Structure of PDB 5zz2 Chain A

Receptor sequence
>5zz2A (length=299) Species: 9606 (Homo sapiens) [Search protein sequence]
EETRELQSLAAAVVPSAQTLKITDFSFSDFELSDLETALCTIRMFTDLNL
VQNFQMKHEVLCRWILSVKKNYRKNVAYHNWRHAFNTAQCMFAALKAGKI
QNKLTDLEILALLIAALSHDLDHRGVNNSYIQCHSIMEHHHFDQCLMILN
SPGNQILSGLSIEEYKTTLKIIKQAILATDLALYIKRRGEFFELIRKNQF
NLEDPHQKELFLAMLMTACDLSAITKPWPIQQRIAELVATEFFDQGEKKN
KIPSMQVGFIDAICLQLYEALTHVSEDCFPLLDGCRKNRQKWQALAEQQ
3D structure
PDB5zz2 Optimization of Chromeno[2,3- c]pyrrol-9(2 H)-ones as Highly Potent, Selective, and Orally Bioavailable PDE5 Inhibitors: Structure-Activity Relationship, X-ray Crystal Structure, and Pharmacodynamic Effect on Pulmonary Arterial Hypertension.
ChainA
Resolution2.6 Å
3D
structure
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Enzymatic activity
Enzyme Commision number 3.1.4.35: 3',5'-cyclic-GMP 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 A H617 H653 D654 D764 H83 H119 D120 D220
BS02 9M0 A L725 A767 I768 Q775 A783 F786 F787 Q817 F820 L181 A223 I224 Q231 A239 F242 F243 Q256 F259 PDBbind-CN: -logKd/Ki=8.85,IC50=1.41nM
BindingDB: IC50=1.4nM
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:5zz2, PDBe:5zz2, PDBj:5zz2
PDBsum5zz2
PubMed30148362
UniProtO76074|PDE5A_HUMAN cGMP-specific 3',5'-cyclic phosphodiesterase (Gene Name=PDE5A)

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