International union of basic and clinical pharmacology. CXII: adenosine receptors: a further update

AP IJzerman, KA Jacobson, CE Müller… - Pharmacological …, 2022 - Elsevier
Abstract Our previous International Union of Basic and Clinical Pharmacology report on the
nomenclature and classification of adenosine receptors (2011) contained a number of …

Biased signalling: from simple switches to allosteric microprocessors

JS Smith, RJ Lefkowitz, S Rajagopal - Nature reviews Drug discovery, 2018 - nature.com
G protein-coupled receptors (GPCRs) are the largest class of receptors in the human
genome and some of the most common drug targets. It is now well established that GPCRs …

Biased receptor signaling in drug discovery

T Kenakin, EL Barker - Pharmacological reviews, 2019 - Elsevier
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 …

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 …

Biased signaling of G protein coupled receptors (GPCRs): Molecular determinants of GPCR/transducer selectivity and therapeutic potential

M Seyedabadi, MH Ghahremani, PR Albert - Pharmacology & therapeutics, 2019 - Elsevier
G protein coupled receptors (GPCRs) convey signals across membranes via interaction with
G proteins. Originally, an individual GPCR was thought to signal through one G protein …

A kinetic view of GPCR allostery and biased agonism

JR Lane, LT May, RG Parton, PM Sexton… - Nature chemical …, 2017 - nature.com
G-protein-coupled receptors (GPCRs) are one of the most tractable classes of drug targets.
These dynamic proteins can adopt multiple active states that are linked to distinct functional …

A3 Adenosine Receptors as Modulators of Inflammation: From Medicinal Chemistry to Therapy

KA Jacobson, S Merighi, K Varani… - Medicinal research …, 2018 - Wiley Online Library
The A3 adenosine receptor (A3AR) subtype is a novel, promising therapeutic target for
inflammatory diseases, such as rheumatoid arthritis (RA) and psoriasis, as well as liver …

Biased ligands of G protein-coupled receptors (GPCRs): Structure–functional selectivity relationships (SFSRs) and therapeutic potential

L Tan, W Yan, JD McCorvy, J Cheng - Journal of medicinal …, 2018 - ACS Publications
G protein-coupled receptors (GPCRs) signal through both G-protein-dependent and G-
protein-independent pathways, and β-arrestin recruitment is the most recognized one of the …

Mu-Opioid receptor biased ligands: A safer and painless discovery of analgesics?

A Madariaga-Mazón, AF Marmolejo-Valencia, Y Li… - Drug discovery today, 2017 - Elsevier
Highlights•μ-OR biased agonists represent promising analgesics with improved therapeutic
profiles.•Protein-ligand interactions might account for biased ligands functional …

Human Adenosine A2A Receptor: Molecular Mechanism of Ligand Binding and Activation

B Carpenter, G Lebon - Frontiers in pharmacology, 2017 - frontiersin.org
Adenosine receptors (ARs) comprise the P1 class of purinergic receptors and belong to the
largest family of integral membrane proteins in the human genome, the G protein-coupled …