BioCentury
ARTICLE | Cover Story

NSD2 momentum

October 10, 2013 7:00 AM UTC

Although NSD2 has been genetically linked to multiple myeloma for more than 15 years, drug discovery efforts against the target have lagged behind other histone methyltransferases including DOT1L and EZH2. Now, a Novartis Institutes for BioMedical Research and Broad Institute of MIT and Harvard collaboration and an independent Northwestern University team have identified activating mutations in NSD2 that drive a subset of leukemias,1,2 and a second Novartis team has made the best case to date that inhibiting the protein could help treat MM.3

DOT1L (histone methyltransferase DOT1L) and EZH2 (enhancer of zeste homolog 2) drive genetically defined subsets of leukemia. In the last year, Epizyme Inc. and its partners Celgene Corp. and Eisai Co. Ltd. have advanced inhibitors of the proteins into the clinic, and multiple companies have inhibitors of EZH2 in preclinical development...