Discovery of AZD4625, a Covalent Allosteric Inhibitor of the Mutant GTPase KRAS

Autor: Jason G, Kettle, Sharan K, Bagal, Sue, Bickerton, Michael S, Bodnarchuk, Scott, Boyd, Jason, Breed, Rodrigo J, Carbajo, Doyle J, Cassar, Atanu, Chakraborty, Sabina, Cosulich, Iain, Cumming, Michael, Davies, Nichola L, Davies, Andrew, Eatherton, Laura, Evans, Lyman, Feron, Shaun, Fillery, Emma S, Gleave, Frederick W, Goldberg, Lyndsey, Hanson, Stephanie, Harlfinger, Martin, Howard, Rachel, Howells, Anne, Jackson, Paul, Kemmitt, Gillian, Lamont, Scott, Lamont, Hilary J, Lewis, Libin, Liu, Michael J, Niedbala, Christopher, Phillips, Radek, Polanski, Piotr, Raubo, Graeme, Robb, David M, Robinson, Sarah, Ross, Matthew G, Sanders, Michael, Tonge, Rebecca, Whiteley, Stephen, Wilkinson, Junsheng, Yang, Wenman, Zhang
Rok vydání: 2022
Předmět:
Zdroj: Journal of medicinal chemistry. 65(9)
ISSN: 1520-4804
Popis: KRAS is an archetypal high-value intractable oncology drug target. The glycine to cysteine mutation at codon 12 represents an Achilles heel that has now rendered this important GTPase druggable. Herein, we report our structure-based drug design approach that led to the identification of
Databáze: OpenAIRE