MINIREVIEW Agonists and Allosteric Modulators of the Calcium-Sensing Receptor and Their Therapeutic Applications
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چکیده
□S Influence of the Stereoisomeric Position of the Reactive Acetate Groups of the Benzo[b]Acronycine derivative S23906-1 on Its DNA Alkylation, Helix-Opening, Cytotoxic, and Antitumor Activities Sabine Depauw, Thomas Gaslonde, Stéphane Léonce, Laurence Kraus-Berthier, William Laine, Gaëlle Lenglet, Angèle Chiaroni, Bruno Pfeiffer, Christian Bailly, Sylvie Michel, François Tillequin, Alain Pierré, and Marie-Hélène David-Cordonnier 1172
منابع مشابه
Agonists and allosteric modulators of the calcium-sensing receptor and their therapeutic applications.
The calcium-sensing receptor (CaR) belongs to the G protein-coupled receptor superfamily, with a characteristic structure consisting of seven transmembrane helices, an intracellular C-terminal and an extracellular N terminal domain. The primary physiological function of the CaR is the maintenance of constant blood Ca2+ levels, as a result of its ability to sense very small changes in extracellu...
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The human extracellular Ca(2+)-sensing receptor (CaR), a member of the G protein-coupled receptor family 3, plays a key role in the regulation of extracellular calcium homeostasis. It is one of just a few G protein-coupled receptors with a large number of naturally occurring mutations identified in patients. In contrast to the small sizes of its agonists, this large dimeric receptor consists of...
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Allosteric modulators that are targeting the calcium-sensing receptor (CaSR) hold great therapeutic potential, and elucidating the molecular basis for modulation would thus benefit the development of novel therapeutics. In the present study, we aimed at investigating the mechanism of allosteric modulation in CaSR by testing dimers carrying mutations in the allosteric site of one or both of the ...
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