NCIt definition : An orally bioavailable selective molecular glue degrader (MGD) of the translational
termination factor GSPT1, with potential antineoplastic activity. Upon oral administration,
MRT-2359 targets and binds to GSPT1, thereby promoting complex formation between the
E3 ubiquitin ligase component cereblon (CRBN) and GSPT1, and inducing GSPT1 degradation
in a CRBN- and degron-dependent manner. This downregulates L-MYC and N-MYC, thereby
disrupting MYC-driven protein translation and reducing MYC-oncogenic signaling. This
inhibits proliferation in MYC-driven tumors. The translation termination factor GSPT1,
a G-loop degron-containing protein, plays a key role in protein translation in MYC-driven
cancers.;
Semantic type(s)