Receptor modulator

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A receptor modulator, or receptor ligand, is a general term for a substance, endogenous or exogenous, that binds to and regulates the activity of chemical receptors. They are ligands that can act on different parts of receptors and regulate activity in a positive, negative, or neutral direction with varying degrees of efficacy. Categories of these modulators include receptor agonists and receptor antagonists, as well as receptor partial agonists, inverse agonists, orthosteric modulators, and allosteric modulators,[1] Examples of receptor modulators in modern medicine include CFTR modulators,[2] selective androgen receptor modulators (SARMs), and muscarinic ACh receptor modulators.

See also


  1. ^ van Westen GJ, Gaulton A, Overington JP (April 2014). "Chemical, target, and bioactive properties of allosteric modulation". PLOS Computational Biology. 10 (4): e1003559. Bibcode:2014PLSCB..10E3559V. doi:10.1371/journal.pcbi.1003559. PMC 3974644. PMID 24699297.
  2. ^ "CFTR Modulator Therapies". Cystic Fibrosis Foundation. Retrieved 2020-12-08.