化学
磷脂酰肌醇
激酶
药物发现
药理学
效力
PI3K/AKT/mTOR通路
生物化学
阿尔法(金融)
信号转导
体外
医学
结构效度
护理部
患者满意度
作者
Pascal Furet,Vito Guagnano,Robin A. Fairhurst,Patricia Imbach‐Weese,Ian Bruce,Mark Knapp,Christine Fritsch,Francesca Blasco,Joachim Blanz,Reiner Aichholz,Jacques Hamon,Doriano Fabbro,Giorgio Caravatti
标识
DOI:10.1016/j.bmcl.2013.05.007
摘要
Phosphatidylinositol-3-kinase α (PI3Kα) is a therapeutic target of high interest in anticancer drug research. On the basis of a binding model rationalizing the high selectivity and potency of a particular series of 2-aminothiazole compounds in inhibiting PI3Kα, a medicinal chemistry program has led to the discovery of the clinical candidate NVP-BYL719.
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