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词条 PDE10A
释义

  1. Inhibitors

  2. Research

  3. References

  4. Further reading

{{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

  • Compound 96: IC50 = 700 pM, high selectivity against all other members of the PDE family[4]
  • Papaverine[5]
  • PF-2545920[6]
  • TAK-063: IC50 = 300 pM[7]
  • AMG 579[8]

Research

Preliminary evidence indicates a possible link between PDE10A expression and obesity in mice and humans.[9]

References

1. ^{{cite journal |vauthors=Fujishige K, Kotera J, Michibata H, Yuasa K, Takebayashi S, Okumura K, Omori K | title = Cloning and characterization of a novel human phosphodiesterase that hydrolyzes both cAMP and cGMP (PDE10A) | journal = J Biol Chem | volume = 274 | issue = 26 | pages = 18438–45 |date=Jul 1999 | pmid = 10373451 | pmc = | doi =10.1074/jbc.274.26.18438 }}
2. ^{{cite web | title = Entrez Gene: PDE10A phosphodiesterase 10A| url = https://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=10846| accessdate = }}
3. ^{{cite journal |vauthors=Fujishige K, Kotera J, Yuasa K, Omori K | title = The human phosphodiesterase PDE10A gene genomic organization and evolutionary relatedness with other PDEs containing GAF domains | journal = Eur. J. Biochem. | volume = 267 | issue = 19 | pages = 5943–51 |date=October 2000 | pmid = 10998054 | doi = 10.1046/j.1432-1327.2000.01661.x | url = | issn = }}
4. ^{{cite journal | last1 = Malamas | first1 = MS| year = 2011 | title = Highly potent, selective, and orally active phosphodiesterase 10A inhibitors | url = | journal = J. Med. Chem. | volume = 54 | issue = 21| pages = 7621–38 | doi = 10.1021/jm2009138 | pmid = 21988093 |display-authors=etal}}
5. ^{{cite journal |vauthors=Siuciak JA, Chapin DS, Harms JF, etal |title=Inhibition of the striatum-enriched phosphodiesterase PDE10A: a novel approach to the treatment of psychosis |journal=Neuropharmacology |volume=51 |issue=2 |pages=386–96 |date=August 2006 |pmid=16780899 |doi=10.1016/j.neuropharm.2006.04.013 |url=http://linkinghub.elsevier.com/retrieve/pii/S0028-3908(06)00106-7}}
6. ^{{cite journal | pmid = 19630403 | doi=10.1021/jm900521k | volume=52 | issue=16 | title=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 |date=August 2009 | journal=J. Med. Chem. | pages=5188–96 |vauthors=Verhoest PR, Chapin DS, Corman M, etal }}
7. ^{{cite journal |vauthors=Kunitomo J, Yoshikawa M, Fushimi M, etal |title=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 |journal=J. Med. Chem. |volume=57 |issue=22 |pages=9627–43 |year=2014 |pmid=25384088 |doi=10.1021/jm5013648 |url=}}
8. ^{{cite journal | last1 = Hu | display-authors = etal | year = 2014 | title = 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)". | url = | journal = J Med Chem | volume = | issue = | page = }}
9. ^{{cite journal | last1 = Hankir | first1 = Mohammed K | display-authors = etal | year = 2016 | title = A novel thermoregulatory role for PDE10A in mouse and human adipocytes. | url = http://embomolmed.embopress.org/content/early/2016/05/31/emmm.201506085.long | journal = EMBO Molecular Medicine | volume = | issue = | page = }}

Further reading

{{refbegin | 2}}
  • {{cite journal |vauthors=Loughney K, Snyder PB, Uher L, etal |title=Isolation and characterization of PDE10A, a novel human 3', 5'-cyclic nucleotide phosphodiesterase. |journal=Gene |volume=234 |issue= 1 |pages= 109–17 |year= 1999 |pmid= 10393245 |doi=10.1016/S0378-1119(99)00171-7 }}
  • {{cite journal |vauthors=Kotera J, Fujishige K, Yuasa K, Omori K |title=Characterization and phosphorylation of PDE10A2, a novel alternative splice variant of human phosphodiesterase that hydrolyzes cAMP and cGMP. |journal=Biochem. Biophys. Res. Commun. |volume=261 |issue= 3 |pages= 551–7 |year= 1999 |pmid= 10441464 |doi= 10.1006/bbrc.1999.1013 }}
  • {{cite journal |vauthors=Zauli G, Milani D, Mirandola P, etal |title=HIV-1 Tat protein down-regulates CREB transcription factor expression in PC12 neuronal cells through a phosphatidylinositol 3-kinase/AKT/cyclic nucleoside phosphodiesterase pathway. |journal=FASEB J. |volume=15 |issue= 2 |pages= 483–91 |year= 2001 |pmid= 11156964 |doi= 10.1096/fj.00-0354com }}
  • {{cite journal |vauthors=Frame M, Wan KF, Tate R, etal |title=The gamma subunit of the rod photoreceptor cGMP phosphodiesterase can modulate the proteolysis of two cGMP binding cGMP-specific phosphodiesterases (PDE6 and PDE5) by caspase-3. |journal=Cell. Signal. |volume=13 |issue= 10 |pages= 735–41 |year= 2001 |pmid= 11602184 |doi=10.1016/S0898-6568(01)00193-0 }}
  • {{cite journal |vauthors=Strausberg RL, Feingold EA, Grouse LH, etal |title=Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences. |journal=Proc. Natl. Acad. Sci. U.S.A. |volume=99 |issue= 26 |pages= 16899–903 |year= 2003 |pmid= 12477932 |doi= 10.1073/pnas.242603899 | pmc=139241 }}
  • {{cite journal |vauthors=Mungall AJ, Palmer SA, Sims SK, etal |title=The DNA sequence and analysis of human chromosome 6. |journal=Nature |volume=425 |issue= 6960 |pages= 805–11 |year= 2003 |pmid= 14574404 |doi= 10.1038/nature02055 }}
  • {{cite journal |vauthors=Ota T, Suzuki Y, Nishikawa T, etal |title=Complete sequencing and characterization of 21,243 full-length human cDNAs. |journal=Nat. Genet. |volume=36 |issue= 1 |pages= 40–5 |year= 2004 |pmid= 14702039 |doi= 10.1038/ng1285 }}
  • {{cite journal |vauthors=Gerhard DS, Wagner L, Feingold EA, etal |title=The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC). |journal=Genome Res. |volume=14 |issue= 10B |pages= 2121–7 |year= 2004 |pmid= 15489334 |doi= 10.1101/gr.2596504 | pmc=528928 }}
  • {{cite journal |vauthors=Gross-Langenhoff M, Hofbauer K, Weber J, etal |title=cAMP is a ligand for the tandem GAF domain of human phosphodiesterase 10 and cGMP for the tandem GAF domain of phosphodiesterase 11. |journal=J. Biol. Chem. |volume=281 |issue= 5 |pages= 2841–6 |year= 2006 |pmid= 16330539 |doi= 10.1074/jbc.M511468200 }}
  • {{cite journal |vauthors=Chappie TA, Helal CJ, Hou X |title=Current Landscape of Phosphodiesterase 10A (PDE10A) Inhibition. |journal=J. Med. Chem. |volume=55 |issue=17 |pages= 7299–7331 |year= 2012 |pmid= 22834877 |doi=10.1021/jm3004976}}
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