共价小分子激酶抑制剂的研究进展。
Progress with covalent small-molecule kinase inhibitors.
机构信息
Department of Biomedical Engineering, University of Virginia, Charlottesville, VA 22908, USA.
Department of Biomedical Engineering, University of Virginia, Charlottesville, VA 22908, USA.
出版信息
Drug Discov Today. 2018 Mar;23(3):727-735. doi: 10.1016/j.drudis.2018.01.035. Epub 2018 Jan 11.
PMID:29337202
Abstract
With reduced risk of toxicity and high selectivity, covalent small-molecule kinase inhibitors (CSKIs) have emerged rapidly. Through the lens of structural system pharmacology, here we review this rapid progress by considering design strategies and the challenges and opportunities offered by current CSKIs.
摘要
具有降低毒性风险和高选择性的共价小分子激酶抑制剂 (CSKIs) 已经迅速出现。通过结构系统药理学的视角，我们通过考虑设计策略以及当前 CSKIs 带来的挑战和机遇，来回顾这一快速发展。
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