Development of substrate-selective probes for affinity pulldown of histone demethylases.

ABSTRACT: JmjC-domain containing histone demethylases (JHDMs) play critical roles in many key cellular processes and have been implicated in multiple disease conditions. Each enzyme within this family is known to have a strict substrate scope, specifically the position of the lysine within the histone and its degree of methylation. While much progress has been made in determining the substrates of each enzyme, new methods with which to systematically profile each histone mark are greatly needed. Novel chemical tools have the potential to fill this role and, furthermore, can be used as probes to answer fundamental questions about these enzymes and serve as potential therapeutic leads. In this work, we first investigated three small-molecule probes differing in the degree of "methylation state" and th

SUBMITTER: Marholz LJ 

PROVIDER: S-EPMC4301071 | biostudies-literature | 2015 Jan

REPOSITORIES: biostudies-literature