Discovery of a novel class NSD2 inhibitor for multiple myeloma with t(4;14)^.

ABSTRACT: The prognosis for multiple myeloma (MM) has continued to improve with the development of a series of novel molecular targeted drugs over time. However, the prognosis remains poor for cases with high-risk chromosomal abnormalities. Of such abnormalities, t(4;14) is the second most common, occurring in 15% of patients with MM. MM cells carrying t(4;14) strongly express histone methyltransferase with a SET domain, called NSD2, making them resistant to drugs against MM. Therefore, NSD2 is a promising therapeutic target for MM carrying t(4;14). Subsequently, we performed high-throughput screening and identified RK-0080552 (RK-552) as a novel class NSD2 inhibitor. RK-552 was significantly cytotoxic against t(4;14)⁺ MM compared with t(4;14)^- MM cells in vitro and in vivo via

SUBMITTER: Matsuoka S 

PROVIDER: S-EPMC12423681 | biostudies-literature | 2025 May

REPOSITORIES: biostudies-literature