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Inhibition of RAS function through targeting an allosteric regulatory site.
Spencer-Smith R, Koide A, Zhou Y, Eguchi RR, Sha F, Gajwani P, Santana D, Gupta A, Jacobs M, Herrero-Garcia E, Cobbert J, Lavoie H, Smith M, Rajakulendran T, Dowdell E, Okur MN, Dementieva I, Sicheri F, Therrien M, Hancock JF, Ikura M, Koide S, O'Bryan JP. Spencer-Smith R, et al. Among authors: lavoie h. Nat Chem Biol. 2017 Jan;13(1):62-68. doi: 10.1038/nchembio.2231. Epub 2016 Nov 7. Nat Chem Biol. 2017. PMID: 27820802 Free PMC article.
MEK drives BRAF activation through allosteric control of KSR proteins.
Lavoie H, Sahmi M, Maisonneuve P, Marullo SA, Thevakumaran N, Jin T, Kurinov I, Sicheri F, Therrien M. Lavoie H, et al. Nature. 2018 Feb 22;554(7693):549-553. doi: 10.1038/nature25478. Epub 2018 Feb 12. Nature. 2018. PMID: 29433126 Free PMC article.
Functional characterization of a PROTAC directed against BRAF mutant V600E.
Posternak G, Tang X, Maisonneuve P, Jin T, Lavoie H, Daou S, Orlicky S, Goullet de Rugy T, Caldwell L, Chan K, Aman A, Prakesch M, Poda G, Mader P, Wong C, Maier S, Kitaygorodsky J, Larsen B, Colwill K, Yin Z, Ceccarelli DF, Batey RA, Taipale M, Kurinov I, Uehling D, Wrana J, Durocher D, Gingras AC, Al-Awar R, Therrien M, Sicheri F. Posternak G, et al. Among authors: lavoie h. Nat Chem Biol. 2020 Nov;16(11):1170-1178. doi: 10.1038/s41589-020-0609-7. Epub 2020 Aug 10. Nat Chem Biol. 2020. PMID: 32778845 Free PMC article.
Dimerization-induced allostery in protein kinase regulation.
Lavoie H, Li JJ, Thevakumaran N, Therrien M, Sicheri F. Lavoie H, et al. Trends Biochem Sci. 2014 Oct;39(10):475-86. doi: 10.1016/j.tibs.2014.08.004. Epub 2014 Sep 11. Trends Biochem Sci. 2014. PMID: 25220378 Review.
100 results