The Receptor Concept: Prejudice, Prediction, and Paradox

Abstract

This is a time of “great expectations” in the field of hormone and neurotransmitter action. Recent advances in our understanding of receptors have been so dramatic that we appear to be at the threshold of finally resolving the molecular nature of cellular receptors. The nature of these receptors is an important issue in biology which transcends endocrinology and neural transmission; it concerns the cardinal problem in the broad area of intercellular and intracellular communication. The once “elusive” receptors for hormones and neurotransmitters, long postulated to be the primary functional units for initiation of biological action, now appear to be “real” molecules. Specific macromolecular binding units for certain hormones and transmitters, with kinetic and specificity characteristics expected for a receptor have been reported. They can be isolated and manipulated. In several cases these receptors, derived either from the “cytosol” or solubilized from plasma membranes have been isolated in pure form. It is widely accepted that if we now follow the same strategy so successfully employed by the enzymologists (first isolate, then proceed to chemical characterization and determination of subunit sequences, conformational analysis, finally X-ray analysis) that the intimate molecular details of receptor structure and function will be clarified.

The studies described have been aided by grants from the Rockefeller Foundation and NIH Grant PO l-HD-06273.