期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 6, 期 11, 页码 1128-1133出版社
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.5b00215
关键词
MAP4K4; HGK; ZC1; kinase inhibitor; MAP4K4 inhibitor; P-loop; PF-6260933
Recent studies in adipose tissue, pancreas, muscle, and macrophages suggest that MAP4K4, a serine/threonine protein kinase may be a viable target for antidiabetic drugs. As part of the evaluation of MAP4K4 as a novel antidiabetic target, a tool compound, 16 (PF-6260933) and a lead 17 possessing excellent kinome selectivity and suitable properties were delivered to establish proof of concept in vivo. The medicinal chemistry effort that led to the discovery of these lead compounds is described herein together with in vivo pharmacokinetic properties and activity in a model of insulin resistance.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据