Efficiency measures the conversion of agonist binding energy into receptor conformational change.

ABSTRACT: Receptors alternate between resting↔active conformations that bind agonists with low↔high affinity. Here, we define a new agonist attribute, energy efficiency (η), as the fraction of ligand-binding energy converted into the mechanical work of the activation conformational change. η depends only on the resting/active agonist-binding energy ratio. In a plot of activation energy versus binding energy (an "efficiency" plot), the slope gives η and the y intercept gives the receptor's intrinsic activation energy (without agonists; ΔG₀). We used single-channel electrophysiology to estimate η for eight different agonists and ΔG₀ in human endplate acetylcholine receptors (AChRs). From published equilibrium constants, we also estimated η for agonists of K_Ca1.1 (BK ch

SUBMITTER: Nayak TK 

PROVIDER: S-EPMC6445574 | biostudies-literature | 2019 Apr

REPOSITORIES: biostudies-literature