T Kenakin, A Christopoulos - Nature reviews Drug discovery, 2013 - nature.com
Agonists of seven-transmembrane receptors, also known as G protein-coupled receptors (GPCRs), do not uniformly activate all cellular signalling pathways linked to a given seven …
A great deal of experimental evidence suggests that ligands can stabilize different receptor active states that go on to interact with cellular signaling proteins to form a range of different …
H Kitano - Nature Reviews Genetics, 2004 - nature.com
Robustness is a ubiquitously observed property of biological systems. It is considered to be a fundamental feature of complex evolvable systems. It is attained by several underlying …
T Kenakin, LJ Miller - Pharmacological reviews, 2010 - ASPET
It is useful to consider seven transmembrane receptors (7TMRs) as disordered proteins able to allosterically respond to a number of binding partners. Considering 7TMRs as allosteric …
The concept of biased agonism has recently come to the fore with the realization that seven- transmembrane receptors (7TMRs, also known as G protein–coupled receptors, or GPCRs) …
Members of the heterotrimeric guanine nucleotide–binding protein (G protein)–coupled receptor (GPCR) family play key roles in many physiological functions and are extensively …
Glycine is a major neurotransmitter involved in several fundamental neuronal processes. The identity of the metabotropic receptor mediating slow neuromodulatory effects of glycine …
KA Berg, WP Clarke - International Journal of …, 2018 - academic.oup.com
Constitutive receptor activity/inverse agonism and functional selectivity/biased agonism are 2 concepts in contemporary pharmacology that have major implications for the use of drugs …
WK Kroeze, DJ Sheffler, BL Roth - Journal of cell science, 2003 - journals.biologists.com
G-protein-coupled receptors (GPCRs) constitute a large and diverse family of proteins whose primary function is to transduce extracellular stimuli into intracellular signals. They …