Mechanism of Action and Structure–Activity Relationships of Tetracyclic Small Molecules Acting as Universal Positive Allosteric Modulators of the Cholecystokinin Receptor
Abstract:As part of an ongoing effort to develop a drug targeting the type 1 cholecystokinin receptor (CCK1R) to help prevent and/or treat obesity, we recently performed a high throughput screening effort of small molecules seeking candidates that enhanced the action of the natural agonist, CCK, thus acting as positive allosteric modulators without exhibiting intrinsic agonist action. Such probes would be expected to act in a temporally finite way to enhance CCK action to induce satiety during and after a meal and pote… Show more
“…Dengler et al [6] investigated the molecular basis for the cholecystokinin (CCK) action of type 1 CCK receptor (CCK1R) positive allosteric modulator (PAM) ligands. Their findings expanded our understanding of the structure-activity relationships of molecules with tetracyclic scaffolds.…”
Plasma and intracellular membranes are characterized by different lipid compositions that enable proteins to localize to distinct subcellular compartments [...]
“…Dengler et al [6] investigated the molecular basis for the cholecystokinin (CCK) action of type 1 CCK receptor (CCK1R) positive allosteric modulator (PAM) ligands. Their findings expanded our understanding of the structure-activity relationships of molecules with tetracyclic scaffolds.…”
Plasma and intracellular membranes are characterized by different lipid compositions that enable proteins to localize to distinct subcellular compartments [...]
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