Possible Treatment Found for RAS-Driven Cancers
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."