Tuesday, June 27, 2017

Residue-Specific Peptide Modification: A Chemist’s Guide

Justine N. deGruyter, Lara R. Malins, and Phil S. Baran

Department of Chemistry, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037

DOI: 10.1021/acs.biochem.7b00536

Advances in bioconjugation and native protein modification are appearing at a blistering pace, making it increasingly time consuming for practitioners to identify the best chemical method to modify a specific amino acid residue in a complex setting. The purpose of this perspective is to provide an informative, graphically-rich manual highlighting significant advances in the field over the past decade. This guide will help triage candidate methods for peptide alteration, and will serve as a starting point for those seeking to solve longstanding challenges.

Discovery of Carbodiimide Warheads to Selectively and Covalently Target Aspartic Acid in KRASG12D

Ludovica S. Sirocchi, Maximilian Scharnweber, Sarah Oberndorfer, Gabriella Siszler, Krzysztof M. Zak, Klaus Rumpel, Ralph A. Neumüller, and ...