Mechanism of action of a nanomolar potent, allosteric antagonist of the thyroid-stimulating hormone receptor

British Journal of Pharmacology

Volumn 165, Issue 7, 2012, Pages 2314-2324

  Van Koppen, Chris J ^a   De Gooyer, Marcel E ^a   Karstens, Willem Jan ^a   Plate, Ralf ^a   Conti, Paolo G M ^a   Van Achterberg, Tanja A E ^a   Van Amstel, Monique G A ^a   Brands, Jolanda H G M ^a   Wat, Jesse ^a   Berg, Rob J W ^a   Lane, J Robert D ^b   Miltenburg, Andre M M ^a   Timmers, C Marco ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

^b MONASH UNIVERSITY   (Australia)

Author keywords

allosterism; antagonism; G protein coupled receptor; Graves' disease; Graves' ophthalmopathy; thyroid; TSH

Indexed keywords

ADENYLATE CYCLASE; FOLLITROPIN; HORMONE RECEPTOR BLOCKING AGENT; LUTEINIZING HORMONE RECEPTOR; ORG 274178 0; ORG 274179 0; THYROID STIMULATING HORMONE RECEPTOR ANTAGONIST; THYROTROPIN RECEPTOR; UNCLASSIFIED DRUG;

ALLOSTERISM; ANIMAL CELL; ARTICLE; CONTROLLED STUDY; CROSS REACTION; DRUG EFFICACY; DRUG MECHANISM; DRUG POTENCY; DRUG STRUCTURE; ENDOCRINE OPHTHALMOPATHY; GRAVES DISEASE; HUMAN; IC 50; NONHUMAN; PRIORITY JOURNAL; SIGNAL TRANSDUCTION;

ADENYLATE CYCLASE; AMINOQUINOLINES; ANIMALS; CHO CELLS; CRICETINAE; CRICETULUS; DRUG EVALUATION, PRECLINICAL; GRAVES DISEASE; HUMANS; MOLECULAR WEIGHT; MUTAGENESIS, SITE-DIRECTED; RATS; RECEPTORS, THYROTROPIN; RECOMBINANT PROTEINS; SIGNAL TRANSDUCTION; THYROTROPIN;

EID: 84858170565     PISSN: 00071188     EISSN: 14765381     Source Type: Journal    
DOI: 10.1111/j.1476-5381.2011.01709.x     Document Type: Article

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