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Literature summary for 3.1.4.53 extracted from

  • Tsai, L.C.; Shimizu-Albergine, M.; Beavo, J.A.
    The high-affinity cAMP-specific phosphodiesterase 8B controls steroidogenesis in the mouse adrenal gland (2011), Mol. Pharmacol., 79, 639-648.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.1.4.53

Protein Variants

Protein Variants Comment Organism
additional information generation of PDE8B KO mice, that show elevated levels of urinary corticosterone in both basal and stressed conditions compared with their littermate wild-type controls Mus musculus

Inhibitors

Inhibitors Comment Organism Structure
dipyridamole inhibits PDE8 at high concentrations Mus musculus
additional information unlike other cAMP-specific PDEs, PDE8s are insensitive to a common nonselective PDE inhibitor, 3-isobutyl-1-methylxanthine (IBMX), but ca be inhibited by a high concentration of dipyridamole Mus musculus
PF-04957325 a selective PDE8 inhibitor Mus musculus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
adenosine 3',5'-cyclic phosphate + H2O Mus musculus both PDE8A and 8B hydrolyze cAMP with a very high affinity adenosine 5'-phosphate
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 ?

Organism

Organism UniProt Comment Textmining
Mus musculus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
adrenal gland
-
 Mus musculus
-
Y-1 cell
-
 Mus musculus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
adenosine 3',5'-cyclic phosphate + H2O
-
 Mus musculus adenosine 5'-phosphate
-
 ?
adenosine 3',5'-cyclic phosphate + H2O both PDE8A and 8B hydrolyze cAMP with a very high affinity Mus musculus adenosine 5'-phosphate
-
 ?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000002
-
 PDE8B, pH and temperature not specified in the publication Mus musculus PF-04957325
0.0000007
-
 PDE8A, pH and temperature not specified in the publication Mus musculus PF-04957325

General Information

General Information Comment Organism
malfunction PDE8B KO mice have elevated levels of urinary corticosterone in both basal and stressed conditions compared with their littermate wild-type controls. PDE8B KO mice exhibit adrenal hypersensitivity toward adrenocorticotropin. PDE8B gene ablation increases mRNA expressions of StAR protein and MC2R Mus musculus
physiological function importance of PDE8s in cAMP regulation of steroid production. PDE8A plays an important role in regulating a pool of cAMP that promotes testicular steroidogenesis. PDE8B regulates adrenocorticotropin-stimulated AZF steroidogenesis by both short- and long-term mechanisms Mus musculus