词条 | PDE10A |
释义 |
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
ResearchPreliminary evidence indicates a possible link between PDE10A expression and obesity in mice and humans.[9] References1. ^{{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. ^1 {{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. ^1 {{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}}
1 : EC 3.1.4 |
随便看 |
开放百科全书收录14589846条英语、德语、日语等多语种百科知识,基本涵盖了大多数领域的百科知识,是一部内容自由、开放的电子版国际百科全书。