基于 HRK 衍生的约束肽的 BCL-x 抑制剂的合理设计。
Rational design of Harakiri (HRK)-derived constrained peptides as BCL-x inhibitors.
机构信息
School of Chemistry, University of Leeds, Woodhouse Lane, Leeds, LS2 9JT, UK.
Astbury Centre for Structural Molecular Biology, University of Leeds, Woodhouse Lane, Leeds, LS2 9JT, UK.
出版信息
Chem Commun (Camb). 2023 Feb 7;59(12):1697-1700. doi: 10.1039/d2cc06029a.
Abstract
Using the HRK BH3 domain, sequence hybridization and methods we show dibromomaleimide staple scanning can be used to inform the design of BCL-x selective peptidomimetic ligands. These HRK-inspired reagents may serve as starting points for the discovery of therapeutics to target BCL-x-overexpressed cancers.
摘要
利用 HRK BH3 结构域、序列杂交和 方法，我们表明二溴马来酰亚胺订书钉扫描可用于为 BCL-x 选择性肽模拟配体的设计提供信息。这些受 HRK 启发的试剂可作为发现针对 BCL-x 过表达癌症的治疗药物的起点。
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