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Page 1
Maximizing lipophilic efficiency: the use of Free-Wilson analysis in the design of inhibitors of acetyl-CoA carboxylase.
Freeman-Cook KD, Amor P, Bader S, Buzon LM, Coffey SB, Corbett JW, Dirico KJ, Doran SD, Elliott RL, Esler W, Guzman-Perez A, Henegar KE, Houser JA, Jones CS, Limberakis C, Loomis K, McPherson K, Murdande S, Nelson KL, Phillion D, Pierce BS, Song W, Sugarman E, Tapley S, Tu M, Zhao Z. Freeman-Cook KD, et al. Among authors: esler w. J Med Chem. 2012 Jan 26;55(2):935-42. doi: 10.1021/jm201503u. Epub 2012 Jan 11. J Med Chem. 2012. PMID: 22148323
Discovery of small molecule isozyme non-specific inhibitors of mammalian acetyl-CoA carboxylase 1 and 2.
Corbett JW, Freeman-Cook KD, Elliott R, Vajdos F, Rajamohan F, Kohls D, Marr E, Zhang H, Tong L, Tu M, Murdande S, Doran SD, Houser JA, Song W, Jones CJ, Coffey SB, Buzon L, Minich ML, Dirico KJ, Tapley S, McPherson RK, Sugarman E, Harwood HJ Jr, Esler W. Corbett JW, et al. Among authors: esler w. Bioorg Med Chem Lett. 2010 Apr 1;20(7):2383-8. doi: 10.1016/j.bmcl.2009.04.091. Epub 2009 Apr 24. Bioorg Med Chem Lett. 2010. PMID: 20219367
Discovery of triazolopyrimidine-based PDE8B inhibitors: exceptionally ligand-efficient and lipophilic ligand-efficient compounds for the treatment of diabetes.
DeNinno MP, Wright SW, Etienne JB, Olson TV, Rocke BN, Corbett JW, Kung DW, DiRico KJ, Andrews KM, Millham ML, Parker JC, Esler W, van Volkenburg M, Boyer DD, Houseknecht KL, Doran SD. DeNinno MP, et al. Among authors: esler w. Bioorg Med Chem Lett. 2012 Sep 1;22(17):5721-6. doi: 10.1016/j.bmcl.2012.06.079. Epub 2012 Jul 6. Bioorg Med Chem Lett. 2012. PMID: 22858141
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: esler w. J Med Chem. 2013 Sep 12;56(17):7110-9. doi: 10.1021/jm401033t. Epub 2013 Aug 27. J Med Chem. 2013. PMID: 23981033
Decreasing the rate of metabolic ketone reduction in the discovery of a clinical acetyl-CoA carboxylase inhibitor for the treatment of diabetes.
Griffith DA, Kung DW, Esler WP, Amor PA, Bagley SW, Beysen C, Carvajal-Gonzalez S, Doran SD, Limberakis C, Mathiowetz AM, McPherson K, Price DA, Ravussin E, Sonnenberg GE, Southers JA, Sweet LJ, Turner SM, Vajdos FF. Griffith DA, et al. Among authors: esler wp. J Med Chem. 2014 Dec 26;57(24):10512-26. doi: 10.1021/jm5016022. Epub 2014 Dec 11. J Med Chem. 2014. PMID: 25423286 Free PMC article. Clinical Trial.
Discovery of spirocyclic-diamine inhibitors of mammalian acetyl CoA-carboxylase.
Kung DW, Griffith DA, Esler WP, Vajdos FF, Mathiowetz AM, Doran SD, Amor PA, Bagley SW, Banks T, Cabral S, Ford K, Garcia-Irizarry CN, Landis MS, Loomis K, McPherson K, Niosi M, Rockwell KL, Rose C, Smith AC, Southers JA, Tapley S, Tu M, Valentine JJ. Kung DW, et al. Among authors: esler wp. Bioorg Med Chem Lett. 2015 Nov 15;25(22):5352-6. doi: 10.1016/j.bmcl.2015.09.035. Epub 2015 Sep 15. Bioorg Med Chem Lett. 2015. PMID: 26411795
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.
Acetyl-CoA Carboxylase Inhibition Improves Multiple Dimensions of NASH Pathogenesis in Model Systems.
Ross TT, Crowley C, Kelly KL, Rinaldi A, Beebe DA, Lech MP, Martinez RV, Carvajal-Gonzalez S, Boucher M, Hirenallur-Shanthappa D, Morin J, Opsahl AC, Vargas SR, Bence KK, Pfefferkorn JA, Esler WP. Ross TT, et al. Among authors: esler wp. Cell Mol Gastroenterol Hepatol. 2020;10(4):829-851. doi: 10.1016/j.jcmgh.2020.06.001. Epub 2020 Jun 9. Cell Mol Gastroenterol Hepatol. 2020. PMID: 32526482 Free PMC article.
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: esler wp. 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
De novo lipogenesis is essential for platelet production in humans.
Kelly KL, Reagan WJ, Sonnenberg GE, Clasquin M, Hales K, Asano S, Amor PA, Carvajal-Gonzalez S, Shirai N, Matthews MD, Li KW, Hellerstein MK, Vera NB, Ross TT, Cappon G, Bergman A, Buckeridge C, Sun Z, Qejvanaj EZ, Schmahai T, Beebe D, Pfefferkorn JA, Esler WP. Kelly KL, et al. Among authors: esler wp. Nat Metab. 2020 Oct;2(10):1163-1178. doi: 10.1038/s42255-020-00272-9. Epub 2020 Sep 14. Nat Metab. 2020. PMID: 32929234 Clinical Trial.
53 results