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表皮生长因子受体激酶靶向杂合试剂对半胱氨酸的铂化作用。

Platination of cysteine by an epidermal growth factor receptor kinase-targeted hybrid agent.

机构信息

Department of Chemistry, Wake Forest University, Wake Downtown Campus, Winston-Salem, NC 27101, USA.

Department of Internal Medicine, Section on Molecular Medicine, Wake Forest School of Medicine, Winston-Salem, NC 27157, USA.

出版信息

Chem Commun (Camb). 2018 Jul 11;54(54):7479-7482. doi: 10.1039/c8cc04251a. Epub 2018 Jun 19.

DOI:10.1039/c8cc04251a
PMID:29915817
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7050444/
Abstract

Hybrid molecules have been developed which are comprised of a tyrosine kinase-targeted, quinazoline-based scaffold and a flexibly linked dia(m)minechloridoPt(ii) moiety. The target compounds maintain high affinity and selectivity for ErbB family kinase proteins and one of the derivatives induces platinum adducts with a pharmacologically important cysteine residue.

摘要

已经开发出了一种杂化分子，它由一个酪氨酸激酶靶向的、基于喹唑啉的支架和一个灵活连接的二（氨）氯代铂（II）部分组成。目标化合物对 ErbB 家族激酶蛋白保持高亲和力和选择性，其中一种衍生物诱导铂加合物与具有重要药理学意义的半胱氨酸残基结合。

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