G-protein-coupled bile acid receptor 1 (GPBAR1, TGR5) agonists reduce the production of proinflammatory cytokines and stabilize the alternative macrophage phenotype

Journal of Medicinal Chemistry

Volumn 57, Issue 24, 2014, Pages 10343-10354

  Högenauer, Klemens ^a   Arista, Luca ^a   Schmiedeberg, Niko ^a   Werner, Gudrun ^a   Jaksche, Herbert ^a   Bouhelal, Rochdi ^a   Nguyen, Deborah G ^b,c   Bhat, B Ganesh ^b   Raad, Layla ^a   Rauld, Celine ^a   Carballido, José M ^a  

^a NOVARTIS PHARMA AG   (Switzerland)

^b GENOMICS INSTITUTE OF THE NOVARTIS RESEARCH FOUNDATION   (United States)

^c Organovo Inc   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

3 METHYL N PHENETHYL N PHENYLISONICOTINAMIDE; 4 FLUORO 2 METHYL N ((2 METHYL 1H INDOL 4 YL)METHYL)ANILINE; CYTOKINE; DEXAMETHASONE; G PROTEIN COUPLED BILE ACID RECEPTOR 1; G PROTEIN COUPLED RECEPTOR; GAMMA INTERFERON; INTERLEUKIN 10; INTERLEUKIN 12; INTERLEUKIN 1BETA; ISONICOTINAMIDE; LIPOPOLYSACCHARIDE; LITHIUM 3 METHYLPYRIDAZINE 4 CARBOXYLATE; N (2 METHOXYBENZYL) 2 (TRIFLUOROMETHOXY)ANILINE; N (2 METHOXYBENZYL) 3 METHYL N (2 (TRIFLUOROMETHOXY)PHENYL)ISONICOTINAMIDE; N (2 METHOXYBENZYL) 3 METHYL N PHENYLISONICOTINAMIDE; N (3,5 DICHLOROPHENYL) N (2 METHOXYBENZYL) 3 METHYLISONICOTINAMIDE; N (4 FLUORO 2 METHYLPHENYL) 3 METHYL N ((2 METHYL 1H INDOL 4 YL)METHYL)ISONICOTINAMIDE; N BENZYL 1,4 DIMETHYL N PHENYL 1H IMIDAZOLE 5 CARBOXAMIDE; N BENZYL 2 METHYL N PHENYLISONICOTINAMIDE; N BENZYL 3 METHYL N PHENYLISONICOTINAMIDE; N BENZYL 3 METHYL N PHENYLPYRIDAZINE 4 CARBOXAMIDE; N BENZYL 3,5 DIMETHYL N PHENYLISOXAZOLE 4 CARBOXAMIDE; N BENZYL 4 METHYL N PHENYLNICOTINAMIDE; N BENZYL N PHENYLISONICOTINAMIDE; N ISOBUTYL 3 METHYL N PHENYLISONICOTINAMIDE; N,N DIBENZYL 3 METHYLISONICOTINAMIDE; NONSTEROID ANTIINFLAMMATORY AGENT; TUMOR NECROSIS FACTOR ALPHA; UNCLASSIFIED DRUG; ANTIINFLAMMATORY AGENT; CALCIUM; CYCLIC AMP; GPBAR1 PROTEIN, MOUSE; INDOLE DERIVATIVE; N-(4-FLUORO-2-METHYLPHENYL)-3-METHYL-N-((2-METHYL-1H-INDOL-4-YL)METHYL)ISONICOTINAMIDE; NICOTINAMIDE;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANTIINFLAMMATORY ACTIVITY; AREA UNDER THE CURVE; ARTICLE; CELL DIFFERENTIATION; CONTROLLED STUDY; CYTOKINE PRODUCTION; CYTOKINE RELEASE; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG DEVELOPMENT; DRUG HALF LIFE; DRUG IDENTIFICATION; DRUG POTENCY; DRUG STRUCTURE; DRUG SYNTHESIS; EC50; HIGH THROUGHPUT SCREENING; HUMAN; HUMAN CELL; IMMUNOMODULATION; IN VITRO STUDY; IN VIVO STUDY; INFLAMMATION; KNOCKOUT MOUSE; LIPOPHILICITY; LIVER MICROSOME; MACROPHAGE; MALE; MAXIMUM PLASMA CONCENTRATION; MONOCYTE; MOUSE; NONHUMAN; PHENOTYPE; PROTEIN EXPRESSION; STRUCTURE ACTIVITY RELATION; TH1 CELL; TH17 CELL; TIME TO MAXIMUM PLASMA CONCENTRATION; TREATMENT RESPONSE; AGONISTS; ANALOGS AND DERIVATIVES; ANIMAL; C57BL MOUSE; CHEMISTRY; DRUG EFFECTS; ENZYME LINKED IMMUNOSORBENT ASSAY; IMMUNOLOGY; JURKAT CELL LINE; METABOLISM; PHYSIOLOGY;

ANIMALS; ANTI-INFLAMMATORY AGENTS; CALCIUM; CYCLIC AMP; ENZYME-LINKED IMMUNOSORBENT ASSAY; HUMANS; INDOLES; INFLAMMATION; INTERLEUKIN-10; INTERLEUKIN-12; JURKAT CELLS; LIPOPOLYSACCHARIDES; MACROPHAGES; MICE; MICE, INBRED C57BL; MICE, KNOCKOUT; MONOCYTES; NIACINAMIDE; RECEPTORS, G-PROTEIN-COUPLED; TUMOR NECROSIS FACTOR-ALPHA;

EID: 84920109139     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm501052c     Document Type: Article

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