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Page 1
Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers.
Hatzivassiliou G, Haling JR, Chen H, Song K, Price S, Heald R, Hewitt JF, Zak M, Peck A, Orr C, Merchant M, Hoeflich KP, Chan J, Luoh SM, Anderson DJ, Ludlam MJ, Wiesmann C, Ultsch M, Friedman LS, Malek S, Belvin M. Hatzivassiliou G, et al. Among authors: zak m. Nature. 2013 Sep 12;501(7466):232-6. doi: 10.1038/nature12441. Epub 2013 Aug 11. Nature. 2013. PMID: 23934108
Structure-based discovery of C-2 substituted imidazo-pyrrolopyridine JAK1 inhibitors with improved selectivity over JAK2.
Labadie S, Dragovich PS, Barrett K, Blair WS, Bergeron P, Chang C, Deshmukh G, Eigenbrot C, Ghilardi N, Gibbons P, Hurley CA, Johnson A, Kenny JR, Kohli PB, Kulagowski JJ, Liimatta M, Lupardus PJ, Mendonca R, Murray JM, Pulk R, Shia S, Steffek M, Ubhayakar S, Ultsch M, van Abbema A, Ward S, Zak M. Labadie S, et al. Among authors: zak m. Bioorg Med Chem Lett. 2012 Dec 15;22(24):7627-33. doi: 10.1016/j.bmcl.2012.10.008. Epub 2012 Oct 11. Bioorg Med Chem Lett. 2012. PMID: 23107482
Discovery and optimization of C-2 methyl imidazopyrrolopyridines as potent and orally bioavailable JAK1 inhibitors with selectivity over JAK2.
Zak M, Mendonca R, Balazs M, Barrett K, Bergeron P, Blair WS, Chang C, Deshmukh G, Devoss J, Dragovich PS, Eigenbrot C, Ghilardi N, Gibbons P, Gradl S, Hamman C, Hanan EJ, Harstad E, Hewitt PR, Hurley CA, Jin T, Johnson A, Johnson T, Kenny JR, Koehler MF, Bir Kohli P, Kulagowski JJ, Labadie S, Liao J, Liimatta M, Lin Z, Lupardus PJ, Maxey RJ, Murray JM, Pulk R, Rodriguez M, Savage S, Shia S, Steffek M, Ubhayakar S, Ultsch M, van Abbema A, Ward SI, Xiao L, Xiao Y. Zak M, et al. J Med Chem. 2012 Jul 12;55(13):6176-93. doi: 10.1021/jm300628c. Epub 2012 Jun 28. J Med Chem. 2012. PMID: 22698084
Identification of C-2 hydroxyethyl imidazopyrrolopyridines as potent JAK1 inhibitors with favorable physicochemical properties and high selectivity over JAK2.
Zak M, Hurley CA, Ward SI, Bergeron P, Barrett K, Balazs M, Blair WS, Bull R, Chakravarty P, Chang C, Crackett P, Deshmukh G, DeVoss J, Dragovich PS, Eigenbrot C, Ellwood C, Gaines S, Ghilardi N, Gibbons P, Gradl S, Gribling P, Hamman C, Harstad E, Hewitt P, Johnson A, Johnson T, Kenny JR, Koehler MF, Bir Kohli P, Labadie S, Lee WP, Liao J, Liimatta M, Mendonca R, Narukulla R, Pulk R, Reeve A, Savage S, Shia S, Steffek M, Ubhayakar S, van Abbema A, Aliagas I, Avitabile-Woo B, Xiao Y, Yang J, Kulagowski JJ. Zak M, et al. J Med Chem. 2013 Jun 13;56(11):4764-85. doi: 10.1021/jm4004895. Epub 2013 May 31. J Med Chem. 2013. PMID: 23659214
Fragment-based design of 3-aminopyridine-derived amides as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
Dragovich PS, Zhao G, Baumeister T, Bravo B, Giannetti AM, Ho YC, Hua R, Li G, Liang X, Ma X, O'Brien T, Oh A, Skelton NJ, Wang C, Wang W, Wang Y, Xiao Y, Yuen PW, Zak M, Zhao Q, Zheng X. Dragovich PS, et al. Among authors: zak m. Bioorg Med Chem Lett. 2014 Feb 1;24(3):954-62. doi: 10.1016/j.bmcl.2013.12.062. Epub 2013 Dec 21. Bioorg Med Chem Lett. 2014. PMID: 24433859
Lung-restricted inhibition of Janus kinase 1 is effective in rodent models of asthma.
Dengler HS, Wu X, Peng I, Rinderknecht CH, Kwon Y, Suto E, Kohli PB, Liimatta M, Barrett K, Lloyd J, Cain G, Briggs M, Addo S, Salmon G, Ubhayakar S, Deshmukh G, Shahidi-Latham SK, Quiason-Huynh CM, Jackman J, Liu J, Ray NC, Goodacre SC, Johnson A, McKenzie BS, Lee WP, Zak M, Kenny JR, Ghilardi N. Dengler HS, et al. Among authors: zak m. Sci Transl Med. 2018 Nov 21;10(468):eaao2151. doi: 10.1126/scitranslmed.aao2151. Sci Transl Med. 2018. PMID: 30463918
A restricted role for TYK2 catalytic activity in human cytokine responses revealed by novel TYK2-selective inhibitors.
Sohn SJ, Barrett K, Van Abbema A, Chang C, Kohli PB, Kanda H, Smith J, Lai Y, Zhou A, Zhang B, Yang W, Williams K, Macleod C, Hurley CA, Kulagowski JJ, Lewin-Koh N, Dengler HS, Johnson AR, Ghilardi N, Zak M, Liang J, Blair WS, Magnuson S, Wu LC. Sohn SJ, et al. Among authors: zak m. J Immunol. 2013 Sep 1;191(5):2205-16. doi: 10.4049/jimmunol.1202859. Epub 2013 Jul 26. J Immunol. 2013. PMID: 23894201 Free PMC article.
Design and evaluation of novel 8-oxo-pyridopyrimidine Jak1/2 inhibitors.
Labadie S, Barrett K, Blair WS, Chang C, Deshmukh G, Eigenbrot C, Gibbons P, Johnson A, Kenny JR, Kohli PB, Liimatta M, Lupardus PJ, Shia S, Steffek M, Ubhayakar S, van Abbema A, Zak M. Labadie S, et al. Among authors: zak m. Bioorg Med Chem Lett. 2013 Nov 1;23(21):5923-30. doi: 10.1016/j.bmcl.2013.08.082. Epub 2013 Aug 27. Bioorg Med Chem Lett. 2013. PMID: 24042009
342 results