Wednesday, July 22, 2020

The Chemical Biology of Reversible Lysine Post-translational Modifications

Zhipeng A. Wang, Philip A. Cole

Cell Chem. Biol. 2020

Lysine (Lys) residues in proteins undergo a wide range of reversible post-translational modifications (PTMs), which can regulate enzyme activities, chromatin structure, protein-protein interactions, protein stability, and cellular localization. Here we discuss the “writers,” “erasers,” and “readers” of some of the common protein Lys PTMs and summarize examples of their major biological impacts. We also review chemical biology approaches, from small-molecule probes to protein chemistry technologies, that have helped to delineate Lys PTM functions and show promise for a diverse set of biomedical applications.

β-d-Arabinofuranose-configured Cyclitol Aziridines as Selective, Brain-penetrant Covalent GBA2 Inhibitors

Rob F. Lammers, Qin Su, Laura Mazo, Wendy A. Offen, Roelof Ottenhoff, Mats J. Bulterman, Martijn van der Lienden, Maria J. Ferraz, Florian K...