Gaddum Memorial Lecture 2014: receptors as an evolving concept: from switches to biased microprocessors.

ABSTRACT: This review is based on the JR Vane Medal Lecture presented at the BPS Winter Meeting in December 2014 by T. Kenakin. A recording of the lecture is included as supporting information and can also be viewed online here: https://www.youtube.com/watch?v=xrP81AQ8l-8. Pharmacological models used to describe drug agonism and antagonism have evolved over the past 20 years from a parsimonious model describing single active and inactive receptor states to models of multiconformational receptor systems modified by ligand conformational selection. These latter models describe the observed, presently underexploited, pharmacological mechanism of ligand-directed biased signalling. Biased signals can be quantified with transduction coefficients (ΔΔLog(τ/KA) values), a scale grounded in the Black/Leff ope

SUBMITTER: Kenakin T 

PROVIDER: S-EPMC4556465 | biostudies-literature | 2015 Sep

REPOSITORIES: biostudies-literature