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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
6
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pubmed:dateCreated |
2005-2-28
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pubmed:abstractText |
Two classes of quinazolinone derivatives and quinoxaline derivatives were identified as potent and selective poly(ADP-ribose) polymerase-1 and 2 (PARP-1) and (PARP-2) inhibitors, respectively. In PARP enzyme assays using recombinant PARP-1 and PARP-2, quinazolinone derivatives displayed relatively high selectivity for PARP-1 and quinoxaline derivatives showed superior selectivity for PARP-2. SBDD analysis via a combination of X-ray structural study and homology modeling suggested distinct interactions of inhibitors with PARP-1 and PARP-2. These findings provide a new structural framework for the design of selective inhibitors for PARP-1 and PARP-2.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Feb
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pubmed:issn |
0014-5793
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pubmed:author |
pubmed-author:HattoriKoujiK,
pubmed-author:IshidaJunyaJ,
pubmed-author:IwashitaAkinoriA,
pubmed-author:KamijoKazunoriK,
pubmed-author:KidoYoshiyukiY,
pubmed-author:KinoshitaTakayoshiT,
pubmed-author:MatsuokaNobuyaN,
pubmed-author:MiyakeHiroshiH,
pubmed-author:MuranoKenjiK,
pubmed-author:MutohSeitaroS,
pubmed-author:OhkuboMitsuruM,
pubmed-author:WarizayaMasaichiM,
pubmed-author:YamamotoHirofumiH
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pubmed:issnType |
Print
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pubmed:day |
28
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pubmed:volume |
579
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1389-93
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pubmed:meshHeading |
pubmed-meshheading:15733846-Crystallography, X-Ray,
pubmed-meshheading:15733846-Enzyme Inhibitors,
pubmed-meshheading:15733846-Humans,
pubmed-meshheading:15733846-Models, Molecular,
pubmed-meshheading:15733846-Molecular Structure,
pubmed-meshheading:15733846-Poly(ADP-ribose) Polymerases,
pubmed-meshheading:15733846-Protein Conformation,
pubmed-meshheading:15733846-Quinazolines,
pubmed-meshheading:15733846-Quinoxalines,
pubmed-meshheading:15733846-Structure-Activity Relationship
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pubmed:year |
2005
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pubmed:articleTitle |
Discovery of quinazolinone and quinoxaline derivatives as potent and selective poly(ADP-ribose) polymerase-1/2 inhibitors.
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pubmed:affiliation |
Medicinal Biology Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., 2-1-6 Kashima, Osaka 532-8514, Japan. aki_iwashita@po.fujisawa.co.jp
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pubmed:publicationType |
Journal Article
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