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Page 1
Design, synthesis, and biological evaluation of pyrazolopyrimidine-sulfonamides as potent multiple-mitotic kinase (MMK) inhibitors (part I).
Zhang L, Fan J, Chong JH, Cesena A, Tam BY, Gilson C, Boykin C, Wang D, Aivazian D, Marcotte D, Xiao G, Le Brazidec JY, Piao J, Lundgren K, Hong K, Vu K, Nguyen K, Gan LS, Silvian L, Ling L, Teng M, Reff M, Takeda N, Timple N, Wang Q, Morena R, Khan S, Zhao S, Li T, Lee WC, Taveras AG, Chao J. Zhang L, et al. Among authors: marcotte d. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5633-7. doi: 10.1016/j.bmcl.2011.06.129. Epub 2011 Jul 13. Bioorg Med Chem Lett. 2011. PMID: 21798738
Structure-based design of low-nanomolar PIM kinase inhibitors.
Ishchenko A, Zhang L, Le Brazidec JY, Fan J, Chong JH, Hingway A, Raditsis A, Singh L, Elenbaas B, Hong VS, Marcotte D, Silvian L, Enyedy I, Chao J. Ishchenko A, et al. Among authors: marcotte d. Bioorg Med Chem Lett. 2015 Feb 1;25(3):474-80. doi: 10.1016/j.bmcl.2014.12.041. Epub 2014 Dec 19. Bioorg Med Chem Lett. 2015. PMID: 25575657
ATP-Competitive MLKL Binders Have No Functional Impact on Necroptosis.
Ma B, Marcotte D, Paramasivam M, Michelsen K, Wang T, Bertolotti-Ciarlet A, Jones JH, Moree B, Butko M, Salafsky J, Sun X, McKee T, Silvian LF. Ma B, et al. Among authors: marcotte d. PLoS One. 2016 Nov 10;11(11):e0165983. doi: 10.1371/journal.pone.0165983. eCollection 2016. PLoS One. 2016. PMID: 27832137 Free PMC article.
Discovery and characterization of non-ATP site inhibitors of the mitogen activated protein (MAP) kinases.
Comess KM, Sun C, Abad-Zapatero C, Goedken ER, Gum RJ, Borhani DW, Argiriadi M, Groebe DR, Jia Y, Clampit JE, Haasch DL, Smith HT, Wang S, Song D, Coen ML, Cloutier TE, Tang H, Cheng X, Quinn C, Liu B, Xin Z, Liu G, Fry EH, Stoll V, Ng TI, Banach D, Marcotte D, Burns DJ, Calderwood DJ, Hajduk PJ. Comess KM, et al. Among authors: marcotte d. ACS Chem Biol. 2011 Mar 18;6(3):234-44. doi: 10.1021/cb1002619. Epub 2011 Jan 20. ACS Chem Biol. 2011. PMID: 21090814
Enabling structure-based drug design of Tyk2 through co-crystallization with a stabilizing aminoindazole inhibitor.
Argiriadi MA, Goedken ER, Banach D, Borhani DW, Burchat A, Dixon RW, Marcotte D, Overmeyer G, Pivorunas V, Sadhukhan R, Sousa S, Moore NS, Tomlinson M, Voss J, Wang L, Wishart N, Woller K, Talanian RV. Argiriadi MA, et al. Among authors: marcotte d. BMC Struct Biol. 2012 Sep 20;12:22. doi: 10.1186/1472-6807-12-22. BMC Struct Biol. 2012. PMID: 22995073 Free PMC article.
Elucidation of the GSK3α Structure Informs the Design of Novel, Paralog-Selective Inhibitors.
Amaral B, Capacci A, Anderson T, Tezer C, Bajrami B, Lulla M, Lucas B, Chodaparambil JV, Marcotte D, Kumar PR, Murugan P, Spilker K, Cullivan M, Wang T, Peterson AC, Enyedy I, Ma B, Chen T, Yousaf Z, Calhoun M, Golonzhka O, Dillon GM, Koirala S. Amaral B, et al. Among authors: marcotte d. ACS Chem Neurosci. 2023 Mar 15;14(6):1080-1094. doi: 10.1021/acschemneuro.2c00476. Epub 2023 Feb 22. ACS Chem Neurosci. 2023. PMID: 36812145 Free PMC article.
Discovery of structural diverse reversible BTK inhibitors utilized to develop a novel in vivo CD69 and CD86 PK/PD mouse model.
Vandeveer GH, Arduini RM, Baker DP, Barry K, Bohnert T, Bowden-Verhoek JK, Conlon P, Cullen PF, Guan B, Jenkins TJ, Liao SY, Lin L, Liu YT, Marcotte D, Mertsching E, Metrick CM, Negrou E, Powell N, Scott D, Silvian LF, Hopkins BT. Vandeveer GH, et al. Among authors: marcotte d. Bioorg Med Chem Lett. 2023 Jan 15;80:129108. doi: 10.1016/j.bmcl.2022.129108. Epub 2022 Dec 17. Bioorg Med Chem Lett. 2023. PMID: 36538993
Discovery of Potent, Selective, and Brain-Penetrant Apoptosis Signal-Regulating Kinase 1 (ASK1) Inhibitors that Modulate Brain Inflammation In Vivo.
Jones JH, Xin Z, Himmelbauer M, Dechantsreiter M, Enyedy I, Hedde J, Fang T, Coomaraswamy J, King KW, Murugan P, Santoro JC, Hesson T, Walther DM, Wei R, Zheng F, Marcotte DJ, Spilker K, Kumar PR, Liu Y, Gilfillan R, Gonzalez-Lopez de Turiso F. Jones JH, et al. Among authors: marcotte dj. J Med Chem. 2021 Oct 28;64(20):15402-15419. doi: 10.1021/acs.jmedchem.1c01458. Epub 2021 Oct 15. J Med Chem. 2021. PMID: 34653340
84 results