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Nidufexor (LMB763), a Novel FXR Modulator for the Treatment of Nonalcoholic Steatohepatitis.
Chianelli D, Rucker PV, Roland J, Tully DC, Nelson J, Liu X, Bursulaya B, Hernandez ED, Wu J, Prashad M, Schlama T, Liu Y, Chu A, Schmeits J, Huang DJ, Hill R, Bao D, Zoll J, Kim Y, Groessl T, McNamara P, Liu B, Richmond W, Sancho-Martinez I, Phimister A, Seidel HM, Badman MK, Joseph SB, Laffitte B, Molteni V. Chianelli D, et al. Among authors: laffitte b. J Med Chem. 2020 Apr 23;63(8):3868-3880. doi: 10.1021/acs.jmedchem.9b01621. Epub 2020 Feb 5. J Med Chem. 2020. PMID: 31940200
Discovery of Tropifexor (LJN452), a Highly Potent Non-bile Acid FXR Agonist for the Treatment of Cholestatic Liver Diseases and Nonalcoholic Steatohepatitis (NASH).
Tully DC, Rucker PV, Chianelli D, Williams J, Vidal A, Alper PB, Mutnick D, Bursulaya B, Schmeits J, Wu X, Bao D, Zoll J, Kim Y, Groessl T, McNamara P, Seidel HM, Molteni V, Liu B, Phimister A, Joseph SB, Laffitte B. Tully DC, et al. Among authors: laffitte b. J Med Chem. 2017 Dec 28;60(24):9960-9973. doi: 10.1021/acs.jmedchem.7b00907. Epub 2017 Dec 8. J Med Chem. 2017. PMID: 29148806
Tropifexor-Mediated Abrogation of Steatohepatitis and Fibrosis Is Associated With the Antioxidative Gene Expression Profile in Rodents.
Hernandez ED, Zheng L, Kim Y, Fang B, Liu B, Valdez RA, Dietrich WF, Rucker PV, Chianelli D, Schmeits J, Bao D, Zoll J, Dubois C, Federe GC, Chen L, Joseph SB, Klickstein LB, Walker J, Molteni V, McNamara P, Meeusen S, Tully DC, Badman MK, Xu J, Laffitte B. Hernandez ED, et al. Among authors: laffitte b. Hepatol Commun. 2019 May 17;3(8):1085-1097. doi: 10.1002/hep4.1368. eCollection 2019 Aug. Hepatol Commun. 2019. PMID: 31388629 Free PMC article.
Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of the Novel Non-Bile Acid FXR Agonist Tropifexor (LJN452) in Healthy Volunteers.
Badman MK, Chen J, Desai S, Vaidya S, Neelakantham S, Zhang J, Gan L, Danis K, Laffitte B, Klickstein LB. Badman MK, et al. Among authors: laffitte b. Clin Pharmacol Drug Dev. 2020 Apr;9(3):395-410. doi: 10.1002/cpdd.762. Epub 2019 Dec 10. Clin Pharmacol Drug Dev. 2020. PMID: 31823525 Free PMC article. Clinical Trial.
Selective DYRK1A Inhibitor for the Treatment of Type 1 Diabetes: Discovery of 6-Azaindole Derivative GNF2133.
Liu YA, Jin Q, Zou Y, Ding Q, Yan S, Wang Z, Hao X, Nguyen B, Zhang X, Pan J, Mo T, Jacobsen K, Lam T, Wu TY, Petrassi HM, Bursulaya B, DiDonato M, Gordon WP, Liu B, Baaten J, Hill R, Nguyen-Tran V, Qiu M, Zhang YQ, Kamireddy A, Espinola S, Deaton L, Ha S, Harb G, Jia Y, Li J, Shen W, Schumacher AM, Colman K, Glynne R, Pan S, McNamara P, Laffitte B, Meeusen S, Molteni V, Loren J. Liu YA, et al. Among authors: laffitte b. J Med Chem. 2020 Mar 26;63(6):2958-2973. doi: 10.1021/acs.jmedchem.9b01624. Epub 2020 Feb 20. J Med Chem. 2020. PMID: 32077280
A Dual Inhibitor of DYRK1A and GSK3β for β-Cell Proliferation: Aminopyrazine Derivative GNF4877.
Liu YA, Jin Q, Ding Q, Hao X, Mo T, Yan S, Zou Y, Huang Z, Zhang X, Gao W, Wu TY, Li C, Bursalaya B, Di Donato M, Zhang YQ, Deaton L, Shen W, Taylor B, Kamireddy A, Harb G, Li J, Jia Y, Schumacher AM, Laffitte B, Glynne R, Pan S, McNamara P, Molteni V, Loren J. Liu YA, et al. Among authors: laffitte b. ChemMedChem. 2020 Aug 19;15(16):1562-1570. doi: 10.1002/cmdc.202000183. Epub 2020 Jul 2. ChemMedChem. 2020. PMID: 32613743
40 results