Article
Partial agonism, neutral antagonism, and inverse agonism at the human wild-type and constitutively active cholecystokinin-2 receptors.
Molecular pharmacology - 1 Mar 2006
Foucaud Magali, Tikhonova Irina G, Langer Ingrid, Escrieut Chantal, Dufresne Marlène, Seva Cathy, Maigret Bernard, Fourmy Daniel
Abstract excerpt
Cholecystokinin receptor-2 (CCK2R) is a G protein receptor that regulates a number of physiological functions. Activation of CCK2R and/or expression of a constitutively active CCK2R variant may contribute to human diseases, including digestive cancers. Search for antagonists of the CCK2R has been an important challenge during the last few years, leading to discovery of a set of chemically distinct compounds....
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