苯并咪唑类化合物作为选择性 rho 激酶抑制剂的发展。
The development of benzimidazoles as selective rho kinase inhibitors.
机构信息
Department of Molecular Therapeutics and Translational Research Institute, The Scripps Research Institute, Scripps Florida, Jupiter, FL 33458, USA.
出版信息
Bioorg Med Chem Lett. 2010 Mar 15;20(6):1939-43. doi: 10.1016/j.bmcl.2010.01.124. Epub 2010 Feb 1.
Rho Kinase (ROCK) is a serine/threonine kinase whose inhibition could prove beneficial in numerous therapeutic areas. We have developed a promising class of ATP-competitive inhibitors based upon a benzimidazole scaffold, which show excellent potency toward ROCK (IC(50)<10nM). This report details the optimization of selectivity for ROCK over other related kinases such as Protein kinase A (PKA).
Rho 激酶（ROCK）是一种丝氨酸/苏氨酸激酶，其抑制作用可能在许多治疗领域有益。我们已经开发了一类有前途的基于苯并咪唑骨架的 ATP 竞争性抑制剂，它们对 ROCK（IC（50）<10nM）表现出优异的效力。本报告详细介绍了对 ROCK 相对于其他相关激酶（如蛋白激酶 A（PKA））的选择性进行优化的情况。
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