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Page 1
Identification and Optimization of Novel Small c-Abl Kinase Activators Using Fragment and HTS Methodologies.
Simpson GL, Bertrand SM, Borthwick JA, Campobasso N, Chabanet J, Chen S, Coggins J, Cottom J, Christensen SB, Dawson HC, Evans HL, Hobbs AN, Hong X, Mangatt B, Munoz-Muriedas J, Oliff A, Qin D, Scott-Stevens P, Ward P, Washio Y, Yang J, Young RJ. Simpson GL, et al. Among authors: cottom j. J Med Chem. 2019 Feb 28;62(4):2154-2171. doi: 10.1021/acs.jmedchem.8b01872. Epub 2019 Feb 11. J Med Chem. 2019. PMID: 30689376
Discovery and characterization of a cell-permeable, small-molecule c-Abl kinase activator that binds to the myristoyl binding site.
Yang J, Campobasso N, Biju MP, Fisher K, Pan XQ, Cottom J, Galbraith S, Ho T, Zhang H, Hong X, Ward P, Hofmann G, Siegfried B, Zappacosta F, Washio Y, Cao P, Qu J, Bertrand S, Wang DY, Head MS, Li H, Moores S, Lai Z, Johanson K, Burton G, Erickson-Miller C, Simpson G, Tummino P, Copeland RA, Oliff A. Yang J, et al. Among authors: cottom j. Chem Biol. 2011 Feb 25;18(2):177-86. doi: 10.1016/j.chembiol.2010.12.013. Chem Biol. 2011. PMID: 21338916
Structure-guided optimization of small molecule c-Abl activators.
Hong X, Cao P, Washio Y, Simpson G, Campobasso N, Yang J, Borthwick J, Burton G, Chabanet J, Bertrand S, Evans H, Young RJ, Qu J, Li H, Cottom J, Ward P, Zhang H, Ho T, Qin D, Christensen S, Head MS. Hong X, et al. Among authors: cottom j. J Comput Aided Mol Des. 2014 Feb;28(2):75-87. doi: 10.1007/s10822-014-9731-5. Epub 2014 Feb 27. J Comput Aided Mol Des. 2014. PMID: 24573412 Free PMC article.
Identification of Purines and 7-Deazapurines as Potent and Selective Type I Inhibitors of Troponin I-Interacting Kinase (TNNI3K).
Lawhorn BG, Philp J, Zhao Y, Louer C, Hammond M, Cheung M, Fries H, Graves AP, Shewchuk L, Wang L, Cottom JE, Qi H, Zhao H, Totoritis R, Zhang G, Schwartz B, Li H, Sweitzer S, Holt DA, Gatto GJ Jr, Kallander LS. Lawhorn BG, et al. Among authors: cottom je. J Med Chem. 2015 Sep 24;58(18):7431-48. doi: 10.1021/acs.jmedchem.5b00931. Epub 2015 Sep 10. J Med Chem. 2015. PMID: 26355916
Monoacidic Inhibitors of the Kelch-like ECH-Associated Protein 1: Nuclear Factor Erythroid 2-Related Factor 2 (KEAP1:NRF2) Protein-Protein Interaction with High Cell Potency Identified by Fragment-Based Discovery.
Davies TG, Wixted WE, Coyle JE, Griffiths-Jones C, Hearn K, McMenamin R, Norton D, Rich SJ, Richardson C, Saxty G, Willems HM, Woolford AJ, Cottom JE, Kou JP, Yonchuk JG, Feldser HG, Sanchez Y, Foley JP, Bolognese BJ, Logan G, Podolin PL, Yan H, Callahan JF, Heightman TD, Kerns JK. Davies TG, et al. Among authors: cottom je. J Med Chem. 2016 Apr 28;59(8):3991-4006. doi: 10.1021/acs.jmedchem.6b00228. Epub 2016 Apr 12. J Med Chem. 2016. PMID: 27031670
Discovery and Development of TMPRSS6 Inhibitors Modulating Hepcidin Levels in Human Hepatocytes.
Béliveau F, Tarkar A, Dion SP, Désilets A, Ghinet MG, Boudreault PL, St-Georges C, Marsault É, Paone D, Collins J, Macphee CH, Campobasso N, Groy A, Cottom J, Ouellette M, Pope AJ, Leduc R. Béliveau F, et al. Among authors: cottom j. Cell Chem Biol. 2019 Nov 21;26(11):1559-1572.e9. doi: 10.1016/j.chembiol.2019.09.004. Epub 2019 Sep 19. Cell Chem Biol. 2019. PMID: 31543462 Free article.
Discovery of 6-({4-[2-(4-tert-butylphenyl)-1H-benzimidazol-4-yl]piperazin-1-yl}methyl)quinoxaline (WAY-207024): an orally active antagonist of the gonadotropin releasing hormone receptor (GnRH-R).
Pelletier JC, Chengalvala MV, Cottom JE, Feingold IB, Green DM, Hauze DB, Huselton CA, Jetter JW, Kopf GS, Lundquist JT, Magolda RL, Mann CW, Mehlmann JF, Rogers JF, Shanno LK, Adams WR, Tio CO, Wrobel JE. Pelletier JC, et al. J Med Chem. 2009 Apr 9;52(7):2148-52. doi: 10.1021/jm801572m. J Med Chem. 2009. PMID: 19271735
TLR2 agonism reverses chemotherapy-induced neutropenia in Macaca fascicularis.
Laping NJ, DeMartino MP, Cottom JE, Axten JM, Emery JG, Guss JH, Burman M, Foley JJ, Cheung M, Oliff A, Kumar S. Laping NJ, et al. Among authors: cottom je. Blood Adv. 2017 Dec 8;1(26):2553-2562. doi: 10.1182/bloodadvances.2017010611. eCollection 2017 Dec 12. Blood Adv. 2017. PMID: 29296907 Free PMC article.
2-phenyl-4-piperazinylbenzimidazoles: orally active inhibitors of the gonadotropin releasing hormone (GnRH) receptor.
Pelletier JC, Chengalvala M, Cottom J, Feingold I, Garrick L, Green D, Hauze D, Huselton C, Jetter J, Kao W, Kopf GS, Lundquist JT 4th, Mann C, Mehlmann J, Rogers J, Shanno L, Wrobel J. Pelletier JC, et al. Among authors: cottom j. Bioorg Med Chem. 2008 Jul 1;16(13):6617-40. doi: 10.1016/j.bmc.2008.05.024. Epub 2008 May 11. Bioorg Med Chem. 2008. PMID: 18511284
90 results