Receptor Theory and the Ligand-Macromolecule Complex

Research output: Chapter in Book/Report/Conference proceedingChapter

3 Scopus citations


A key concept in biological sciences including pharmacology and toxicology is that bioactive small molecules such as drugs, hormones, and nutrients must achieve adequate concentration at a target site in order to elicit a biological response. For many chemicals, the ultimate site of action is a cognate protein or 'receptor.' The main criteria for the operational term 'receptor' are the functions of recognition and transduction. By this definition, a receptor must recognize a distinct chemical entity and translate information from that entity into a form that the cell can interpret, and alter its state accordingly. This altered state may be a change in permeability, activation of a guanine nucleotide regulatory protein, or an alteration in the transcription of DNA. To differentiate a receptor from an enzyme, the recognition unit should not chemically alter the small molecule and, to differentiate from a binding protein, a receptor must produce a biochemical change and transmit the signal. Often the receptor is a protein and a single component of a large complex of macromolecules that may include other proteins, RNA, and DNA.

Original languageEnglish (US)
Title of host publicationComprehensive Toxicology
Subtitle of host publicationSecond Edition
PublisherElsevier Inc.
Number of pages24
ISBN (Print)9780080468846
StatePublished - Jan 1 2010

All Science Journal Classification (ASJC) codes

  • Medicine(all)


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