击中移动目标：靶向瞬时蛋白质状态。
Hitting a moving target: targeting transient protein states.
机构信息
Laboratory for Molecular Design and Pharmaceutical Biophysics, Department of Pharmaceutical and Medicinal Chemistry, Institute of Pharmacy, Eberhard Karls University Tuebingen, Auf der Morgenstelle 8, 72076 Tuebingen, Germany.
出版信息
Structure. 2013 Dec 3;21(12):2095-7. doi: 10.1016/j.str.2013.11.003.
In this issue of Structure, Bista and colleagues report that inhibitors of the MDM2/p53 interaction can be designed to interact with a transiently folded α-helical segment of the MDM2 lid region. This suggests that targeting transient protein states in PPI inhibitor design could be a promising strategy to improve affinity and/or selectivity profiles.
在本期《结构》中，Bista 及其同事报告称，可以设计出与 MDM2 盖子区域的瞬态折叠α螺旋片段相互作用的 MDM2/p53 相互作用抑制剂。这表明，在 PPI 抑制剂设计中针对瞬态蛋白质状态可能是提高亲和力和/或选择性的有前途的策略。
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