Structure of PDB 4pm0 Chain A

Receptor sequence
>4pm0A (length=318) Species: 9606 (Homo sapiens) [Search protein sequence]
DYNGQAKCMLEKVGNWNFDIFLFDRLTNGNSLVSLTFHLFSLHGLIEYFH
LDMMKLRRFLVMIQEDYHSQNPYHNAVHAADVTQAMHCYLKEPKLANSVT
PWDILLSLIAAATHDLDHPGVNQPFLIKTNHYLATLYKNTSVLENHHWRS
AVGLLRESGLFSHLPLESRQQMETQIGALILATDISRQNEYLSLFRSHLD
RGDLCLEDTRHRHLVLQMALKCADICNPCRTWELSKQWSEKVTEEFFHQG
DIEKKYHLGVSPLCDRHTESIANIQIGFMTYLVEPLFTEWARFSNTRLSQ
TMLGHVGLNKASWKGLQR
3D structure
PDB4pm0 Discovery of 2-(Cyclopentylamino)thieno[3,2-d]pyrimidin-4(3H)-one Derivatives as a New Series of Potent Phosphodiesterase 7 Inhibitors.
ChainA
Resolution2.1 Å
3D
structure
Catalytic site residues are labeled in the structure
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Enzymatic activity
Catalytic site (original residue number in PDB) S169 A250
Catalytic site (residue number reindexed from 1) S31 A112
Enzyme Commision number 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 ZN A H216 H252 D253 D362 H78 H114 D115 D224
BS02 32V A Y211 I363 N365 V380 F384 I412 Q413 F416 Y73 I225 N227 V242 F246 I274 Q275 F278 MOAD: ic50=45nM
PDBbind-CN: -logKd/Ki=7.35,IC50=45nM
BindingDB: IC50=45nM
Gene Ontology
Molecular Function
GO:0004114 3',5'-cyclic-nucleotide phosphodiesterase activity
GO:0008081 phosphoric diester hydrolase activity
Biological Process
GO:0007165 signal transduction

View graph for
Molecular Function

View graph for
Biological Process
External links
PDB RCSB:4pm0, PDBe:4pm0, PDBj:4pm0
PDBsum4pm0
PubMed25383422
UniProtQ13946|PDE7A_HUMAN High affinity 3',5'-cyclic-AMP phosphodiesterase 7A (Gene Name=PDE7A)

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