[Allele-specific inhibitors of mutant KRAS are in the focus of RASopathy consortium].

[Allele-specific inhibitors of mutant KRAS are in the focus of RASopathy consortium].
Magy Onkol. 2019 Dec 09;63(4):310-323
Authors: Nyíri K, Koppány G, Pálfy G, Vida I, Tóth S, Orgován Z, Ranðeloviæ I, Baranyi M, Molnár E, Keserû MG, Tóvári J, Perczel A, Vértessy BG, Tímár J
Abstract
The RASopathy consortium was built from research groups of the Budapest University of Technology and Economics, Eötvös Loránd University, Semmelweis University and two startups: KINETO Lab Ltd. and Fototronic Ltd. The goal was to design and test novel covalent and allele-specific KRAS small molecular inhibitors. KRAS is the most frequently mutated human oncogene which was unsuccessfully targeted until recently. The consortium established G12C-expressing bacterial and human cancer cell models (homo- and heterozygous variants) of lung, colorectal and pancreatic tumors. Using covalent fragment and acrylamide warhead libraries we were able to select novel candidates of small molecular G12C-specific inhibitors which were compared to published best-in-class drug candidates.
PMID: 31821386 [PubMed - in process]

Source: Magyar Onkologia - December 8, 2019 Category: Cancer & Oncology Authors: Nyíri K, Koppány G, Pálfy G, Vida I, Tóth S, Orgován Z, Ranðeloviæ I, Baranyi M, Molnár E, Keserû MG, Tóvári J, Perczel A, Vértessy BG, Tímár J Tags: Magy Onkol Source Type: research