Ontology highlight
ABSTRACT:
SUBMITTER: Morrison MJ
PROVIDER: S-EPMC5942779 | biostudies-literature | 2018
REPOSITORIES: biostudies-literature
Morrison Michael J MJ Boriack-Sjodin P Ann PA Swinger Kerren K KK Wigle Tim J TJ Sadalge Dipti D Kuntz Kevin W KW Scott Margaret Porter MP Janzen William P WP Chesworth Richard R Duncan Kenneth W KW Harvey Darren M DM Lampe John W JW Mitchell Lorna H LH Copeland Robert A RA
PloS one 20180509 5
WHSC1 is a histone methyltransferase that is responsible for mono- and dimethylation of lysine 36 on histone H3 and has been implicated as a driver in a variety of hematological and solid tumors. Currently, there is a complete lack of validated chemical matter for this important drug discovery target. Herein we report on the first fully validated WHSC1 inhibitor, PTD2, a norleucine-containing peptide derived from the histone H4 sequence. This peptide exhibits micromolar affinity towards WHSC1 in ...[more]