Issue 9, 2014
From the journal:

MedChemComm

A versatile acid-labile linker for antibody–drug conjugates†

Mathew C. Finniss,‡a   Kevin S. Chu,‡b   Charles J. Bowerman,a   J. Christopher Luft,abc   Zishan A. Haroonbef  and  Joseph M. DeSimone§*abcdefghi  

* Corresponding authors

a Lineberger Comprehensive Cancer Center, University of North Carolina at Chapel Hill, USA
E-mail: desimone@unc.edu

b Department of Pharmaceutical Sciences, University of North Carolina at Chapel Hill, USA

c Department of Chemistry, University of North Carolina at Chapel Hill, USA

d Department of Biochemistry and Biophysics, University of North Carolina at Chapel Hill, USA

e Carolina Center of Cancer Nanotechnology Excellence, University of North Carolina at Chapel Hill, USA

f Institute for Nanomedicine, University of North Carolina at Chapel Hill, USA

g Institute for Advanced Materials, University of North Carolina at Chapel Hill, USA

h Department of Chemical and Biomolecular Engineering, North Carolina State University, USA

i Sloan-Kettering Institute for Cancer Research, Memorial Sloan-Kettering Cancer Center, USA

Abstract

Antibody drug conjugates (ADC) couple therapeutic monoclonal antibodies (mAb) with potent toxins through a linker that is stable within systemic circulation, but cleaves within the target cells. In this report, silyl ether chemistry was used to couple the mAb trastuzumab with the chemotherapeutic, gemcitabine, to demonstrate the use of silyl ethers as a potential linker for ADCs.

Graphical abstract: A versatile acid-labile linker for antibody–drug conjugates

About
Cited by
Related
Download options Please wait...

Supplementary files

Article information

DOI
https://doi.org/10.1039/C4MD00150H
Article type
Concise Article
Submitted
01 Apr 2014
Accepted
13 Jun 2014
First published
16 Jun 2014

Med. Chem. Commun., 2014,5, 1355-1358

Author version available

Download author version (PDF)

Permissions

Request permissions

A versatile acid-labile linker for antibody–drug conjugates

M. C. Finniss, K. S. Chu, C. J. Bowerman, J. C. Luft, Z. A. Haroon and J. M. DeSimone, Med. Chem. Commun., 2014, 5, 1355 DOI: 10.1039/C4MD00150H

To request permission to reproduce material from this article, please go to the Copyright Clearance Center request page.

If you are an author contributing to an RSC publication, you do not need to request permission provided correct acknowledgement is given.

If you are the author of this article, you do not need to request permission to reproduce figures and diagrams provided correct acknowledgement is given. If you want to reproduce the whole article in a third-party publication (excluding your thesis/dissertation for which permission is not required) please go to the Copyright Clearance Center request page.

Read more about how to correctly acknowledge RSC content.

Spotlight

Advertisements