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pubmed-article:21481589pubmed:abstractTexta-FABP is indespensible in inflammation and may serve as a new potential drug target for inflammation related diseases. We have successfully designed and synthesized a series of aromatic substituted pyrazoles as new human a-FABP inhibitors. The compounds strongly bound to the hydrophobic binding pocket of a-FABP, while showed significantly lower binding affinities to the closely related homologue protein h-FABP. The most potent and selective compound 5 g bound to a-FABP with an apparent K(i) value below 1.0 nM, while did not inhibit h-FABP at 50 ?M and thus represents one of the most potent and selective a-FABP inhibitors to date. The strong binding capacity of these inhibitors was further validated by their effective blockade of inflammatory responses as determined by the production of pro-inflammatory cytokines upon LPS stimulation. Compound 5 g may serve as a lead compound for developing new effective therapeutic agent for prevention and treatment of atherosclerosis, type 2 diabetes and other inflammatory and metabolic related diseases.lld:pubmed
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pubmed-article:21481589pubmed:authorpubmed-author:WangYuYlld:pubmed
pubmed-article:21481589pubmed:authorpubmed-author:XuAiminAlld:pubmed
pubmed-article:21481589pubmed:authorpubmed-author:LiuXiujieXlld:pubmed
pubmed-article:21481589pubmed:authorpubmed-author:WuDonghaiDlld:pubmed
pubmed-article:21481589pubmed:authorpubmed-author:LiHonglinHlld:pubmed
pubmed-article:21481589pubmed:authorpubmed-author:HuangXiaoliXlld:pubmed
pubmed-article:21481589pubmed:authorpubmed-author:DingKeKlld:pubmed
pubmed-article:21481589pubmed:authorpubmed-author:HuiXiaoyanXlld:pubmed
pubmed-article:21481589pubmed:authorpubmed-author:WangDongyeDlld:pubmed
pubmed-article:21481589pubmed:authorpubmed-author:LinWanhuaWlld:pubmed
pubmed-article:21481589pubmed:authorpubmed-author:DiaoYanyanYlld:pubmed
pubmed-article:21481589pubmed:copyrightInfoCopyright © 2011 Elsevier Ltd. All rights reserved.lld:pubmed
pubmed-article:21481589pubmed:issnTypeElectroniclld:pubmed
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pubmed-article:21481589pubmed:volume21lld:pubmed
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pubmed-article:21481589pubmed:year2011lld:pubmed
pubmed-article:21481589pubmed:articleTitleNew aromatic substituted pyrazoles as selective inhibitors of human adipocyte fatty acid-binding protein.lld:pubmed
pubmed-article:21481589pubmed:affiliationKey Laboratory of Regenerative Biology and Institute of Chemical Biology, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, #190 Kaiyuan Avenue, Guangzhou Science Park, Guangzhou 510530, PR China.lld:pubmed
pubmed-article:21481589pubmed:publicationTypeJournal Articlelld:pubmed
pubmed-article:21481589pubmed:publicationTypeResearch Support, Non-U.S. Gov'tlld:pubmed
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