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Structure-based design and optimization of a new class of small molecule inhibitors targeting the P-stalk binding pocket of ricin.
Rudolph MJ, Dutta A, Tsymbal AM, McLaughlin JE, Chen Y, Davis SA, Theodorous SA, Pierce M, Algava B, Zhang X, Szekely Z, Roberge JY, Li XP, Tumer NE. Rudolph MJ, et al. Among authors: roberge jy. Bioorg Med Chem. 2024 Feb 15;100:117614. doi: 10.1016/j.bmc.2024.117614. Epub 2024 Feb 5. Bioorg Med Chem. 2024. PMID: 38340640 Free article.
Structure-Activity Relationship of a Pyrrole Based Series of PfPKG Inhibitors as Anti-Malarials.
Gilleran JA, Ashraf K, Delvillar M, Eck T, Fondekar R, Miller EB, Hutchinson A, Dong A, Seitova A, De Souza ML, Augeri D, Halabelian L, Siekierka J, Rotella DP, Gordon J, Childers WE, Grier MC, Staker BL, Roberge JY, Bhanot P. Gilleran JA, et al. Among authors: roberge jy. J Med Chem. 2024 Mar 14;67(5):3467-3503. doi: 10.1021/acs.jmedchem.3c01795. Epub 2024 Feb 19. J Med Chem. 2024. PMID: 38372781
Identification of purine inhibitors of phosphodiesterase 7 (PDE7).
Pitts WJ, Vaccaro W, Huynh T, Leftheris K, Roberge JY, Barbosa J, Guo J, Brown B, Watson A, Donaldson K, Starling GC, Kiener PA, Poss MA, Dodd JH, Barrish JC. Pitts WJ, et al. Among authors: roberge jy. Bioorg Med Chem Lett. 2004 Jun 7;14(11):2955-8. doi: 10.1016/j.bmcl.2004.03.021. Bioorg Med Chem Lett. 2004. PMID: 15125967
Discovery of 2-(phenoxypyridine)-3-phenylureas as small molecule P2Y1 antagonists.
Chao H, Turdi H, Herpin TF, Roberge JY, Liu Y, Schnur DM, Poss MA, Rehfuss R, Hua J, Wu Q, Price LA, Abell LM, Schumacher WA, Bostwick JS, Steinbacher TE, Stewart AB, Ogletree ML, Huang CS, Chang M, Cacace AM, Arcuri MJ, Celani D, Wexler RR, Lawrence RM. Chao H, et al. Among authors: roberge jy. J Med Chem. 2013 Feb 28;56(4):1704-14. doi: 10.1021/jm301708u. Epub 2013 Feb 18. J Med Chem. 2013. PMID: 23368907
Design, synthesis, and biological evaluation of deuterated C-aryl glycoside as a potent and long-acting renal sodium-dependent glucose cotransporter 2 inhibitor for the treatment of type 2 diabetes.
Xu G, Lv B, Roberge JY, Xu B, Du J, Dong J, Chen Y, Peng K, Zhang L, Tang X, Feng Y, Xu M, Fu W, Zhang W, Zhu L, Deng Z, Sheng Z, Welihinda A, Sun X. Xu G, et al. Among authors: roberge jy. J Med Chem. 2014 Feb 27;57(4):1236-51. doi: 10.1021/jm401780b. Epub 2014 Feb 12. J Med Chem. 2014. PMID: 24456245
Discovery and initial SAR of imidazoquinoxalines as inhibitors of the Src-family kinase p56(Lck).
Chen P, Norris D, Iwanowicz EJ, Spergel SH, Lin J, Gu HH, Shen Z, Wityak J, Lin TA, Pang S, De Fex HF, Pitt S, Shen DR, Doweyko AM, Bassolino DA, Roberge JY, Poss MA, Chen BC, Schieven GL, Barrish JC. Chen P, et al. Among authors: roberge jy. Bioorg Med Chem Lett. 2002 May 20;12(10):1361-4. doi: 10.1016/s0960-894x(02)00191-9. Bioorg Med Chem Lett. 2002. PMID: 11992777
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