Rigosertib show promise in cancers with mutations in RAS genes.
Mutations in RAS genes are very common, but treating this mutation has proven elusive since the mutant RAS protein lacks a drug-binding pocket. Researchers have not been able to make much progress towards developing drugs to target RAS oncogenes.
A new study published by Cell states that researchers were able to create a new mechanism for targeting mutant RAS oncogenes, however.
Researchers were able to identify a small molecule, rigosertib or ON01910.Na, which is able to inhibit different signaling pathways activated by RAS oncogenes.
According to the study, this molecule is able to act as a protein-protein interaction inhibitor that stops binding between RAS and signaling proteins that transform a cell into a cancer cell.
Researchers performed structural experiments to confirm rigosertib’s actions, as well as to demonstrate its potential to become a targeted mechanism for RAS-driven cancers.
"This discovery is a significant breakthrough for the cancer field," said Vivek Reddy, MD, lead researcher. "Rigosertib's mechanism of action represents a new paradigm for attacking the intractable RAS oncogenes. Our current focus is to use the information from our studies with rigosertib to design the next generation of small molecule RAS-targeting therapies, and we are excited to have recently identified several compounds which we think improve on the qualities of rigosertib."