利用距离匹配半胱氨酸交联剂实现细胞穿透：一种将 Mdm2/Mdmx 的细胞穿透肽双重抑制剂的简便方法。
Achieving cell penetration with distance-matching cysteine cross-linkers: a facile route to cell-permeable peptide dual inhibitors of Mdm2/Mdmx.
机构信息
Department of Chemistry, State University of New York at Buffalo, Buffalo, New York 14260, USA.
出版信息
Chem Commun (Camb). 2011 Sep 7;47(33):9396-8. doi: 10.1039/c1cc13320a. Epub 2011 Jul 19.
Abstract
We report the design of bisarylmethylene bromides as a new class of rigid, distance-matching cysteine cross-linkers. By cross-linking a peptide dual inhibitor of Mdm2/Mdmx containing cysteines at i,i+7 positions, dramatic enhancement in cell permeability was achieved, along with increased helicity and biological activity.
摘要
我们报告了双芳基亚甲基溴化物的设计，将其作为一类新型刚性、距离匹配半胱氨酸交联剂。通过交联含有 i,i+7 位半胱氨酸的 Mdm2/Mdmx 肽双抑制剂，实现了细胞通透性的显著增强，同时增加了螺旋度和生物活性。
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