含联苯骨架的小分子、非肽类、非 ATP 竞争型 polo 样激酶 1（Plk1）抑制剂。
Small-molecular, non-peptide, non-ATP-competitive polo-like kinase 1 (Plk1) inhibitors with a terphenyl skeleton.
机构信息
Institute of Molecular and Cellular Biosciences, The University of Tokyo, 1-1-1 Yayoi, Bunkyo-ku, Tokyo 113-0032, Japan.
出版信息
Bioorg Med Chem. 2013 Feb 1;21(3):608-17. doi: 10.1016/j.bmc.2012.11.054. Epub 2012 Dec 11.
PMID:23276450
Abstract
Polo-like kinase (Plk) 1 is a serine-threonine protein kinase that plays a role in cell division, and its overexpression is highly correlated with aggressiveness and prognosis of many cancers. We have designed, synthesized and evaluated a series of terphenyl compounds as inhibitors of the kinase activity of Plk1. Some of them act as non-ATP-competitive Plk1 inhibitors.
摘要
丝氨酸/苏氨酸蛋白激酶 Polo 样激酶 1（Plk1）在细胞分裂中发挥作用，其过表达与许多癌症的侵袭性和预后高度相关。我们设计、合成并评价了一系列三联苯类化合物作为 Plk1 激酶活性的抑制剂。其中一些化合物为非 ATP 竞争性 Plk1 抑制剂。
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