Binding Energy and the Stimulation of Hormone Receptors

  • T. J. Franklin
Conference paper


To fulfill their physiological roles a hormonal agonist and its receptor must first recognize each other and proceed to a highly specific binding interaction. It is generally believed that this interaction leads to some degree of conformational change in the receptor (receptor stimulation) which in many cases is coupled to an effector system that regulates the intracellular levels of a second messenger such as cyclic AMP or calcium ions. Amplification of the signal arising from the agonist-receptor interaction usually depends upon the initiation of a cascade by the second messenger which culminates in the appropriate biological end response. In other instances the receptor directly controls ion fluxes across the cell membranes (e.g. nicotinic receptors). Steroid receptors after stimulation translocate to the cell nucleus and activate transcription of specific regions of the genome. The amplification systems, which are such a striking feature of hormonal and neuroendocrine action, have been the subject of intense research activity for the past two decades. The situation is very different with regard to the nature of the primary interaction between agonists and their receptors and the conformational changes that ensue. There have been a few reports of efforts to analyze the basic thermodynamics of the binding phenomenon in receptor systems which will be discussed later but little or no effort has been directed to the study of the influence of ligand structure on essential conformational changes in the receptor.


Conformational Change Partial Agonist Transition State Theory Mass Action Model Binding Energy Contribution 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.


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Copyright information

© Springer-Verlag Berlin Heidelberg 1986

Authors and Affiliations

  • T. J. Franklin
    • 1
  1. 1.Pharmaceuticals DivisionImperial Chemical Industries PLCMacclesfield, CheshireUK

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