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Page 1
Synthesis, crystal structure, and activity of pyrazole-based inhibitors of p38 kinase.
Graneto MJ, Kurumbail RG, Vazquez ML, Shieh HS, Pawlitz JL, Williams JM, Stallings WC, Geng L, Naraian AS, Koszyk FJ, Stealey MA, Xu XD, Weier RM, Hanson GJ, Mourey RJ, Compton RP, Mnich SJ, Anderson GD, Monahan JB, Devraj R. Graneto MJ, et al. Among authors: vazquez ml. J Med Chem. 2007 Nov 15;50(23):5712-9. doi: 10.1021/jm0611915. Epub 2007 Oct 19. J Med Chem. 2007. PMID: 17948975
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: vazquez ml. 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
Distinction of microsomal prostaglandin E synthase-1 (mPGES-1) inhibition from cyclooxygenase-2 inhibition in cells using a novel, selective mPGES-1 inhibitor.
Mbalaviele G, Pauley AM, Shaffer AF, Zweifel BS, Mathialagan S, Mnich SJ, Nemirovskiy OV, Carter J, Gierse JK, Wang JL, Vazquez ML, Moore WM, Masferrer JL. Mbalaviele G, et al. Among authors: vazquez ml. Biochem Pharmacol. 2010 May 15;79(10):1445-54. doi: 10.1016/j.bcp.2010.01.003. Epub 2010 Jan 11. Biochem Pharmacol. 2010. PMID: 20067770
Discovery and SAR of PF-4693627, a potent, selective and orally bioavailable mPGES-1 inhibitor for the potential treatment of inflammation.
Arhancet GB, Walker DP, Metz S, Fobian YM, Heasley SE, Carter JS, Springer JR, Jones DE, Hayes MJ, Shaffer AF, Jerome GM, Baratta MT, Zweifel B, Moore WM, Masferrer JL, Vazquez ML. Arhancet GB, et al. Among authors: vazquez ml. Bioorg Med Chem Lett. 2013 Feb 15;23(4):1114-9. doi: 10.1016/j.bmcl.2012.11.109. Epub 2012 Dec 6. Bioorg Med Chem Lett. 2013. PMID: 23260349
Novel benzoxazole inhibitors of mPGES-1.
Kablaoui N, Patel S, Shao J, Demian D, Hoffmaster K, Berlioz F, Vazquez ML, Moore WM, Nugent RA. Kablaoui N, et al. Among authors: vazquez ml. Bioorg Med Chem Lett. 2013 Feb 1;23(3):907-11. doi: 10.1016/j.bmcl.2012.10.040. Epub 2012 Oct 16. Bioorg Med Chem Lett. 2013. PMID: 23266122
Synthesis and biological evaluation of substituted benzoxazoles as inhibitors of mPGES-1: use of a conformation-based hypothesis to facilitate compound design.
Walker DP, Arhancet GB, Lu HF, Heasley SE, Metz S, Kablaoui NM, Franco FM, Hanau CE, Scholten JA, Springer JR, Fobian YM, Carter JS, Xing L, Yang S, Shaffer AF, Jerome GM, Baratta MT, Moore WM, Vazquez ML. Walker DP, et al. Among authors: vazquez ml. Bioorg Med Chem Lett. 2013 Feb 15;23(4):1120-6. doi: 10.1016/j.bmcl.2012.11.107. Epub 2012 Dec 12. Bioorg Med Chem Lett. 2013. PMID: 23298810
Development of a high-throughput crystal structure-determination platform for JAK1 using a novel metal-chelator soaking system.
Caspers NL, Han S, Rajamohan F, Hoth LR, Geoghegan KF, Subashi TA, Vazquez ML, Kaila N, Cronin CN, Johnson E, Kurumbail RG. Caspers NL, et al. Among authors: vazquez ml. Acta Crystallogr F Struct Biol Commun. 2016 Nov 1;72(Pt 11):840-845. doi: 10.1107/S2053230X16016356. Epub 2016 Oct 27. Acta Crystallogr F Struct Biol Commun. 2016. PMID: 27827355 Free PMC article.
Identification of N-{cis-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases.
Vazquez ML, Kaila N, Strohbach JW, Trzupek JD, Brown MF, Flanagan ME, Mitton-Fry MJ, Johnson TA, TenBrink RE, Arnold EP, Basak A, Heasley SE, Kwon S, Langille J, Parikh MD, Griffin SH, Casavant JM, Duclos BA, Fenwick AE, Harris TM, Han S, Caspers N, Dowty ME, Yang X, Banker ME, Hegen M, Symanowicz PT, Li L, Wang L, Lin TH, Jussif J, Clark JD, Telliez JB, Robinson RP, Unwalla R. Vazquez ML, et al. J Med Chem. 2018 Feb 8;61(3):1130-1152. doi: 10.1021/acs.jmedchem.7b01598. Epub 2018 Jan 23. J Med Chem. 2018. PMID: 29298069
Macrocyclic Retinoic Acid Receptor-Related Orphan Receptor C2 Inverse Agonists.
Schnute ME, Trujillo JI, Lee KL, Unwalla R, Vajdos FF, Kauppi B, Nuhant P, Flick AC, Crouse KK, Zhao Y, Samuel A, Lombardo V, Taylor AP, Brault AL, Knafels JD, Vazquez ML, Berstein G. Schnute ME, et al. Among authors: vazquez ml. ACS Med Chem Lett. 2023 Jan 18;14(2):191-198. doi: 10.1021/acsmedchemlett.2c00500. eCollection 2023 Feb 9. ACS Med Chem Lett. 2023. PMID: 36793423 Free PMC article.
111 results