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266 results

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Page 1
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: herr m. 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
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: herr m. 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
Discovery and Optimization of Imidazopyridine-Based Inhibitors of Diacylglycerol Acyltransferase 2 (DGAT2).
Futatsugi K, Kung DW, Orr ST, Cabral S, Hepworth D, Aspnes G, Bader S, Bian J, Boehm M, Carpino PA, Coffey SB, Dowling MS, Herr M, Jiao W, Lavergne SY, Li Q, Clark RW, Erion DM, Kou K, Lee K, Pabst BA, Perez SM, Purkal J, Jorgensen CC, Goosen TC, Gosset JR, Niosi M, Pettersen JC, Pfefferkorn JA, Ahn K, Goodwin B. Futatsugi K, et al. Among authors: herr m. J Med Chem. 2015 Sep 24;58(18):7173-85. doi: 10.1021/acs.jmedchem.5b01006. J Med Chem. 2015. PMID: 26349027
Discovery and characterization of novel inhibitors of the sodium-coupled citrate transporter (NaCT or SLC13A5).
Huard K, Brown J, Jones JC, Cabral S, Futatsugi K, Gorgoglione M, Lanba A, Vera NB, Zhu Y, Yan Q, Zhou Y, Vernochet C, Riccardi K, Wolford A, Pirman D, Niosi M, Aspnes G, Herr M, Genung NE, Magee TV, Uccello DP, Loria P, Di L, Gosset JR, Hepworth D, Rolph T, Pfefferkorn JA, Erion DM. Huard K, et al. Among authors: herr m. Sci Rep. 2015 Dec 1;5:17391. doi: 10.1038/srep17391. Sci Rep. 2015. PMID: 26620127 Free PMC article.
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: herr m. 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
Small structural changes of the imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitors produce an improved safety profile.
Futatsugi K, Huard K, Kung DW, Pettersen JC, Flynn DA, Gosset JR, Aspnes GE, Barnes RJ, Cabral S, Dowling MS, Fernando DP, Goosen TC, Gorczyca WP, Hepworth D, Herr M, Lavergne S, Li Q, Niosi M, Orr STM, Pardo ID, Perez SM, Purkal J, Schmahai TJ, Shirai N, Shoieb AM, Zhou J, Goodwin B. Futatsugi K, et al. Among authors: herr m. Medchemcomm. 2016 Nov 22;8(4):771-779. doi: 10.1039/c6md00564k. eCollection 2017 Apr 1. Medchemcomm. 2016. PMID: 30108796 Free PMC article.
Identification of Tetrahydropyrido[4,3-d]pyrimidine Amides as a New Class of Orally Bioavailable TGR5 Agonists.
Piotrowski DW, Futatsugi K, Warmus JS, Orr ST, Freeman-Cook KD, Londregan AT, Wei L, Jennings SM, Herr M, Coffey SB, Jiao W, Storer G, Hepworth D, Wang J, Lavergne SY, Chin JE, Hadcock JR, Brenner MB, Wolford AC, Janssen AM, Roush NS, Buxton J, Hinchey T, Kalgutkar AS, Sharma R, Flynn DA. Piotrowski DW, et al. Among authors: herr m. ACS Med Chem Lett. 2012 Nov 9;4(1):63-8. doi: 10.1021/ml300277t. eCollection 2013 Jan 10. ACS Med Chem Lett. 2012. PMID: 24900564 Free PMC article.
The discovery of novel calcium sensing receptor negative allosteric modulators.
Balan G, Bauman J, Bhattacharya S, Castrodad M, Healy DR, Herr M, Humphries P, Jennings S, Kalgutkar AS, Kapinos B, Khot V, Lazarra K, Li M, Li Y, Neagu C, Oliver R, Piotrowski DW, Price D, Qi H, Simmons HA, Southers J, Wei L, Zhang Y, Paralkar VM. Balan G, et al. Among authors: herr m. Bioorg Med Chem Lett. 2009 Jun 15;19(12):3328-32. doi: 10.1016/j.bmcl.2009.04.044. Epub 2009 Apr 18. Bioorg Med Chem Lett. 2009. PMID: 19442519
266 results