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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. Medchemcomm. 2016 Nov 22;8(4):771-779. doi: 10.1039/c6md00564k. eCollection 2017 Apr 1. Medchemcomm. 2016. PMID: 30108796 Free PMC article.
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. 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
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: futatsugi k. 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.
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. 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: futatsugi k. Sci Rep. 2015 Dec 1;5:17391. doi: 10.1038/srep17391. Sci Rep. 2015. PMID: 26620127 Free PMC article.
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: futatsugi k. 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
Identification of Morpholino-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-ones as Nonsteroidal Mineralocorticoid Antagonists.
Piotrowski DW, Futatsugi K, Casimiro-Garcia A, Wei L, Sammons MF, Herr M, Jiao W, Lavergne SY, Coffey SB, Wright SW, Song K, Loria PM, Banker ME, Petersen DN, Bauman J. Piotrowski DW, et al. Among authors: futatsugi k. J Med Chem. 2018 Feb 8;61(3):1086-1097. doi: 10.1021/acs.jmedchem.7b01515. Epub 2018 Jan 23. J Med Chem. 2018. PMID: 29300474
Discovery of PF-06835919: A Potent Inhibitor of Ketohexokinase (KHK) for the Treatment of Metabolic Disorders Driven by the Overconsumption of Fructose.
Futatsugi K, Smith AC, Tu M, Raymer B, Ahn K, Coffey SB, Dowling MS, Fernando DP, Gutierrez JA, Huard K, Jasti J, Kalgutkar AS, Knafels JD, Pandit J, Parris KD, Perez S, Pfefferkorn JA, Price DA, Ryder T, Shavnya A, Stock IA, Tsai AS, Tesz GJ, Thuma BA, Weng Y, Wisniewska HM, Xing G, Zhou J, Magee TV. Futatsugi K, et al. J Med Chem. 2020 Nov 25;63(22):13546-13560. doi: 10.1021/acs.jmedchem.0c00944. Epub 2020 Sep 27. J Med Chem. 2020. PMID: 32910646
39 results