Determination of dependence of binding parameters on receptor occupancy

✍ Scribed by Aldo Rescigno; James S. Beck; H. Joseph Goren

• Book ID: 104272444
• Publisher: Springer
• Year: 1982
• Tongue: English
• Weight: 591 KB
• Volume: 44
• Category: Article
• ISSN: 1522-9602
• DOI: 10.1016/s0092-8240(82)80052-9

✦ Synopsis

Measurements of the binding of ligand to receptors that are macromolecules, either free or components of biomembranes, often show deviation from what is expected of a simple reaction described by an association and a dissociation rate constant. A more versatile model and more discriminating experiments are required for a satisfactory explanation. This paper is based on a general model of the binding reaction in which the rate constants and equilibrium constant are dependent upon occupancy of receptors. The analysis of the model leads to three kinds of experiments: (1) equilibrium measurements which permit quantitative determination of a dissociation equilibrium parameter as a function of receptor occupancy; (2) measurements prior to equilibrium which yield the same information; and (3) measurements prior to equilibrium which reveal quantitatively the dependence of both association and dissociation rate parameters separately, on occupancy.