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Page 1
Discovery of the Potent and Selective MC4R Antagonist PF-07258669 for the Potential Treatment of Appetite Loss.
Garnsey MR, Smith AC, Polivkova J, Arons AL, Bai G, Blakemore C, Boehm M, Buzon LM, Campion SN, Cerny M, Chang SC, Coffman K, Farley KA, Fonseca KR, Ford KK, Garren J, Kong JX, Koos MRM, Kung DW, Lian Y, Li MM, Li Q, Martinez-Alsina LA, O'Connor R, Ogilvie K, Omoto K, Raymer B, Reese MR, Ryder T, Samp L, Stevens KA, Widlicka DW, Yang Q, Zhu K, Fortin JP, Sammons MF. Garnsey MR, et al. Among authors: polivkova j. J Med Chem. 2023 Mar 9;66(5):3195-3211. doi: 10.1021/acs.jmedchem.2c02012. Epub 2023 Feb 19. J Med Chem. 2023. PMID: 36802610
Discovery of new piperidine amide triazolobenzodiazepinones as intestinal-selective CCK1 receptor agonists.
Cameron KO, Beretta EE, Chen Y, Chu-Moyer M, Fernando D, Gao H, Kohrt J, Lavergne S, Jardine Pda S, Guzman-Perez A, Hoth C, Perry DA, Hadcock JR, Gautreau D, Makowski M, Perez S, Polivkova J, Rogers L, Scott DO, Swick AG, Thiede L, Trebino CE, Trilles RV, Wilmowski J, Zhang Y. Cameron KO, et al. Among authors: polivkova j. Bioorg Med Chem Lett. 2012 Apr 15;22(8):2943-7. doi: 10.1016/j.bmcl.2012.02.049. Epub 2012 Feb 23. Bioorg Med Chem Lett. 2012. PMID: 22424974
Identification of potent, selective, CNS-targeted inverse agonists of the ghrelin receptor.
McClure KF, Jackson M, Cameron KO, Kung DW, Perry DA, Orr ST, Zhang Y, Kohrt J, Tu M, Gao H, Fernando D, Jones R, Erasga N, Wang G, Polivkova J, Jiao W, Swartz R, Ueno H, Bhattacharya SK, Stock IA, Varma S, Bagdasarian V, Perez S, Kelly-Sullivan D, Wang R, Kong J, Cornelius P, Michael L, Lee E, Janssen A, Steyn SJ, Lapham K, Goosen T. McClure KF, et al. Among authors: polivkova j. Bioorg Med Chem Lett. 2013 Oct 1;23(19):5410-4. doi: 10.1016/j.bmcl.2013.07.044. Epub 2013 Jul 30. Bioorg Med Chem Lett. 2013. PMID: 23953189
Spirolactam-based acetyl-CoA carboxylase inhibitors: toward improved metabolic stability of a chromanone lead structure.
Griffith DA, Dow RL, Huard K, Edmonds DJ, Bagley SW, Polivkova J, Zeng D, Garcia-Irizarry CN, Southers JA, Esler W, Amor P, Loomis K, McPherson K, Bahnck KB, Préville C, Banks T, Moore DE, Mathiowetz AM, Menhaji-Klotz E, Smith AC, Doran SD, Beebe DA, Dunn MF. Griffith DA, et al. Among authors: polivkova j. J Med Chem. 2013 Sep 12;56(17):7110-9. doi: 10.1021/jm401033t. Epub 2013 Aug 27. J Med Chem. 2013. PMID: 23981033
Discovery of Selective Small Molecule Inhibitors of Monoacylglycerol Acyltransferase 3.
Huard K, Londregan AT, Tesz G, Bahnck KB, Magee TV, Hepworth D, Polivkova J, Coffey SB, Pabst BA, Gosset JR, Nigam A, Kou K, Sun H, Lee K, Herr M, Boehm M, Carpino PA, Goodwin B, Perreault C, Li Q, Jorgensen CC, Tkalcevic GT, Subashi TA, Ahn K. Huard K, et al. Among authors: polivkova j. J Med Chem. 2015 Sep 24;58(18):7164-72. doi: 10.1021/acs.jmedchem.5b01008. Epub 2015 Sep 8. J Med Chem. 2015. PMID: 26258602
Optimization of a Dicarboxylic Series for in Vivo Inhibition of Citrate Transport by the Solute Carrier 13 (SLC13) Family.
Huard K, Gosset JR, Montgomery JI, Gilbert A, Hayward MM, Magee TV, Cabral S, Uccello DP, Bahnck K, Brown J, Purkal J, Gorgoglione M, Lanba A, Futatsugi K, Herr M, Genung NE, Aspnes G, Polivkova J, Garcia-Irizarry CN, Li Q, Canterbury D, Niosi M, Vera NB, Li Z, Khunte B, Siderewicz J, Rolph T, Erion DM. Huard K, et al. Among authors: polivkova j. J Med Chem. 2016 Feb 11;59(3):1165-75. doi: 10.1021/acs.jmedchem.5b01752. Epub 2016 Jan 27. J Med Chem. 2016. PMID: 26734723
Optimization of Metabolic and Renal Clearance in a Series of Indole Acid Direct Activators of 5'-Adenosine Monophosphate-Activated Protein Kinase (AMPK).
Edmonds DJ, Kung DW, Kalgutkar AS, Filipski KJ, Ebner DC, Cabral S, Smith AC, Aspnes GE, Bhattacharya SK, Borzilleri KA, Brown JA, Calabrese MF, Caspers NL, Cokorinos EC, Conn EL, Dowling MS, Eng H, Feng B, Fernando DP, Genung NE, Herr M, Kurumbail RG, Lavergne SY, Lee EC, Li Q, Mathialagan S, Miller RA, Panteleev J, Polivkova J, Rajamohan F, Reyes AR, Salatto CT, Shavnya A, Thuma BA, Tu M, Ward J, Withka JM, Xiao J, Cameron KO. Edmonds DJ, et al. Among authors: polivkova j. J Med Chem. 2018 Mar 22;61(6):2372-2383. doi: 10.1021/acs.jmedchem.7b01641. Epub 2018 Feb 28. J Med Chem. 2018. PMID: 29466005
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: polivkova j. 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
Discovery of Ervogastat (PF-06865571): A Potent and Selective Inhibitor of Diacylglycerol Acyltransferase 2 for the Treatment of Non-alcoholic Steatohepatitis.
Futatsugi K, Cabral S, Kung DW, Huard K, Lee E, Boehm M, Bauman J, Clark RW, Coffey SB, Crowley C, Dechert-Schmitt AM, Dowling MS, Dullea R, Gosset JR, Kalgutkar AS, Kou K, Li Q, Lian Y, Loria PM, Londregan AT, Niosi M, Orozco C, Pettersen JC, Pfefferkorn JA, Polivkova J, Ross TT, Sharma R, Stock IA, Tesz G, Wisniewska H, Goodwin B, Price DA. Futatsugi K, et al. Among authors: polivkova j. J Med Chem. 2022 Nov 24;65(22):15000-15013. doi: 10.1021/acs.jmedchem.2c01200. Epub 2022 Nov 2. J Med Chem. 2022. PMID: 36322383
38 results