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Items: 6

1.

Targeting diacylglycerol acyltransferase 2 for the treatment of nonalcoholic steatohepatitis.

Amin NB, Carvajal-Gonzalez S, Purkal J, Zhu T, Crowley C, Perez S, Chidsey K, Kim AM, Goodwin B.

Sci Transl Med. 2019 Nov 27;11(520). pii: eaav9701. doi: 10.1126/scitranslmed.aav9701.

PMID:
31776293
2.

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.

Sci Transl Med. 2019 May 15;11(492). pii: eaau8465. doi: 10.1126/scitranslmed.aau8465.

PMID:
31092695
3.

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.

Medchemcomm. 2016 Nov 22;8(4):771-779. doi: 10.1039/c6md00564k. eCollection 2017 Apr 1.

4.

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.

J Med Chem. 2016 Feb 11;59(3):1165-75. doi: 10.1021/acs.jmedchem.5b01752. Epub 2016 Jan 27.

PMID:
26734723
5.

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.

J Med Chem. 2015 Sep 24;58(18):7173-85. doi: 10.1021/acs.jmedchem.5b01006.

PMID:
26349027
6.

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.

PLoS One. 2014 May 23;9(5):e97139. doi: 10.1371/journal.pone.0097139. eCollection 2014.

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