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Discovery of Fragment-Derived Small Molecules for in Vivo Inhibition of Ketohexokinase (KHK).
J Med Chem. 2017 Sep 28;60(18):7835-7849. doi: 10.1021/acs.jmedchem.7b00947. Epub 2017 Sep 11.
J Med Chem. 2017.
PMID: 28853885
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.
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
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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.
Sci Rep. 2015 Dec 1;5:17391. doi: 10.1038/srep17391.
Sci Rep. 2015.
PMID: 26620127
Free PMC article.
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The combination of exercise training and sodium-glucose cotransporter-2 inhibition improves glucose tolerance and exercise capacity in a rodent model of type 2 diabetes.
Linden MA, Ross TT, Beebe DA, Gorgoglione MF, Hamilton KL, Miller BF, Braun B, Esler WP.
Linden MA, et al. Among authors: gorgoglione mf.
Metabolism. 2019 Aug;97:68-80. doi: 10.1016/j.metabol.2019.05.009. Epub 2019 May 25.
Metabolism. 2019.
PMID: 31132381
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The hepatoselective glucokinase activator PF-04991532 ameliorates hyperglycemia without causing hepatic steatosis in diabetic rats.
Erion DM, Lapworth A, Amor PA, Bai G, Vera NB, Clark RW, Yan Q, Zhu Y, Ross TT, Purkal J, Gorgoglione M, Zhang G, Bonato V, Baker L, Barucci N, D'Aquila T, Robertson A, Aiello RJ, Yan J, Trimmer J, Rolph TP, Pfefferkorn JA.
Erion DM, et al.
PLoS One. 2014 May 23;9(5):e97139. doi: 10.1371/journal.pone.0097139. eCollection 2014.
PLoS One. 2014.
PMID: 24858947
Free PMC article.
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Human sebum requires de novo lipogenesis, which is increased in acne vulgaris and suppressed by acetyl-CoA carboxylase inhibition.
Esler WP, Tesz GJ, Hellerstein MK, Beysen C, Sivamani R, Turner SM, Watkins SM, Amor PA, Carvajal-Gonzalez S, Geoly FJ, Biddle KE, Purkal JJ, Fitch M, Buckeridge C, Silvia AM, Griffith DA, Gorgoglione M, Hassoun L, Bosanac SS, Vera NB, Rolph TP, Pfefferkorn JA, Sonnenberg GE.
Esler WP, et al.
Sci Transl Med. 2019 May 15;11(492):eaau8465. doi: 10.1126/scitranslmed.aau8465.
Sci Transl Med. 2019.
PMID: 31092695
Clinical Trial.
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Determination of Unbound Partition Coefficient and in Vitro-in Vivo Extrapolation for SLC13A Transporter-Mediated Uptake.
Riccardi K, Li Z, Brown JA, Gorgoglione MF, Niosi M, Gosset J, Huard K, Erion DM, Di L.
Riccardi K, et al. Among authors: gorgoglione mf.
Drug Metab Dispos. 2016 Oct;44(10):1633-42. doi: 10.1124/dmd.116.071837. Epub 2016 Jul 14.
Drug Metab Dispos. 2016.
PMID: 27417179
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Depot-specific differences and insufficient subcutaneous adipose tissue angiogenesis in human obesity.
Gealekman O, Guseva N, Hartigan C, Apotheker S, Gorgoglione M, Gurav K, Tran KV, Straubhaar J, Nicoloro S, Czech MP, Thompson M, Perugini RA, Corvera S.
Gealekman O, et al.
Circulation. 2011 Jan 18;123(2):186-94. doi: 10.1161/CIRCULATIONAHA.110.970145. Epub 2011 Jan 3.
Circulation. 2011.
PMID: 21200001
Free PMC article.
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