PDE10A
Template:Short description Template:Infobox gene cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A is an enzyme that in humans is encoded by the PDE10A gene.[1][2]
Various cellular responses are regulated by the second messengers cAMP and cGMP. Phosphodiesterases, such as PDE10A, eliminate cAMP- and cGMP-mediated intracellular signaling by hydrolyzing the cyclic nucleotide to the corresponding nucleoside 5-prime monophosphate.[2][3]
Inhibitors
<templatestyles src="Stack/styles.css"/>
_in_tube_model.png){kind=link}
Script error: No such module "Check for unknown parameters".
- AMG-579[5]
- Balipodect (TAK-063): IC50 = 300 pM[6]
- Compound 96: IC50 = 700 pM, high selectivity against all other members of the PDE family[4]
- CPL500036[7]
- Mardepodect (PF-2545920)[8]
- MK-8189
- Papaverine[9]
- Tofisopam
Research
Preliminary evidence indicates a possible link between PDE10A expression and obesity in mice and humans.[10] PDE10A is a regulatory protein involved in the signaling of the striatum, a region of the brain important for controlling movement and cognition. Dysfunction of the striatum has been linked to the development of schizophrenia. Inhibition of PDE10A has been identified as a potential treatment for the disorder, and an inhibitor compound (MK-8189) is as of February 2023 in Phase 2b clinical development for the treatment of schizophrenia.[11]
References
<templatestyles src="Reflist/styles.css" />
- ↑ Script error: No such module "Citation/CS1".
- ↑ a b Script error: No such module "citation/CS1".
- ↑ Script error: No such module "Citation/CS1".
- ↑ a b Script error: No such module "Citation/CS1".
- ↑ Script error: No such module "Citation/CS1".
- ↑ Script error: No such module "Citation/CS1".
- ↑ Script error: No such module "Citation/CS1".
- ↑ Script error: No such module "Citation/CS1".
- ↑ Script error: No such module "Citation/CS1".
- ↑ Script error: No such module "Citation/CS1".
- ↑ Script error: No such module "Citation/CS1".
Script error: No such module "Check for unknown parameters".
Further reading
<templatestyles src="Refbegin/styles.css" />
- Script error: No such module "Citation/CS1".
- Script error: No such module "Citation/CS1".
- Script error: No such module "Citation/CS1".
- Script error: No such module "Citation/CS1".
- Script error: No such module "Citation/CS1".
- Script error: No such module "Citation/CS1".
This article incorporates text from the United States National Library of Medicine, which is in the public domain.
Template:PDB Gallery Script error: No such module "Navbox". Script error: No such module "Navbox". Template:Portal bar