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Magy Onkol. 2019 Dec 9;63(4):310-323. Epub 2019 Nov 25.

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

[Article in Hungarian; Abstract available in Hungarian from the publisher]

Author information

1
Alkalmazott Biotechnológiai és Élelmiszertudományi Tanszék, BME, Természettudományi Kutatóközpont, Budapest, Hungary.
2
Szerkezeti Kémia és Biológia Laboratórium, Budapest, Hungary.
3
Enzimológiai Intézet, Budapest, Hungary.
4
ELTE Kémiai Intézet, Gyógyszerkémiai Kutatócsoport, Budapest, Hungary.
5
KINETO Lab Kft., Budapest, Hungary.
6
II. Sz. Patológiai Intézet, Semmelweis Egyetem, Budapest, Hungary. jtimar@gmail.com.
7
MTA-ELTE Fehérjemodellezõ Kutatócsoport, Budapest, Hungary.

Abstract

in English, Hungarian

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
[Indexed for MEDLINE]
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