Kathryn Keenan

TL;DR: The discovery of GSK3685032 is reported, a potent first-in-class DNMT1-selective inhibitor that was shown via crystallographic studies to compete with the active-site loop ofDNMT1 for penetration into hemi-methylated DNA between two CpG base pairs.

TL;DR: Investigating the biomarkers of activity of the clinical BET inhibitor GSK525762 across cancer cell lines and demonstrating that KRAS mutations are novel resistance biomarkers highlight a potential to enhance the clinical benefit of BET and MEK inhibitors and provide a strong rationale for clinical evaluation of BET/MEK combination therapies in cancer.

TL;DR: It is demonstrated that selective, non-covalent inhibitors of DNMT1 may provide benefit over traditional DNA incorporating hypomethylating agents.

TL;DR: Mechanism-based combination strategies for BET inhibitors in NUT midline carcinoma are suggested and potential treatment strategies to improve response in this highly aggressive disease are suggested.

TL;DR: In this article, a simplified MS-based platform for histone methylation analysis was proposed, which uses chemical acetylation with d0-acetic anhydride to collapse all the differently acetylated histone forms into one form, greatly reducing the complexity of the peptide mixture.