One RAS mutation can now be drugged because it offers a reactive handle. Most RAS mutations do not, so new chemistry is needed to grab other amino acids.
KRAS G12C inhibitors work by covalently modifying a cysteine. G12D, G12V and G13D, which together account for most RAS-driven cancer, lack that cysteine. Aspartate-targeting and lysine-targeting covalent chemistries, non-covalent tri-complex RAS(ON) inhibitors and pan-RAS agents are all in early clinical development. The proposal is a focused public-private chemistry programme on non-cysteine covalent warheads with tolerable reactivity, plus open sharing of failed warhead chemotypes.
One bottleneck page and 24 idea pages on OnCo cite this paper by its DOI; this record gives the citation a page of its own so a reader can follow it without leaving OnCo. Read the abstract above alongside the citing pages listed under Related; the record was created automatically from the Europe PMC entry and its figures have not been checked by hand.
One of the most cited trial reports Europe PMC returns for KRAS in Colorectal cancer, so it is a natural first reading for anyone weighing the idea it is linked from. The record was linked automatically by title and abstract; read the abstract above and the paper itself before relying on any figure.
One of the most cited trial reports Europe PMC returns for KRAS in Colorectal cancer, so it is a natural first reading for anyone weighing the idea it is linked from. The record was linked automatically by title and abstract; read the abstract above and the paper itself before relying on any figure.
One of the most cited trial reports Europe PMC returns for KRAS in Colorectal cancer, so it is a natural first reading for anyone weighing the idea it is linked from. The record was linked automatically by title and abstract; read the abstract above and the paper itself before relying on any figure.
Shares Prognostic role of KRAS and BRAF in stage II and III resected colon cancer: results of the translational study on the PETACC-3, EORTC 40993, SAKK 60-00 trial, Cetuximab plus irinotecan, fluorouracil, and leucovorin as first-line treatment for metastatic colorectal cancer: updated analysis of overall survival according to tumor KRAS and BRAF mutation status, Wild-type KRAS is required for panitumumab efficacy in patients with metastatic colorectal cancer, Study of Daraxonrasib (RMC-6236) in Patients With Resected Pancreatic Ductal Adenocarcinoma (PDAC).
Shares RASolute 302, Revolution Medicines, Daraxonrasib, KRAS & RAS inhibitors.
Shares Revolution Medicines, Adagrasib, Daraxonrasib, Sotorasib.
Shares CodeBreaK 300, Adagrasib, Sotorasib, KRAS & RAS inhibitors.
Shares RASolute 302, Daraxonrasib, Sotorasib, KRAS & RAS inhibitors.
Shares Study of Zoldonrasib + Chemo of Investigator's Choice vs Placebo + Chemo of Investigator's Choice as First-line Treatment in Metastatic KRAS G12D-muta, Revolution Medicines, Daraxonrasib, KRAS & RAS inhibitors.
Shares Adagrasib, Sotorasib, KRAS & RAS inhibitors, KRAS.
Shares Study of Daraxonrasib (RMC-6236) in Patients With Resected Pancreatic Ductal Adenocarcinoma (PDAC), Study of Daraxonrasib and Daraxonrasib + GnP as First-line Treatment in Patients With Metastatic Pancreatic Adenocarcinoma, RASolute 302, Revolution Medicines.