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Page 1
Development of Orally Efficacious Allosteric Inhibitors of TNFα via Fragment-Based Drug Design.
Dietrich JD, Longenecker KL, Wilson NS, Goess C, Panchal SC, Swann SL, Petros AM, Hobson AD, Ihle D, Song D, Richardson P, Comess KM, Cox PB, Dombrowski A, Sarris K, Donnelly-Roberts DL, Duignan DB, Gomtsyan A, Jung P, Krueger AC, Mathieu S, McClure A, Stoll VS, Wetter J, Mankovich JA, Hajduk PJ, Vasudevan A, Stoffel RH, Sun C. Dietrich JD, et al. Among authors: donnelly roberts dl. J Med Chem. 2021 Jan 14;64(1):417-429. doi: 10.1021/acs.jmedchem.0c01280. Epub 2020 Dec 30. J Med Chem. 2021. PMID: 33378180
NRF2 activator A-1396076 ameliorates inflammation in autoimmune disease models by inhibiting antigen dependent T cell activation.
Goess C, Terrillon S, Mayo M, Bousquet P, Wallace C, Hart M, Mathieu S, Twomey R, Donnelly-Roberts D, Namovic M, Jung P, Hu M, Richardson P, Esbenshade T, Cuff CA. Goess C, et al. J Transl Autoimmun. 2020 Dec 23;4:100079. doi: 10.1016/j.jtauto.2020.100079. eCollection 2021. J Transl Autoimmun. 2020. PMID: 33490940 Free PMC article.
Structure-activity relationship studies on N'-aryl carbohydrazide P2X7 antagonists.
Nelson DW, Sarris K, Kalvin DM, Namovic MT, Grayson G, Donnelly-Roberts DL, Harris R, Honore P, Jarvis MF, Faltynek CR, Carroll WA. Nelson DW, et al. Among authors: donnelly roberts dl. J Med Chem. 2008 May 22;51(10):3030-4. doi: 10.1021/jm701516f. Epub 2008 Apr 26. J Med Chem. 2008. PMID: 18438986
Discovery of 3-methyl-N-(1-oxy-3',4',5',6'-tetrahydro-2'H-[2,4'-bipyridine]-1'-ylmethyl)benzamide (ABT-670), an orally bioavailable dopamine D4 agonist for the treatment of erectile dysfunction.
Patel MV, Kolasa T, Mortell K, Matulenko MA, Hakeem AA, Rohde JJ, Nelson SL, Cowart MD, Nakane M, Miller LN, Uchic ME, Terranova MA, El-Kouhen OF, Donnelly-Roberts DL, Namovic MT, Hollingsworth PR, Chang R, Martino BR, Wetter JM, Marsh KC, Martin R, Darbyshire JF, Gintant G, Hsieh GC, Moreland RB, Sullivan JP, Brioni JD, Stewart AO. Patel MV, et al. J Med Chem. 2006 Dec 14;49(25):7450-65. doi: 10.1021/jm060662k. J Med Chem. 2006. PMID: 17149874
Synthesis and SAR of 4-aminocyclopentapyrrolidines as N-type Ca²⁺ channel blockers with analgesic activity.
Beebe X, Darczak D, Henry RF, Vortherms T, Janis R, Namovic M, Donnelly-Roberts D, Kage KL, Surowy C, Milicic I, Niforatos W, Swensen A, Marsh KC, Wetter JM, Franklin P, Baker S, Zhong C, Simler G, Gomez E, Boyce-Rustay JM, Zhu CZ, Stewart AO, Jarvis MF, Scott VE. Beebe X, et al. Bioorg Med Chem. 2012 Jul 1;20(13):4128-39. doi: 10.1016/j.bmc.2012.04.057. Epub 2012 May 4. Bioorg Med Chem. 2012. PMID: 22626552
1-aryl-3-(4-pyridine-2-ylpiperazin-1-yl)propan-1-one oximes as potent dopamine D4 receptor agonists for the treatment of erectile dysfunction.
Kolasa T, Matulenko MA, Hakeem AA, Patel MV, Mortell K, Bhatia P, Henry R, Nakane M, Hsieh GC, Terranova MA, Uchic ME, Miller LN, Chang R, Donnelly-Roberts DL, Namovic MT, Hollingsworth PR, Martino B, El Kouhen O, Marsh KC, Wetter JM, Moreland RB, Brioni JD, Stewart AO. Kolasa T, et al. J Med Chem. 2006 Aug 24;49(17):5093-109. doi: 10.1021/jm060279f. J Med Chem. 2006. PMID: 16913699
Synthesis and activity of N-cyanoguanidine-piperazine P2X7 antagonists.
Betschmann P, Bettencourt B, Donnelly-Roberts D, Friedman M, George J, Hirst G, Josephsohn N, Konopacki D, Li B, Maull J, Morytko MJ, Moore NS, Namovic M, Rafferty P, Salmeron-Garcia JA, Tarcsa E, Wang L, Woller K. Betschmann P, et al. Bioorg Med Chem Lett. 2008 Jul 15;18(14):3848-51. doi: 10.1016/j.bmcl.2008.06.055. Epub 2008 Jun 20. Bioorg Med Chem Lett. 2008. PMID: 18595695
Small Molecule and Pooled CRISPR Screens Investigating IL17 Signaling Identify BRD2 as a Novel Contributor to Keratinocyte Inflammatory Responses.
Slivka PF, Hsieh CL, Lipovsky A, Pratt SD, Locklear J, Namovic MT, McDonald HA, Wetter J, Edelmayer R, Hu M, Murphy E, Domanus M, Lu C, Duggan R, King J, Scott VE, Donnelly-Roberts D, Slavin A, Gopalakrishnan S, Chung N, Goedken ER. Slivka PF, et al. ACS Chem Biol. 2019 May 17;14(5):857-872. doi: 10.1021/acschembio.8b00260. Epub 2019 Apr 15. ACS Chem Biol. 2019. PMID: 30938974
81 results