一种高度新颖且具有选择性的mTOR抑制剂的合理发现。
Rational discovery of a highly novel and selective mTOR inhibitor.
作者信息
Jin Stanley, Mikami Satoshi, Scorah Nick, Chen Young, Halkowycz Petro, Shi Lihong, Kahana Jason, Vincent Patrick, de Jong Ron, Atienza Joy, Fabrey Robyn, Zhang Lilly, Lardy Matthew
机构信息
Takeda California, 10410 Science Center Drive, San Diego, CA 92121, United States; Fronthera US Pharmaceuticals, LLC, San Diego, CA, USA.
Takeda California, 10410 Science Center Drive, San Diego, CA 92121, United States.
出版信息
Bioorg Med Chem Lett. 2019 Nov 1;29(21):126659. doi: 10.1016/j.bmcl.2019.126659. Epub 2019 Sep 3.
Aided by Structure Based Drug Discovery (SBDD), we rapidly designed a highly novel and selective series of mTOR inhibitors. This chemotype conveys exquisite kinase selectivity, excellent in vitro and in vivo potencies and ADME safety profiles. These compounds could serve as good tools to explore the potential of TORC inhibition in various human diseases.
在基于结构的药物发现（SBDD）的辅助下，我们迅速设计出了一系列高度新颖且具有选择性的mTOR抑制剂。这种化学类型具有出色的激酶选择性、优异的体外和体内活性以及药代动力学和药效学性质。这些化合物可作为良好的工具，用于探索TORC抑制在各种人类疾病中的潜力。
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