phosphodiesterase 10A

Target id: 1310

Nomenclature: phosphodiesterase 10A

Abbreviated Name: PDE10A

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

   GtoImmuPdb view: OFF :     Currently no data for phosphodiesterase 10A in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - - PDE10A phosphodiesterase 10A
Mouse - - Pde10a phosphodiesterase 10A
Rat - - Pde10a phosphodiesterase 10A
Previous and Unofficial Names
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A | testis-specific phosphodiesterase PDE10A2
Database Links
BRENDA
CATH/Gene3D
DrugBank Target
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  X-ray structure of human PDE10A in complex with the selective inhibitor PF-2545920.
PDB Id:  3HR1
Ligand:  PF-2545920
Resolution:  1.53Å
Species:  Human
References:  2
Enzyme Reaction
EC Number: 3.1.4.17
Rank order of affinity (Human)
cyclic AMP, cyclic GMP  [1]

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Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
compound 19 [PMID: 22142545] Hs Inhibition 9.0 pKi 4
pKi 9.0 (Ki 1x10-9 M) [4]
compound 27 [PMID: 22142545] Hs Inhibition 8.3 pKi 4
pKi 8.3 (Ki 5x10-9 M) [4]
PF-2545920 Hs Inhibition 9.4 pIC50 2
pIC50 9.4 (IC50 3.7x10-10 M) [2]
Tissue Distribution
PDE10A is highly enriched in the brain, and shows a unique expression profile in brain regions that suggest potential for novel antipsychotic (schzophrenia) treatments, and for other disorders affecting the basal ganglia (e.g. bipolar and autism spectrum disorders, and movement disorders such as Parkinson's and Huntington's diseases).
Species:  Human
Technique: 
References:  3

References

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1. Fujishige K, Kotera J, Michibata H, Yuasa K, Takebayashi S, Okumura K, Omori K. (1999) Cloning and characterization of a novel human phosphodiesterase that hydrolyzes both cAMP and cGMP (PDE10A). J. Biol. Chem.274 (26): 18438-45. [PMID:10373451]

2. Verhoest PR, Chapin DS, Corman M, Fonseca K, Harms JF, Hou X, Marr ES, Menniti FS, Nelson F, O'Connor R et al.. (2009) Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia. J. Med. Chem.52 (16): 5188-96. [PMID:19630403]

3. Wilson LS, Brandon NJ. (2015) Emerging biology of PDE10A. Curr. Pharm. Des.21 (3): 378-88. [PMID:25159072]

4. Yang SW, Smotryski J, McElroy WT, Tan Z, Ho G, Tulshian D, Greenlee WJ, Guzzi M, Zhang X, Mullins D et al.. (2012) Discovery of orally active pyrazoloquinolines as potent PDE10 inhibitors for the management of schizophrenia. Bioorg. Med. Chem. Lett.22 (1): 235-9. [PMID:22142545]

How to cite this page

Phosphodiesterases, 3',5'-cyclic nucleotide (PDEs): phosphodiesterase 10A. Last modified on 31/07/2017. Accessed on 21/10/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1310.