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Page 1
Discovery of 3-Cyano- N-(3-(1-isobutyrylpiperidin-4-yl)-1-methyl-4-(trifluoromethyl)-1 H-pyrrolo[2,3- b]pyridin-5-yl)benzamide: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C2 Inverse Agonist.
Schnute ME, Wennerstål M, Alley J, Bengtsson M, Blinn JR, Bolten CW, Braden T, Bonn T, Carlsson B, Caspers N, Chen M, Choi C, Collis LP, Crouse K, Färnegårdh M, Fennell KF, Fish S, Flick AC, Goos-Nilsson A, Gullberg H, Harris PK, Heasley SE, Hegen M, Hromockyj AE, Hu X, Husman B, Janosik T, Jones P, Kaila N, Kallin E, Kauppi B, Kiefer JR, Knafels J, Koehler K, Kruger L, Kurumbail RG, Kyne RE Jr, Li W, Löfstedt J, Long SA, Menard CA, Mente S, Messing D, Meyers MJ, Napierata L, Nöteberg D, Nuhant P, Pelc MJ, Prinsen MJ, Rhönnstad P, Backström-Rydin E, Sandberg J, Sandström M, Shah F, Sjöberg M, Sundell A, Taylor AP, Thorarensen A, Trujillo JI, Trzupek JD, Unwalla R, Vajdos FF, Weinberg RA, Wood DC, Xing L, Zamaratski E, Zapf CW, Zhao Y, Wilhelmsson A, Berstein G. Schnute ME, et al. Among authors: menard ca. J Med Chem. 2018 Dec 13;61(23):10415-10439. doi: 10.1021/acs.jmedchem.8b00392. Epub 2018 Sep 9. J Med Chem. 2018. PMID: 30130103
Design of Potent mRNA Decapping Scavenger Enzyme (DcpS) Inhibitors with Improved Physicochemical Properties To Investigate the Mechanism of Therapeutic Benefit in Spinal Muscular Atrophy (SMA).
Gopalsamy A, Narayanan A, Liu S, Parikh MD, Kyne RE Jr, Fadeyi O, Tones MA, Cherry JJ, Nabhan JF, LaRosa G, Petersen DN, Menard C, Foley TL, Noell S, Ren Y, Loria PM, Maglich-Goodwin J, Rong H, Jones LH. Gopalsamy A, et al. J Med Chem. 2017 Apr 13;60(7):3094-3108. doi: 10.1021/acs.jmedchem.7b00124. Epub 2017 Mar 16. J Med Chem. 2017. PMID: 28257199
Potent inhibitors of LpxC for the treatment of Gram-negative infections.
Brown MF, Reilly U, Abramite JA, Arcari JT, Oliver R, Barham RA, Che Y, Chen JM, Collantes EM, Chung SW, Desbonnet C, Doty J, Doroski M, Engtrakul JJ, Harris TM, Huband M, Knafels JD, Leach KL, Liu S, Marfat A, Marra A, McElroy E, Melnick M, Menard CA, Montgomery JI, Mullins L, Noe MC, O'Donnell J, Penzien J, Plummer MS, Price LM, Shanmugasundaram V, Thoma C, Uccello DP, Warmus JS, Wishka DG. Brown MF, et al. Among authors: menard ca. J Med Chem. 2012 Jan 26;55(2):914-23. doi: 10.1021/jm2014748. Epub 2012 Jan 11. J Med Chem. 2012. PMID: 22175825
Pyridone methylsulfone hydroxamate LpxC inhibitors for the treatment of serious gram-negative infections.
Montgomery JI, Brown MF, Reilly U, Price LM, Abramite JA, Arcari J, Barham R, Che Y, Chen JM, Chung SW, Collantes EM, Desbonnet C, Doroski M, Doty J, Engtrakul JJ, Harris TM, Huband M, Knafels JD, Leach KL, Liu S, Marfat A, McAllister L, McElroy E, Menard CA, Mitton-Fry M, Mullins L, Noe MC, O'Donnell J, Oliver R, Penzien J, Plummer M, Shanmugasundaram V, Thoma C, Tomaras AP, Uccello DP, Vaz A, Wishka DG. Montgomery JI, et al. Among authors: menard ca. J Med Chem. 2012 Feb 23;55(4):1662-70. doi: 10.1021/jm2014875. Epub 2012 Feb 8. J Med Chem. 2012. PMID: 22257165
Rational targeting of active-site tyrosine residues using sulfonyl fluoride probes.
Hett EC, Xu H, Geoghegan KF, Gopalsamy A, Kyne RE Jr, Menard CA, Narayanan A, Parikh MD, Liu S, Roberts L, Robinson RP, Tones MA, Jones LH. Hett EC, et al. Among authors: menard ca. ACS Chem Biol. 2015 Apr 17;10(4):1094-8. doi: 10.1021/cb5009475. Epub 2015 Jan 29. ACS Chem Biol. 2015. PMID: 25571984
Heterocyclic methylsulfone hydroxamic acid LpxC inhibitors as Gram-negative antibacterial agents.
McAllister LA, Montgomery JI, Abramite JA, Reilly U, Brown MF, Chen JM, Barham RA, Che Y, Chung SW, Menard CA, Mitton-Fry M, Mullins LM, Noe MC, O'Donnell JP, Oliver RM 3rd, Penzien JB, Plummer M, Price LM, Shanmugasundaram V, Tomaras AP, Uccello DP. McAllister LA, et al. Among authors: menard ca. Bioorg Med Chem Lett. 2012 Nov 15;22(22):6832-8. doi: 10.1016/j.bmcl.2012.09.058. Epub 2012 Sep 24. Bioorg Med Chem Lett. 2012. PMID: 23046961
In vitro and in vivo effects of 2,4 diaminoquinazoline inhibitors of the decapping scavenger enzyme DcpS: Context-specific modulation of SMN transcript levels.
Cherry JJ, DiDonato CJ, Androphy EJ, Calo A, Potter K, Custer SK, Du S, Foley TL, Gopalsamy A, Reedich EJ, Gordo SM, Gordon W, Hosea N, Jones LH, Krizay DK, LaRosa G, Li H, Mathur S, Menard CA, Patel P, Ramos-Zayas R, Rietz A, Rong H, Zhang B, Tones MA. Cherry JJ, et al. Among authors: menard ca. PLoS One. 2017 Sep 25;12(9):e0185079. doi: 10.1371/journal.pone.0185079. eCollection 2017. PLoS One. 2017. PMID: 28945765 Free PMC article.