Events
MoSMed Research Seminar: BMCS Lecture - Prof Jim Cregg
- Venue: Bedson Building, room 2.76
- Start: Fri, 05 Jun 2026 14:00:01 BST
- End: Fri, 05 Jun 2026 15:00:28 BST
We are delighted to welcome Prof Jim Cregg to Newcastle on 5th June for a talk in Bedson Building, room 2.76.
Title: Discovery of RAS(ON) Tri-Complex Inhibitors
Abstract: RAS proteins are small GTPases that cycle between the GTP-bound RAS(ON) state and GDP-bound RAS(OFF) state. RAS mutations are present in a large fraction of human cancers, notably in lung, colon and pancreatic cancers. These mutations bias RAS in cancer cells towards the RAS(ON) state, which binds and activates effector proteins to drive tumor growth and proliferation. Revolution Medicines has developed a platform of RAS(ON) tri-complex macrocyclic, small molecule inhibitors that bind noncovalently to an abundant intracellular protein, cyclophilin A (CypA). The resulting binary complex selectively engages RAS(ON), forming a tri-complex that sterically inhibits RAS interaction with its downstream effectors. We have generated multiple potent, orally bioavailable, covalent and noncovalent inhibitors including the investigational agents, daraxonrasib (RMC-6236) a RAS(ON) multi-selective inhibitor, elironrasib (RMC-6291) a RAS(ON) G12C-selective inhibitor, and RMC-5127 a RAS (ON) G12V-selective inhibitor.
Find out more about the BCMS lecture series.
