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Potent DGAT1 Inhibitors in the Benzimidazole Class with a Pyridyl-oxy-cyclohexanecarboxylic Acid Moiety.
He S, Hong Q, Lai Z, Wu Z, Yu Y, Kim DW, Ting PC, Kuethe JT, Yang GX, Jian T, Liu J, Guiadeen D, Krikorian AD, Sperbeck DM, Sonatore LM, Wiltsie J, Chung CC, Gibson JT, Lisnock J, Murphy BA, Gorski JN, Liu J, Chen D, Chen X, Wolff M, Tong SX, Madeira M, Karanam BV, Shen DM, Balkovec JM, Pinto S, Nargund RP, DeVita RJ. He S, et al. Among authors: murphy ba. ACS Med Chem Lett. 2013 Jun 6;4(8):773-8. doi: 10.1021/ml400168h. eCollection 2013 Aug 8. ACS Med Chem Lett. 2013. PMID: 24900745 Free PMC article.
Microscale High-Throughput Experimentation as an Enabling Technology in Drug Discovery: Application in the Discovery of (Piperidinyl)pyridinyl-1H-benzimidazole Diacylglycerol Acyltransferase 1 Inhibitors.
Cernak T, Gesmundo NJ, Dykstra K, Yu Y, Wu Z, Shi ZC, Vachal P, Sperbeck D, He S, Murphy BA, Sonatore L, Williams S, Madeira M, Verras A, Reiter M, Lee CH, Cuff J, Sherer EC, Kuethe J, Goble S, Perrotto N, Pinto S, Shen DM, Nargund R, Balkovec J, DeVita RJ, Dreher SD. Cernak T, et al. Among authors: murphy ba. J Med Chem. 2017 May 11;60(9):3594-3605. doi: 10.1021/acs.jmedchem.6b01543. Epub 2017 Mar 2. J Med Chem. 2017. PMID: 28252959
Benzimidazole-based DGAT1 inhibitors with a [3.1.0] bicyclohexane carboxylic acid moiety.
He S, Lai Z, Hong Q, Shang J, Reibarkh M, Kuethe JT, Liu J, Guiadeen D, Krikorian AD, Cernak TA, Dykstra KD, Sperbeck DM, Wu Z, Yu Y, Yang GX, Jian T, Verras A, Sonatore LM, Wiltsie J, Chung CC, Murphy BA, Gorski JN, Liu J, Xiao J, Wolff M, Tong SX, Madeira M, Karanam BV, Shen DM, Balkovec JM, Pinto S, Nargund RP, DeVita RJ. He S, et al. Among authors: murphy ba. Bioorg Med Chem Lett. 2019 May 15;29(10):1182-1186. doi: 10.1016/j.bmcl.2019.03.025. Epub 2019 Mar 21. Bioorg Med Chem Lett. 2019. PMID: 30926247
Accelerating the discovery of DGAT1 inhibitors through the application of parallel medicinal chemistry (PMC).
Yu Y, Wu Z, Shi ZC, He S, Lai Z, Cernak TA, Vachal P, Liu M, Liu J, Hong Q, Jian T, Guiadeen D, Krikorian A, Sperbeck DM, Verras A, Sonatore LM, Murphy BA, Wiltsie J, Chung CC, Gorski JN, Liu J, Xiao J, Wolff M, Tong SX, Madeira M, Karanam BV, Shen DM, Balkovec JM, De Vita RJ, Pinto S, Nargund RP. Yu Y, et al. Among authors: murphy ba. Bioorg Med Chem Lett. 2019 Jun 1;29(11):1380-1385. doi: 10.1016/j.bmcl.2019.03.039. Epub 2019 Mar 27. Bioorg Med Chem Lett. 2019. PMID: 30952592
Discovery of benzodihydroisofurans as novel, potent, bioavailable and brain-penetrant prolylcarboxypeptidase inhibitors.
Shen HC, Ding FX, Jiang J, Verras A, Chabin RM, Xu S, Tong X, Chen Q, Xie D, Lassman ME, Bhatt UR, Garcia-Calvo MM, Geissler W, Shen Z, Murphy BA, Gorski JN, Wiltsie J, SinhaRoy R, Hale JJ, Pinto S, Shen DM. Shen HC, et al. Among authors: murphy ba. Bioorg Med Chem Lett. 2012 Feb 15;22(4):1550-6. doi: 10.1016/j.bmcl.2012.01.002. Epub 2012 Jan 10. Bioorg Med Chem Lett. 2012. PMID: 22264488
Potential mechanism of enhanced postprandial glucagon-like peptide-1 release following treatment with a diacylglycerol acyltransferase 1 inhibitor.
Liu J, McLaren DG, Chen D, Kan Y, Stout SJ, Shen X, Murphy BA, Forrest G, Karanam B, Sonatore L, He S, Roddy TP, Pinto S. Liu J, et al. Among authors: murphy ba. Pharmacol Res Perspect. 2015 Nov 30;3(6):e00193. doi: 10.1002/prp2.193. eCollection 2015 Dec. Pharmacol Res Perspect. 2015. PMID: 27022467 Free PMC article.
Discovery and Pharmacology of a Novel Class of Diacylglycerol Acyltransferase 2 Inhibitors.
Imbriglio JE, Shen DM, Liang R, Marby K, You M, Youm HW, Feng Z, London C, Xiong Y, Tata J, Verras A, Garcia-Calvo M, Song X, Addona GH, McLaren DG, He T, Murphy B, Metzger DE, Salituro G, Deckman D, Chen Q, Jin X, Stout SJ, Wang SP, Wilsie L, Palyha O, Han S, Hubbard BK, Previs SF, Pinto S, Taggart A. Imbriglio JE, et al. J Med Chem. 2015 Dec 10;58(23):9345-53. doi: 10.1021/acs.jmedchem.5b01345. Epub 2015 Nov 20. J Med Chem. 2015. PMID: 26561979
A Series of Novel, Highly Potent, and Orally Bioavailable Next-Generation Tricyclic Peptide PCSK9 Inhibitors.
Tucker TJ, Embrey MW, Alleyne C, Amin RP, Bass A, Bhatt B, Bianchi E, Branca D, Bueters T, Buist N, Ha SN, Hafey M, He H, Higgins J, Johns DG, Kerekes AD, Koeplinger KA, Kuethe JT, Li N, Murphy B, Orth P, Salowe S, Shahripour A, Tracy R, Wang W, Wu C, Xiong Y, Zokian HJ, Wood HB, Walji A. Tucker TJ, et al. J Med Chem. 2021 Nov 25;64(22):16770-16800. doi: 10.1021/acs.jmedchem.1c01599. Epub 2021 Oct 27. J Med Chem. 2021. PMID: 34704436
DGAT2 Inhibition Alters Aspects of Triglyceride Metabolism in Rodents but Not in Non-human Primates.
McLaren DG, Han S, Murphy BA, Wilsie L, Stout SJ, Zhou H, Roddy TP, Gorski JN, Metzger DE, Shin MK, Reilly DF, Zhou HH, Tadin-Strapps M, Bartz SR, Cumiskey AM, Graham TH, Shen DM, Akinsanya KO, Previs SF, Imbriglio JE, Pinto S. McLaren DG, et al. Among authors: murphy ba. Cell Metab. 2018 Jun 5;27(6):1236-1248.e6. doi: 10.1016/j.cmet.2018.04.004. Epub 2018 Apr 26. Cell Metab. 2018. PMID: 29706567 Free article.
307 results