基诺美
可药性
化学
手性(物理)
药物发现
计算生物学
化学空间
激酶
药品
药物开发
药理学
生物化学
生物
基因
量子力学
夸克
物理
手征对称破缺
Nambu–Jona Lasinio模型
作者
Debasmita Saha,Anupreet Kharbanda,Wei Yan,Naga Rajiv Lakkaniga,Brendan Frett,Hong Yu Li
标识
DOI:10.1021/acs.jmedchem.9b00640
摘要
Chirality is important in drug discovery because stereoselective drugs can ameliorate therapeutic difficulties including adverse toxicity and poor pharmacokinetic profiles. The human kinome, a major druggable enzyme class has been exploited to treat a wide range of diseases. However, many kinase inhibitors are planar and overlap in chemical space, which leads to selectivity and toxicity issues. By exploring chirality within the kinome, a new iteration of kinase inhibitors is being developed to better utilize the three-dimensional nature of the kinase active site. Exploration into novel chemical space, in turn, will also improve drug solubility and pharmacokinetic profiles. This perspective explores the role of chirality to improve kinome druggability and will serve as a resource for pioneering kinase inhibitor development to address current therapeutic needs.
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