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phosphodiesterase 8A

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Immunopharmacology Ligand  Target has curated data in GtoImmuPdb

Target id: 1307

Nomenclature: phosphodiesterase 8A

Abbreviated Name: PDE8A

Family: Phosphodiesterases, 3',5'-cyclic nucleotide (PDEs)

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 829 15q25.3 PDE8A phosphodiesterase 8A
Mouse - 823 7 D3 Pde8a phosphodiesterase 8A
Rat - - Pde8a phosphodiesterase 8A
Previous and Unofficial Names Click here for help
high affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8A
Database Links Click here for help
Alphafold O60658 (Hs), O88502 (Mm)
BRENDA 3.1.4.17
CATH/Gene3D 1.10.1300.10
ChEMBL Target CHEMBL4640 (Hs)
DrugBank Target O60658 (Hs)
Ensembl Gene ENSG00000073417 (Hs), ENSMUSG00000025584 (Mm), ENSRNOG00000019005 (Rn)
Entrez Gene 5151 (Hs), 18584 (Mm), 308776 (Rn)
Human Protein Atlas ENSG00000073417 (Hs)
KEGG Enzyme 3.1.4.17
KEGG Gene hsa:5151 (Hs), mmu:18584 (Mm), rno:308776 (Rn)
OMIM 602972 (Hs)
Pharos O60658 (Hs)
UniProtKB O60658 (Hs), O88502 (Mm)
Wikipedia PDE8A (Hs)
Enzyme Reaction Click here for help
EC Number: 3.1.4.17
Rank order of affinity (Human)
cyclic AMP >> cyclic GMP  [2]

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Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
PF-04957325 Small molecule or natural product Primary target of this compound Immunopharmacology Ligand Hs Inhibition 7.4 pIC50 3
⤷ pIC50 7.4 (IC50 4.3x10-8 M) [3]
dipyridamole Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 5.1 pIC50 2
⤷ pIC50 5.1 (IC50 7.94x10-6 M) [2]
Immunopharmacology Comments
The PDE8A-Raf-1 kinase signaling complex has been shown to regulate CD4+ T cell motility, and PDE8A represents a novel target for control of T cell-mediated inflammation [1].

References

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1. Basole CP, Nguyen RK, Lamothe K, Vang A, Clark R, Baillie GS, Epstein PM, Brocke S. (2017) PDE8 controls CD4+ T cell motility through the PDE8A-Raf-1 kinase signaling complex. Cell Signal, 40: 62-72. [PMID:28851628]

2. Fisher DA, Smith JF, Pillar JS, St Denis SH, Cheng JB. (1998) Isolation and characterization of PDE8A, a novel human cAMP-specific phosphodiesterase. Biochem Biophys Res Commun, 246 (3): 570-7. [PMID:9618252]

3. Maurice DH, Ke H, Ahmad F, Wang Y, Chung J, Manganiello VC. (2014) Advances in targeting cyclic nucleotide phosphodiesterases. Nat Rev Drug Discov, 13 (4): 290-314. [PMID:24687066]

Contributors

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