ArticleBioorganic & medicinal chemistry letters2008
Benzodiazepine ligands can act as allosteric modulators of the Type 1 cholecystokinin receptor.
Article in Bioorganic & medicinal chemistry letters, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
16 citing papers in PubMed, 23 citations in OpenAlex.
- Article
- The Nonpeptide Agonist MK-5046 Functions As an Allosteric Agonist for the Bombesin Receptor Subtype-3.The Journal of pharmacology and experimental therapeutics · 2022Article
- Diazepam is not a direct allosteric modulator of αPharmacology research & perspectives · 2019Article
- Cholecystokinin-induced satiety, a key gut servomechanism that is affected by the membrane microenvironment of this receptor.International journal of obesity supplements · 2016Review
- Metabolic Actions of the Type 1 Cholecystokinin Receptor: Its Potential as a Therapeutic Target.Trends in endocrinology and metabolism: TEM · 2016Review
- Molecular Mechanism of Action of Triazolobenzodiazepinone Agonists of the Type 1 Cholecystokinin Receptor. Possible Cooperativity across the Receptor Homodimeric Complex.Journal of medicinal chemistry · 2015Article
- Development of a highly selective allosteric antagonist radioligand for the type 1 cholecystokinin receptor and elucidation of its molecular basis of binding.Molecular pharmacology · 2015Article
- International Union of Basic and Clinical Pharmacology. XC. multisite pharmacology: recommendations for the nomenclature of receptor allosterism and allosteric ligands.Pharmacological reviews · 2014Article
- A type 1 cholecystokinin receptor mutant that mimics the dysfunction observed for wild type receptor in a high cholesterol environment.The Journal of biological chemistry · 2014Article
- Molecular basis for benzodiazepine agonist action at the type 1 cholecystokinin receptor.The Journal of biological chemistry · 2013Article
- Molecular basis for binding and subtype selectivity of 1,4-benzodiazepine antagonist ligands of the cholecystokinin receptor.The Journal of biological chemistry · 2012Article
- Sensitivity of cholecystokinin receptors to membrane cholesterol content.Frontiers in endocrinology · 2012Article
- Fluorescence polarization screening for allosteric small molecule ligands of the cholecystokinin receptor.Assay and drug development technologies · 2011Article
- Therapeutic potential for novel drugs targeting the type 1 cholecystokinin receptor.British journal of pharmacology · 2010Review
- Synthesis and in vitro characterization of radioiodinatable benzodiazepines selective for type 1 and type 2 cholecystokinin receptors.Journal of medicinal chemistry · 2009Article
- Chemical biology investigation of cell death pathways activated by endoplasmic reticulum stress reveals cytoprotective modulators of ASK1.The Journal of biological chemistry · 2009Article
Corrections and comments
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Authors and funding
4 authors at 2 institutions in 2 countries.
Funding
Abstract
The cholecystokinin (CCK(1)) receptor is a G protein-coupled receptor important for nutrient homeostasis. The molecular basis of CCK-receptor binding has been debated, with one prominent model suggesting occupation of the same region of the intramembranous helical bundle as benzodiazepines. Here, we used a specific assay of allosteric ligand interaction to probe the mode of binding of devazepide, a prototypic benzodiazepine ligand. Devazepide elicited marked slowing of dissociation of pre-bound CCK, only possible through binding to a topographically distinct allosteric site. This effect was disrupted by chemical modification of a cysteine in the benzodiazepine-binding pocket. Application of an allosteric model to the equilibrium interaction between a series of benzodiazepine ligands and CCK yielded quantitative estimates of each modulator's affinity for the allosteric site, as well as the degree of negative cooperativity for the interaction between occupied orthosteric and allosteric sites. The allosteric nature of benzodiazepine binding to the CCK(1) receptor provides new opportunities for small molecule drug development.
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Registered trials
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