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Page 1
Activation of the G-protein-coupled receptor 119: a conformation-based hypothesis for understanding agonist response.
McClure KF, Darout E, Guimarães CR, DeNinno MP, Mascitti V, Munchhof MJ, Robinson RP, Kohrt J, Harris AR, Moore DE, Li B, Samp L, Lefker BA, Futatsugi K, Kung D, Bonin PD, Cornelius P, Wang R, Salter E, Hornby S, Kalgutkar AS, Chen Y. McClure KF, et al. Among authors: mascitti v. J Med Chem. 2011 Mar 24;54(6):1948-52. doi: 10.1021/jm200003p. Epub 2011 Mar 1. J Med Chem. 2011. PMID: 21361292
Design and evaluation of a 2-(2,3,6-trifluorophenyl)acetamide derivative as an agonist of the GPR119 receptor.
Mascitti V, Stevens BD, Choi C, McClure KF, Guimarães CR, Farley KA, Munchhof MJ, Robinson RP, Futatsugi K, Lavergne SY, Lefker BA, Cornelius P, Bonin PD, Kalgutkar AS, Sharma R, Chen Y. Mascitti V, et al. Bioorg Med Chem Lett. 2011 Mar 1;21(5):1306-9. doi: 10.1016/j.bmcl.2011.01.088. Epub 2011 Jan 25. Bioorg Med Chem Lett. 2011. PMID: 21310611
From partial to full agonism: identification of a novel 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole as a full agonist of the human GPR119 receptor.
Futatsugi K, Mascitti V, Guimarães CR, Morishita N, Cai C, DeNinno MP, Gao H, Hamilton MD, Hank R, Harris AR, Kung DW, Lavergne SY, Lefker BA, Lopaze MG, McClure KF, Munchhof MJ, Preville C, Robinson RP, Wright SW, Bonin PD, Cornelius P, Chen Y, Kalgutkar AS. Futatsugi K, et al. Among authors: mascitti v. Bioorg Med Chem Lett. 2013 Jan 1;23(1):194-7. doi: 10.1016/j.bmcl.2012.10.119. Epub 2012 Nov 5. Bioorg Med Chem Lett. 2013. PMID: 23177788
Design and synthesis of diazatricyclodecane agonists of the G-protein-coupled receptor 119.
Darout E, Robinson RP, McClure KF, Corbett M, Li B, Shavnya A, Andrews MP, Jones CS, Li Q, Minich ML, Mascitti V, Guimarães CR, Munchhof MJ, Bahnck KB, Cai C, Price DA, Liras S, Bonin PD, Cornelius P, Wang R, Bagdasarian V, Sobota CP, Hornby S, Masterson VM, Joseph RM, Kalgutkar AS, Chen Y. Darout E, et al. Among authors: mascitti v. J Med Chem. 2013 Jan 10;56(1):301-19. doi: 10.1021/jm301626p. Epub 2012 Dec 31. J Med Chem. 2013. PMID: 23234271
Intrinsic electrophilicity of a 4-substituted-5-cyano-6-(2-methylpyridin-3-yloxy)pyrimidine derivative: structural characterization of glutathione conjugates in vitro.
Kalgutkar AS, Mascitti V, Sharma R, Walker GW, Ryder T, McDonald TS, Chen Y, Preville C, Basak A, McClure KF, Kohrt JT, Robinson RP, Munchhof MJ, Cornelius P. Kalgutkar AS, et al. Among authors: mascitti v. Chem Res Toxicol. 2011 Feb 18;24(2):269-78. doi: 10.1021/tx100429x. Epub 2011 Feb 3. Chem Res Toxicol. 2011. PMID: 21288051
Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors.
Mascitti V, Maurer TS, Robinson RP, Bian J, Boustany-Kari CM, Brandt T, Collman BM, Kalgutkar AS, Klenotic MK, Leininger MT, Lowe A, Maguire RJ, Masterson VM, Miao Z, Mukaiyama E, Patel JD, Pettersen JC, Préville C, Samas B, She L, Sobol Z, Steppan CM, Stevens BD, Thuma BA, Tugnait M, Zeng D, Zhu T. Mascitti V, et al. J Med Chem. 2011 Apr 28;54(8):2952-60. doi: 10.1021/jm200049r. Epub 2011 Mar 30. J Med Chem. 2011. PMID: 21449606
Optimizing the Benefit/Risk of Acetyl-CoA Carboxylase Inhibitors through Liver Targeting.
Huard K, Smith AC, Cappon G, Dow RL, Edmonds DJ, El-Kattan A, Esler WP, Fernando DP, Griffith DA, Kalgutkar AS, Ross TT, Bagley SW, Beebe D, Bi YA, Cabral S, Crowley C, Doran SD, Dowling MS, Liras S, Mascitti V, Niosi M, Pfefferkorn JA, Polivkova J, Préville C, Price DA, Shavnya A, Shirai N, Smith AH, Southers JR, Tess DA, Thuma BA, Varma MV, Yang X. Huard K, et al. Among authors: mascitti v. J Med Chem. 2020 Oct 8;63(19):10879-10896. doi: 10.1021/acs.jmedchem.0c00640. Epub 2020 Sep 18. J Med Chem. 2020. PMID: 32809824
C-Aryl glycoside inhibitors of SGLT2: Exploration of sugar modifications including C-5 spirocyclization.
Robinson RP, Mascitti V, Boustany-Kari CM, Carr CL, Foley PM, Kimoto E, Leininger MT, Lowe A, Klenotic MK, Macdonald JI, Maguire RJ, Masterson VM, Maurer TS, Miao Z, Patel JD, Préville C, Reese MR, She L, Steppan CM, Thuma BA, Zhu T. Robinson RP, et al. Among authors: mascitti v. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1569-72. doi: 10.1016/j.bmcl.2010.01.075. Epub 2010 Jan 21. Bioorg Med Chem Lett. 2010. PMID: 20149653
Preclinical species and human disposition of PF-04971729, a selective inhibitor of the sodium-dependent glucose cotransporter 2 and clinical candidate for the treatment of type 2 diabetes mellitus.
Kalgutkar AS, Tugnait M, Zhu T, Kimoto E, Miao Z, Mascitti V, Yang X, Tan B, Walsky RL, Chupka J, Feng B, Robinson RP. Kalgutkar AS, et al. Among authors: mascitti v. Drug Metab Dispos. 2011 Sep;39(9):1609-19. doi: 10.1124/dmd.111.040675. Epub 2011 Jun 20. Drug Metab Dispos. 2011. PMID: 21690265 Clinical Trial.
Pharmacodynamic model of sodium-glucose transporter 2 (SGLT2) inhibition: implications for quantitative translational pharmacology.
Maurer TS, Ghosh A, Haddish-Berhane N, Sawant-Basak A, Boustany-Kari CM, She L, Leininger MT, Zhu T, Tugnait M, Yang X, Kimoto E, Mascitti V, Robinson RP. Maurer TS, et al. Among authors: mascitti v. AAPS J. 2011 Dec;13(4):576-84. doi: 10.1208/s12248-011-9297-2. Epub 2011 Aug 26. AAPS J. 2011. PMID: 21870203 Free PMC article.
33 results