Target Information

Target General Infomation
Target ID
T84133
Former ID
TTDNC00456
Target Name
Phosphodiesterase 10A (PDE10A)
Gene Name
PDE10A
Synonyms
cAMP and cAMPinhibited cGMP 3',5'cyclic phosphodiesterase 10A; PDE10A
Target Type
Clinical Trial
Disease Huntington's disease [ICD9: 294.1, 333.4; ICD10: F02.2, G10]
Schizophrenia [ICD9: 295; ICD10: F20]
Schizoaffective disorder; Schizophrenia [ICD9: 295, 295.70; ICD10: F20, F25]
Function
Plays a role in signal transduction by regulating the intracellular concentration of cyclic nucleotides. Can hydrolyze both cAMP and cGMP, but has higher affinity for cAMP and is more efficient with cAMP as substrate.
BioChemical Class
Phosphoric diester hydrolases
UniProt ID
Q9Y233
EC Number
EC 3.1.4.35
Sequence
MRIEERKSQHLTGLTDEKVKAYLSLHPQVLDEFVSESVSAETVEKWLKRKNNKSEDESAP
KEVSRYQDTNMQGVVYELNSYIEQRLDTGGDNQLLLYELSSIIKIATKADGFALYFLGEC
NNSLCIFTPPGIKEGKPRLIPAGPITQGTTVSAYVAKSRKTLLVEDILGDERFPRGTGLE
SGTRIQSVLCLPIVTAIGDLIGILELYRHWGKEAFCLSHQEVATANLAWASVAIHQVQVC
RGLAKQTELNDFLLDVSKTYFDNIVAIDSLLEHIMIYAKNLVNADRCALFQVDHKNKELY
SDLFDIGEEKEGKPVFKKTKEIRFSIEKGIAGQVARTGEVLNIPDAYADPRFNREVDLYT
GYTTRNILCMPIVSRGSVIGVVQMVNKISGSAFSKTDENNFKMFAVFCALALHCANMYHR
IRHSECIYRVTMEKLSYHSICTSEEWQGLMQFTLPVRLCKEIELFHFDIGPFENMWPGIF
VYMVHRSCGTSCFELEKLCRFIMSVKKNYRRVPYHNWKHAVTVAHCMYAILQNNHTLFTD
LERKGLLIACLCHDLDHRGFSNSYLQKFDHPLAALYSTSTMEQHHFSQTVSILQLEGHNI
FSTLSSSEYEQVLEIIRKAIIATDLALYFGNRKQLEEMYQTGSLNLNNQSHRDRVIGLMM
TACDLCSVTKLWPVTKLTANDIYAEFWAEGDEMKKLGIQPIPMMDRDKKDEVPQGQLGFY
NAVAIPCYTTLTQILPPTEPLLKACRDNLSQWEKVIRGEETATWISSPSVAQKAAASED
Drugs and Mode of Action
Drug(s) OMS824 Drug Info Phase 2 Huntington's disease [548374]
TAK-063 Drug Info Phase 2 Schizophrenia [525237]
FRM-6308 Drug Info Phase 1b Schizophrenia [550786]
AMG 579 Drug Info Phase 1 Schizoaffective disorder; Schizophrenia [549374]
RG7203 Drug Info Discontinued in Phase 1 Schizophrenia [549450]
Inhibitor AMG 579 Drug Info [532898]
FRM-6308 Drug Info [532923]
OMS824 Drug Info [544354]
RG7203 Drug Info [551207]
TAK-063 Drug Info [544471]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Purine metabolism
Morphine addiction
PathWhiz Pathway Purine Metabolism
Reactome cGMP effects
G alpha (s) signalling events
References
Ref 525237ClinicalTrials.gov (NCT02477020) A Phase 2 Efficacy and Safety Study of TAK-063 in Participants With an Acute Exacerbation of Schizophrenia.
Ref 548374Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025042)
Ref 549374Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800035904)
Ref 549450Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800037470)
Ref 550786Clinical pipeline report, company report or official report of Forum pharmaceuticals.
Ref 532898Discovery of clinical candidate 1-(4-(3-(4-(1H-benzo[d]imidazole-2-carbonyl)phenoxy)pyrazin-2-yl)piperidin-1-yl)ethanone (AMG 579), a potent, selective, and efficacious inhibitor of phosphodiesterase10A (PDE10A). J Med Chem. 2014 Aug 14;57(15):6632-41.
Ref 532923Massive schizophrenia genomics study offers new drug directions. Nat Rev Drug Discov. 2014 Sep;13(9):641-2.
Ref 544354New Drugs/Drug News. P T. 2013 November; 38(11): 667-672.
Ref 544471Characterization of Binding and Inhibitory Properties of TAK-063, a Novel Phosphodiesterase 10A Inhibitor. PLoS One. 2015; 10(3): e0122197.
Ref 551207Synaptic synopsis. SciBX 6(41); doi:10.1038/scibx.2013.1153. Oct. 24, 2013

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