Structure of PDB 3hdz Chain A

Receptor sequence
>3hdzA (length=323) Species: 9606 (Homo sapiens) [Search protein sequence]
TRELQSLAAAVVPSAQTLKITDFSFSDFELSDLETALCTIRMFTDLNLVQ
NFQMKHEVLCRWILSVKKNYRKNVAYHNWRHAFNTAQCMFAALKAGKIQN
KLTDLEILALLIAALSHDLDHPGVSNQFLINTNSELALMYNDESVLEHHH
FDQCLMILNSPGNQILSGLSIEEYKTTLKIIKQAILATDLALYIKRRGEF
FELIRKNQFNLEDPHEKELFLAMLMTACDLSAITKPWPIQQRIAELVATE
FFDQGDRERKELNIEPTDLMNREKKNKIPSMQVGFIDAICLQLYEALTHV
SEDCFPLLDGCRKNRQKWQALAE
3D structure
PDB3hdz Identification, synthesis and SAR of amino substituted pyrido[3,2b]pyrazinones as potent and selective PDE5 inhibitors.
ChainA
Resolution1.8 Å
3D
structure
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Enzymatic activity
Enzyme Commision number 3.1.4.35: 3',5'-cyclic-GMP phosphodiesterase.
3.1.4.53: 3',5'-cyclic-AMP 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 PD6 A A767 I768 L804 M816 Q817 F820 A232 I233 L269 M281 Q282 F285 MOAD: ic50=51nM
PDBbind-CN: -logKd/Ki=7.29,IC50=51nM
BS02 ZN A H617 H653 D654 D764 H81 H117 D118 D229
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:3hdz, PDBe:3hdz, PDBj:3hdz
PDBsum3hdz
PubMed19540112
UniProtO76074|PDE5A_HUMAN cGMP-specific 3',5'-cyclic phosphodiesterase (Gene Name=PDE5A);
P27815|PDE4A_HUMAN 3',5'-cyclic-AMP phosphodiesterase 4A (Gene Name=PDE4A)

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