phosphodiesterase 8A | Phosphodiesterases, 3',5'-cyclic nucleotide (PDEs) | IUPHAR/BPS Guide to PHARMACOLOGY

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phosphodiesterase 8A

target has curated data in GtoImmuPdb

Target id: 1307

Nomenclature: phosphodiesterase 8A

Abbreviated Name: PDE8A

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

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - - PDE8A phosphodiesterase 8A
Mouse - - Pde8a phosphodiesterase 8A
Rat - - Pde8a phosphodiesterase 8A
Previous and Unofficial Names
high affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8A
Database Links
BRENDA
CATH/Gene3D
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Pharos
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 3.1.4.17
Rank order of affinity (Human)
cyclic AMP >> cyclic GMP  [2]

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
PF-04957325 Hs Inhibition 7.4 pIC50 3
pIC50 7.4 (IC50 4.3x10-8 M) [3]
dipyridamole 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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