Small-molecule covalent bond formation at tyrosine creates a binding site and inhibits activation of Ral GTPases

Ral (Ras-like) GTPases are directly activated by oncogenic Ras GTPases. Mutant K-Ras (G12C) has enabled the development of covalent K-Ras inhibitors currently in clinical trials. However, Ral, and the overwhelming majority of mutant oncogenic K-Ras, are devoid of a druggable pocket and lack an acces...

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Vydáno v:Proc Natl Acad Sci U S A
Hlavní autoři: Bum-Erdene, Khuchtumur, Liu, Degang, Gonzalez-Gutierrez, Giovanni, Ghozayel, Mona K., Xu, David, Meroueh, Samy O.
Médium: Artigo
Jazyk:Inglês
Vydáno: National Academy of Sciences 2020
Témata:
Biological Sciences
On-line přístup:https://ncbi.nlm.nih.gov/pmc/articles/PMC7132301/
https://ncbi.nlm.nih.gov/pubmed/32179690
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1073/pnas.1913654117
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