Allélspecifikus inhibitorok nyomában: a RASopátia konzorcium célpontjában a KRAS fehérje onkogén mutációi

Translated title of the contribution: Allele-specific inhibitors of mutant KRAS are in the focus of RASopathy consortium

Kinga Nyíri, Gergely Koppány, Gyula Pálfy, István Vida, Szilárd Tóth, Zoltán Orgován, Ivan Ranðeloviæ, Marcell Baranyi, Eszter Molnár, Miklós György Keserû, József Tóvári, András Perczel, Beáta G. Vértessy, József Tímár

Research output: Contribution to journalArticle

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.

Original languageHungarian
Pages (from-to)310-323
Number of pages14
JournalMagyar onkologia
Volume63
Issue number4
Publication statusPublished - Dec 9 2019

    Fingerprint

ASJC Scopus subject areas

  • Medicine(all)

Cite this

Nyíri, K., Koppány, G., Pálfy, G., Vida, I., Tóth, S., Orgován, Z., Ranðeloviæ, I., Baranyi, M., Molnár, E., Keserû, M. G., Tóvári, J., Perczel, A., Vértessy, B. G., & Tímár, J. (2019). Allélspecifikus inhibitorok nyomában: a RASopátia konzorcium célpontjában a KRAS fehérje onkogén mutációi. Magyar onkologia, 63(4), 310-323.