Potent and selective biphenyl azole inhibitors of adipocyte fatty acid binding pirotein (aFABP)

Potent and selective biphenyl azole inhibitors of adipocyte fatty acid binding pirotein (aFABP)
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DOI:
10.1016/j.bmcl.2006.12.044
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发表时间:
2007-06-15
影响因子:
2.7
通讯作者:
Robl, Jeffrey A.
Robl, Jeffrey A.
中科院分区:
医学4区
文献类型:
--
作者:
Sulsky, Richard;Magnin, David R.;Robl, Jeffrey A.

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本文中,我们首次公开了联苯唑类,其是脂肪细胞脂肪酸结合蛋白(aFABP或aP2)的纳摩尔结合剂,对肌肉脂肪酸结合蛋白和表皮脂肪酸结合蛋白具有高达千倍的选择性。此外,还合成了一种新的放射性配体,以确定对三种脂肪酸结合蛋白的结合。(c)2007爱思唯尔有限公司保留所有权利。
Herein we report the first disclosure of biphenyl azoles that are nanomolar binders of adipocyte fatty acid binding protein (aFABP or aP2) with up to thousand-fold selectivity against muscle fatty acid binding protein and epidermal fatty acid binding protein. In addition a new radio-ligand to determine binding against the three fatty acid binding proteins was also synthesized. (c) 2007 Elsevier Ltd. All rights reserved.