Article
Identification of a Highly Cooperative PROTAC Degrader Targeting GTP-Loaded KRAS(On) Alleles.
Journal of the American Chemical Society - 12 Nov 2025
Vetma Vesna, Puoti Ilaria, Karolak Natalia K, Chakraborti Sohini, Diers Emelyne, Girardi Enrico, Khan Shakil, Kidd Giorgia, Kropatsch Katrin G, Mclennan Ross, O'Connor Suzanne, Samwer Matthias, Trainor Nicole, Whitworth Claire, Wijaya Andre J, Wong Jeff Y F, Zollman David, Farnaby William, Popow Johannes, Ciulli Alessio, Ettmayer Peter, McAulay Kirsten
Abstract excerpt
Kirsten rat sarcoma viral oncogene homologue (KRAS) is a frequently mutated oncogene in multiple types of cancer and is a high priority target for oncology drug development. There are many different KRAS mutations, including mutations that favor the GTP-loaded hydrolysis-incompetent "active" state of KRAS, KRAS(on), that can lead to tumorigenesis. However, small molecule interventions thus far have predominantly...
Read the complete abstract on PubMedTopics
- Proto-Oncogene Proteins p21(ras)
- Humans
- Guanosine Triphosphate
- Alleles