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71 results

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Page 1
Structure-based drug design enables conversion of a DFG-in binding CSF-1R kinase inhibitor to a DFG-out binding mode.
Meyers MJ, Pelc M, Kamtekar S, Day J, Poda GI, Hall MK, Michener ML, Reitz BA, Mathis KJ, Pierce BS, Parikh MD, Mischke DA, Long SA, Parlow JJ, Anderson DR, Thorarensen A. Meyers MJ, et al. Among authors: pelc m. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1543-7. doi: 10.1016/j.bmcl.2010.01.078. Epub 2010 Jan 21. Bioorg Med Chem Lett. 2010. PMID: 20137931
Structure based design of novel irreversible FAAH inhibitors.
Wang JL, Bowen SJ, Schweitzer BA, Madsen HM, McDonald J, Pelc MJ, Tenbrink RE, Beidler D, Thorarensen A. Wang JL, et al. Among authors: pelc mj. Bioorg Med Chem Lett. 2009 Oct 15;19(20):5970-4. doi: 10.1016/j.bmcl.2009.07.101. Epub 2009 Jul 25. Bioorg Med Chem Lett. 2009. PMID: 19765986
Discovery of novel spirocyclic inhibitors of fatty acid amide hydrolase (FAAH). Part 2. Discovery of 7-azaspiro[3.5]nonane urea PF-04862853, an orally efficacious inhibitor of fatty acid amide hydrolase (FAAH) for pain.
Meyers MJ, Long SA, Pelc MJ, Wang JL, Bowen SJ, Schweitzer BA, Wilcox MV, McDonald J, Smith SE, Foltin S, Rumsey J, Yang YS, Walker MC, Kamtekar S, Beidler D, Thorarensen A. Meyers MJ, et al. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6545-53. doi: 10.1016/j.bmcl.2011.08.048. Epub 2011 Aug 19. Bioorg Med Chem Lett. 2011. PMID: 21924613
Discovery of novel spirocyclic inhibitors of fatty acid amide hydrolase (FAAH). Part 1: identification of 7-azaspiro[3.5]nonane and 1-oxa-8-azaspiro[4.5]decane as lead scaffolds.
Meyers MJ, Long SA, Pelc MJ, Wang JL, Bowen SJ, Walker MC, Schweitzer BA, Madsen HM, Tenbrink RE, McDonald J, Smith SE, Foltin S, Beidler D, Thorarensen A. Meyers MJ, et al. Among authors: pelc mj. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6538-44. doi: 10.1016/j.bmcl.2011.08.055. Epub 2011 Aug 22. Bioorg Med Chem Lett. 2011. PMID: 21924614
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: pelc mj. 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
Discovery of an Oral Potent Selective Inhibitor of Hematopoietic Prostaglandin D Synthase (HPGDS).
Carron CP, Trujillo JI, Olson KL, Huang W, Hamper BC, Dice T, Neal BE, Pelc MJ, Day JE, Rohrer DC, Kiefer JR, Moon JB, Schweitzer BA, Blake TD, Turner SR, Woerndle R, Case BL, Bono CP, Dilworth VM, Funckes-Shippy CL, Hood BL, Jerome GM, Kornmeier CM, Radabaugh MR, Williams ML, Davies MS, Wegner CD, Welsch DJ, Abraham WM, Warren CJ, Dowty ME, Hua F, Zutshi A, Yang JZ, Thorarensen A. Carron CP, et al. Among authors: pelc mj. ACS Med Chem Lett. 2010 Feb 2;1(2):59-63. doi: 10.1021/ml900025z. eCollection 2010 May 13. ACS Med Chem Lett. 2010. PMID: 24900177 Free PMC article.
A novel autotaxin inhibitor reduces lysophosphatidic acid levels in plasma and the site of inflammation.
Gierse J, Thorarensen A, Beltey K, Bradshaw-Pierce E, Cortes-Burgos L, Hall T, Johnston A, Murphy M, Nemirovskiy O, Ogawa S, Pegg L, Pelc M, Prinsen M, Schnute M, Wendling J, Wene S, Weinberg R, Wittwer A, Zweifel B, Masferrer J. Gierse J, et al. Among authors: pelc m. J Pharmacol Exp Ther. 2010 Jul;334(1):310-7. doi: 10.1124/jpet.110.165845. Epub 2010 Apr 14. J Pharmacol Exp Ther. 2010. PMID: 20392816
71 results