Serotonin 2A Receptor (5-HT2AR) Agonists: Psychedelics and Non-Hallucinogenic Analogues as Emerging Antidepressants

W Duan, D Cao, S Wang, J Cheng - Chemical Reviews, 2023 - ACS Publications
Psychedelics make up a group of psychoactive compounds that induce hallucinogenic
effects by activating the serotonin 2A receptor (5-HT2AR). Clinical trials have demonstrated …

Signalling bias in new drug discovery: detection, quantification and therapeutic impact

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 …

Biased receptor signaling in drug discovery

T Kenakin - Pharmacological reviews, 2019 - ASPET
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 …

Biological robustness

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 …

Seven transmembrane receptors as shapeshifting proteins: the impact of allosteric modulation and functional selectivity on new drug discovery

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 …

Molecular mechanism of β-arrestin-biased agonism at seven-transmembrane receptors

E Reiter, S Ahn, AK Shukla… - Annual review of …, 2012 - annualreviews.org
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) …

Distinct profiles of functional discrimination among G proteins determine the actions of G protein–coupled receptors

I Masuho, O Ostrovskaya, GM Kramer, CD Jones… - Science …, 2015 - science.org
Members of the heterotrimeric guanine nucleotide–binding protein (G protein)–coupled
receptor (GPCR) family play key roles in many physiological functions and are extensively …

Orphan receptor GPR158 serves as a metabotropic glycine receptor: mGlyR

T Laboute, S Zucca, M Holcomb, DN Patil, C Garza… - Science, 2023 - science.org
Glycine is a major neurotransmitter involved in several fundamental neuronal processes.
The identity of the metabotropic receptor mediating slow neuromodulatory effects of glycine …

Making sense of pharmacology: inverse agonism and functional selectivity

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 …

G-protein-coupled receptors at a glance

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 …