Ontology highlight
ABSTRACT:
SUBMITTER: Huang H
PROVIDER: S-EPMC7669657 | biostudies-literature | 2020 Dec
REPOSITORIES: biostudies-literature
Huang Huang H Howard Christina A CA Zari Sergei S Cho Hyo Je HJ Shukla Shirish S Li Hao H Ndoj Juliano J González-Alonso Paula P Nikolaidis Caroline C Abbott Joshua J Rogawski David S DS Potopnyk Mykhaylo A MA Kempinska Katarzyna K Miao Hongzhi H Purohit Trupta T Henderson Andrew A Mapp Anna A Sulis Maria Luisa ML Ferrando Adolfo A Grembecka Jolanta J Cierpicki Tomasz T
Nature chemical biology 20200831 12
The nuclear receptor-binding SET domain (NSD) family of histone methyltransferases is associated with various malignancies, including aggressive acute leukemia with NUP98-NSD1 translocation. While NSD proteins represent attractive drug targets, their catalytic SET domains exist in autoinhibited conformation, presenting notable challenges for inhibitor development. Here, we employed a fragment-based screening strategy followed by chemical optimization, which resulted in the development of the fir ...[more]