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pubmed-article:21330015pubmed:abstractTextNAmPRTase (PBEF/Visfatin) plays a pivotal role in the salvage pathway of NAD(+) biosynthesis. NAmPRTase has been an attractive target for anti-cancer agents that induce apoptosis of tumor cells via a declining plasma NAD(+) level. In this report, a series of structural analogs of FK866 (1), a known NAmPRTase inhibitor, was synthesized and tested for inhibitory activities against the proliferation of cancer cells and human NAmPRTase. Among them, compound 7 showed similar anti-cancer and enzyme inhibitory activities to compound 1. Further investigation of compound 7 with X-ray analysis revealed a co-crystal structure in complex with human NAmPRTase, suggesting that Asp219 in the active site of the enzyme could contribute to an additional interaction with the pyrrole nitrogen of compound 7.lld:pubmed
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pubmed-article:21330015pubmed:authorpubmed-author:KoHyojinHlld:pubmed
pubmed-article:21330015pubmed:authorpubmed-author:EomSoo HyunSHlld:pubmed
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pubmed-article:21330015pubmed:authorpubmed-author:YounHyung-Seo...lld:pubmed
pubmed-article:21330015pubmed:authorpubmed-author:YouHyunHlld:pubmed
pubmed-article:21330015pubmed:copyrightInfoCopyright © 2011 Elsevier Masson SAS. All rights reserved.lld:pubmed
pubmed-article:21330015pubmed:issnTypeElectroniclld:pubmed
pubmed-article:21330015pubmed:volume46lld:pubmed
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pubmed-article:21330015pubmed:year2011lld:pubmed
pubmed-article:21330015pubmed:articleTitleDesign, synthesis and X-ray crystallographic study of NAmPRTase inhibitors as anti-cancer agents.lld:pubmed
pubmed-article:21330015pubmed:affiliationSchool of Life Science, Gwangju Institute of Science and Technology, Gwangju 500-712, Republic of Korea.lld:pubmed
pubmed-article:21330015pubmed:publicationTypeJournal Articlelld:pubmed
pubmed-article:21330015pubmed:publicationTypeResearch Support, Non-U.S. Gov'tlld:pubmed
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