SAR studies on FXR modulators led to the discovery of the first combined FXR antagonistic/TGR5 agonistic compound

Future Medicinal Chemistry

Volumn 8, Issue 2, 2016, Pages 133-148

  Lamers, Christina ^a   Merk, Daniel ^a   Gabler, Matthias ^a   Flesch, Daniel ^a   Kaiser, Astrid ^a   Schubert Zsilavecz, Manfred ^a  

^a GOETHE UNIVERSITY   (Germany)

Author keywords

bile acid receptor modulator; bile acid signaling; farnesoid X receptor; FXR antagonist; metabolic disorders; non alcoholic steatohepatitis

Indexed keywords

3 [2 [2 CHLORO 4 [3 (2,6 DICHLOROPHENYL) 5 ISOPROPYL 4 ISOXAZOLYLMETHOXY]PHENYL]VINYL]BENZOIC ACID; AGENTS INTERACTING WITH TRANSMITTER, HORMONE OR DRUG RECEPTORS; BENZOIC ACID DERIVATIVE; BIPHENYL DERIVATIVE; CARBOXYLIC ACID DERIVATIVE; ESTER DERIVATIVE; FARNESOID X RECEPTOR; FARNESOID X RECEPTOR ANTAGONIST; G PROTEIN COUPLED RECEPTOR; G PROTEIN COUPLED RECEPTOR TGR5 AGONIST; HORMONE RECEPTOR BLOCKING AGENT; PIRINIXIC ACID; PYRIDINOL; PYRIDONE DERIVATIVE; UNCLASSIFIED DRUG; BENZOIC ACID; BILE ACID; CELL RECEPTOR; FARNESOID X-ACTIVATED RECEPTOR; GPBAR1 PROTEIN, HUMAN; PROTEIN BINDING;

ACUTE TOXICITY; ANIMAL CELL; ARTICLE; COLORECTAL CARCINOMA; CONTROLLED STUDY; DRUG POTENCY; DRUG SCREENING; DRUG STRUCTURE; DRUG SYNTHESIS; EC50; HELA CELL LINE; HEPG2 CELL LINE; HUMAN; HUMAN CELL; IC50; IN VITRO STUDY; LIVER CELL CARCINOMA; LIVER MICROSOME; METABOLIC STABILITY; MITSUNOBU REACTION; NONHUMAN; PRIORITY JOURNAL; RAT; STRUCTURE ACTIVITY RELATION; STRUCTURE ANALYSIS; TRANSACTIVATION; AGONISTS; ANTAGONISTS AND INHIBITORS; CHEMISTRY; DRUG EFFECTS; METABOLISM; TRANSCRIPTION INITIATION; TUMOR CELL LINE;

BENZOIC ACID; BILE ACIDS AND SALTS; CELL LINE, TUMOR; HELA CELLS; HUMANS; PROTEIN BINDING; RECEPTORS, CYTOPLASMIC AND NUCLEAR; RECEPTORS, G-PROTEIN-COUPLED; STRUCTURE-ACTIVITY RELATIONSHIP; TRANSCRIPTIONAL ACTIVATION;

EID: 84958051915     PISSN: 17568919     EISSN: 17568927     Source Type: Journal    
DOI: 10.4155/fmc.15.178     Document Type: Article

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