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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: weinberg ra. 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
2-(6-Phenyl-1H-indazol-3-yl)-1H-benzo[d]imidazoles: design and synthesis of a potent and isoform selective PKC-zeta inhibitor.
Trujillo JI, Kiefer JR, Huang W, Thorarensen A, Xing L, Caspers NL, Day JE, Mathis KJ, Kretzmer KK, Reitz BA, Weinberg RA, Stegeman RA, Wrightstone A, Christine L, Compton R, Li X. Trujillo JI, et al. Among authors: weinberg ra. Bioorg Med Chem Lett. 2009 Feb 1;19(3):908-11. doi: 10.1016/j.bmcl.2008.11.105. Epub 2008 Dec 6. Bioorg Med Chem Lett. 2009. PMID: 19097791
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. 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
Homo-timeric structural model of human microsomal prostaglandin E synthase-1 and characterization of its substrate/inhibitor binding interactions.
Xing L, Kurumbail RG, Frazier RB, Davies MS, Fujiwara H, Weinberg RA, Gierse JK, Caspers N, Carter JS, McDonald JJ, Moore WM, Vazquez ML. Xing L, et al. Among authors: weinberg ra. J Comput Aided Mol Des. 2009 Jan;23(1):13-24. doi: 10.1007/s10822-008-9233-4. Epub 2008 Sep 6. J Comput Aided Mol Des. 2009. PMID: 18777160
Expression, purification, characterization and crystallization of non- and phosphorylated states of JAK2 and JAK3 kinase domain.
Hall T, Emmons TL, Chrencik JE, Gormley JA, Weinberg RA, Leone JW, Hirsch JL, Saabye MJ, Schindler JF, Day JE, Williams JM, Kiefer JR, Lightle SA, Harris MS, Guru S, Fischer HD, Tomasselli AG. Hall T, et al. Among authors: weinberg ra. Protein Expr Purif. 2010 Jan;69(1):54-63. doi: 10.1016/j.pep.2009.09.011. Epub 2009 Sep 23. Protein Expr Purif. 2010. PMID: 19781647
Structural and thermodynamic characterization of the TYK2 and JAK3 kinase domains in complex with CP-690550 and CMP-6.
Chrencik JE, Patny A, Leung IK, Korniski B, Emmons TL, Hall T, Weinberg RA, Gormley JA, Williams JM, Day JE, Hirsch JL, Kiefer JR, Leone JW, Fischer HD, Sommers CD, Huang HC, Jacobsen EJ, Tenbrink RE, Tomasselli AG, Benson TE. Chrencik JE, et al. Among authors: weinberg ra. J Mol Biol. 2010 Jul 16;400(3):413-33. doi: 10.1016/j.jmb.2010.05.020. Epub 2010 May 15. J Mol Biol. 2010. PMID: 20478313
Novel insights into the cellular mechanisms of the anti-inflammatory effects of NF-kappaB essential modulator binding domain peptides.
Baima ET, Guzova JA, Mathialagan S, Nagiec EE, Hardy MM, Song LR, Bonar SL, Weinberg RA, Selness SR, Woodard SS, Chrencik J, Hood WF, Schindler JF, Kishore N, Mbalaviele G. Baima ET, et al. Among authors: weinberg ra. J Biol Chem. 2010 Apr 30;285(18):13498-506. doi: 10.1074/jbc.M109.099895. Epub 2010 Feb 18. J Biol Chem. 2010. PMID: 20167598 Free PMC article.
450 results