化学
MDMX公司
肽
立体化学
亲缘关系
复分解
组合化学
膜透性
环肽
生物化学
膜
平方毫米
有机化学
聚合
基因
聚合物
作者
Zhihong Luo,Lei Xu,Xiaomin Tang,Xuejun Zhao,Tong He,William D. Lubell,Jinqiang Zhang
摘要
Novel all-hydrocarbon cross-linked aza-stapled peptides were designed and synthesized for the first time by ring-closing metathesis between two aza-alkenylglycine residues. Three aza-stapled peptidic analogues based on the peptide dual inhibitor of p53-MDM2/MDMX interactions were synthesized and screened for biological activities. Among the three aza-stapled peptides, aSPDI-411 displayed increased anti-tumor activity, binding affinities to both MDM2 and MDMX, and cell membrane permeability compared to its linear peptide counterpart.
科研通智能强力驱动
Strongly Powered by AbleSci AI