PDE10A

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PDE10A
Protein PDE10A PDB 2o8h.png
Available structures
PDB Ortholog search: PDBe RCSB
Identifiers
Aliases PDE10A, HSPDE10A19, ADSD2, IOLOD, phosphodiesterase 10A, LINC00473
External IDs MGI: 1345143 HomoloGene: 4852 GeneCards: PDE10A
RNA expression pattern
PBB GE PDE10A 211170 s at fs.png

PBB GE PDE10A 211171 s at fs.png

PBB GE PDE10A 205501 at fs.png
More reference expression data
Orthologs
Species Human Mouse
Entrez
Ensembl
UniProt
RefSeq (mRNA)

NM_001130690
NM_006661

NM_001290707
NM_011866
NM_001347321

RefSeq (protein)

NP_001124162
NP_006652

NP_001277636.1
NP_035996.2
NP_001277636
NP_001334250
NP_035996

Location (UCSC) Chr 6: 165.33 – 165.99 Mb Chr 17: 8.53 – 8.99 Mb
PubMed search [1] [2]
Wikidata
View/Edit Human View/Edit Mouse

cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A is an enzyme that in humans is encoded by the PDE10A gene.[3][4]

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.[4][5]

Inhibitors[edit]

3d model of compound #96 (Malamas, 2011)[6]

Research[edit]

Preliminary evidence indicates a possible link between PDE10A expression and obesity in mice and humans.[11]

References[edit]

  1. ^ "Human PubMed Reference:". 
  2. ^ "Mouse PubMed Reference:". 
  3. ^ Fujishige K, Kotera J, Michibata H, Yuasa K, Takebayashi S, Okumura K, Omori K (Jul 1999). "Cloning and characterization of a novel human phosphodiesterase that hydrolyzes both cAMP and cGMP (PDE10A)". J Biol Chem. 274 (26): 18438–45. doi:10.1074/jbc.274.26.18438. PMID 10373451. 
  4. ^ a b "Entrez Gene: PDE10A phosphodiesterase 10A". 
  5. ^ Fujishige K, Kotera J, Yuasa K, Omori K (October 2000). "The human phosphodiesterase PDE10A gene genomic organization and evolutionary relatedness with other PDEs containing GAF domains". Eur. J. Biochem. 267 (19): 5943–51. doi:10.1046/j.1432-1327.2000.01661.x. PMID 10998054. 
  6. ^ a b Malamas, MS; et al. (2011). "Highly potent, selective, and orally active phosphodiesterase 10A inhibitors". J. Med. Chem. 54 (21): 7621–38. doi:10.1021/jm2009138. PMID 21988093. 
  7. ^ Siuciak JA, Chapin DS, Harms JF, et al. (August 2006). "Inhibition of the striatum-enriched phosphodiesterase PDE10A: a novel approach to the treatment of psychosis". Neuropharmacology. 51 (2): 386–96. doi:10.1016/j.neuropharm.2006.04.013. PMID 16780899. 
  8. ^ Verhoest PR, Chapin DS, Corman M, et al. (August 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. doi:10.1021/jm900521k. PMID 19630403. 
  9. ^ Kunitomo J, Yoshikawa M, Fushimi M, et al. (2014). "Discovery of 1-[2-Fluoro-4-(1H-pyrazol-1-yl)phenyl]-5-methoxy-3-(1-phenyl-1H-pyrazol-5-yl)pyridazin-4(1H)-one (TAK-063), a Highly Potent, Selective, and Orally Active Phosphodiesterase 10A (PDE10A) Inhibitor". J. Med. Chem. 57 (22): 9627–43. doi:10.1021/jm5013648. PMID 25384088. 
  10. ^ Hu; et al. (2014). "Discovery of Clinical Candidate 1-(4-(3-(4-(1Hbenzo[d]imidazole-2-carbonyl)phenoxy)pyrazin-2-yl)piperidin-1-yl)ethanone (AMG 579), a Potent, Selective, and Efficacious Inhibitor of Phosphodiesterase 10A (PDE10A)".". J Med Chem. 
  11. ^ Hankir, Mohammed K; et al. (2016). "A novel thermoregulatory role for PDE10A in mouse and human adipocytes.". EMBO Molecular Medicine. 

Further reading[edit]

This article incorporates text from the United States National Library of Medicine, which is in the public domain.