Metabolic Actions of the Type 1 Cholecystokinin Receptor: Its Potential as a Therapeutic Target

Laurence J. Miller, Aditya J. Desai

Research output: Contribution to journalReview articlepeer-review

16 Scopus citations

Abstract

Cholecystokinin (CCK) regulates appetite and reduces food intake by activating the type 1 CCK receptor (CCK1R). Attempts to develop CCK1R agonists for obesity have yielded active agents that have not reached clinical practice. Here we discuss why, along with new strategies to target CCK1R more effectively. We examine signaling events and the possibility of developing agents that exhibit ligand-directed bias, to dissociate satiety activity from undesirable side effects. Potential allosteric sites of modulation are also discussed, along with desired properties of a positive allosteric modulator (PAM) without intrinsic agonist action as another strategy to treat obesity. These new types of CCK1R-active drugs could be useful as standalone agents or as part of a rational drug combination for management of obesity.

Original languageEnglish (US)
Pages (from-to)609-619
Number of pages11
JournalTrends in Endocrinology and Metabolism
Volume27
Issue number9
DOIs
StatePublished - 2016

Keywords

  • biased agonists
  • cholecystokinin
  • positive allosteric modulators
  • satiety
  • type 1 cholecystokinin receptor

ASJC Scopus subject areas

  • Endocrinology, Diabetes and Metabolism
  • Endocrinology

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