic50=0.51nM
Gene Ontology
Molecular Function
GO:0004114 3',5'-cyclic-nucleotide phosphodiesterase activity
GO:0008081 phosphoric diester hydrolase activity
Biological Process
GO:0007165 signal transduction

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Molecular Function
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Biological Process
External links
PDB RCSB:5vp1, PDBe:5vp1, PDBj:5vp1
PDBsum5vp1
PubMed29093293
UniProtO00408|PDE2A_HUMAN cGMP-dependent 3',5'-cyclic phosphodiesterase (Gene Name=PDE2A)

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