7TM pharmacology measured by label-free: a holistic approach to cell signalling.

摘要: Ligands acting at 7-transmembrane receptors (7TMs) transduce effects on cellular behaviour in a notion termed efficacy; turn, the or phenotype can be quantified. Underpinning efficacy is ability of ligands to dictate triggering distinct intracellular signalling event(s) system-dependent manner through selective stabilisation receptor conformations. Given wealth putative cell routes species may possess (spectrum activities) and numerous mechanisms by which ligand–receptor pairings signal, call for an integrated solution activity has come light. The potential novel methodologies probe 7TM function such as label-free been subjected much attention recent years. Label-free detection differs greatly from arsenal so-called traditional techniques commonly employed. It provides temporally resolved cumulative readout using intact living cells. holds vast promise enabling behaviours estimated global ‘holistic’ manner. This article will focus key areas interest where particularly impactful late rather than covering principles behind (which have reviewed elsewhere). Firstly, it facilitated endogenous native-like systems that are possibly more physiologically relevant; secondly, offered unprecedented angles probing functional selectivity ligand efficacy.