MRTX1133 is a Highly Selective, First-in-Class Inhibitor of KRAS G12D
Mutant KRAS is an attractive drug target for the treatment of a number of cancers for many decades. Until recently, the high affinity of KRAS for GDP/GTP and the lack of any other apparent binding pocket have significantly hampered the development of KRAS inhibitors. KRAS inhibitor relies on a...
BC-LI-0186 is a Selective Inhibitor of LeuRS and RagD Interaction
BC-LI-0186 is a potent and selective inhibitor of Leucyl-tRNA synthetase (LeuRS) and Ras-related GTP-binding protein D (RagD) interaction (IC50=46.11 nM). It competitively binds to the RagD interacting site of LRS (Kd=42.1 nM). At the same time, it has effects on LRS-Vps34, LRS-EPRS, RagB-RagD association, mTORC1 complex formation, or the...