Issue 54, 2018
From the journal:

Chemical Communications

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

Mu Yang,a   Hanzhi Wu,b   Julie Chu,a   Lucas A. Gabriel,a   Y. Kim,c   Karen S. Anderson,c   Cristina M. Furduib  and  Ulrich Bierbach ORCID logo *a  

* Corresponding authors

a Department of Chemistry, Wake Forest University, Wake Downtown Campus, Winston-Salem, NC 27101, USA
E-mail: bierbau@wfu.edu

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

c Department of Pharmacology, Yale University School of Medicine, New Haven, CT 06520, USA

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.

Graphical abstract: Platination of cysteine by an epidermal growth factor receptor kinase-targeted hybrid agent

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Article information

DOI
https://doi.org/10.1039/C8CC04251A
Article type
Communication
Submitted
29 May 2018
Accepted
11 Jun 2018
First published
12 Jun 2018

Chem. Commun., 2018,54, 7479-7482

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

M. Yang, H. Wu, J. Chu, L. A. Gabriel, Y. Kim, K. S. Anderson, C. M. Furdui and U. Bierbach, Chem. Commun., 2018, 54, 7479 DOI: 10.1039/C8CC04251A

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