[HTML][HTML] Emerging roles of lysophospholipids in health and disease

ST Tan, T Ramesh, XR Toh, LN Nguyen - Progress in Lipid Research, 2020 - Elsevier
Lipids are abundant and play essential roles in human health and disease. The main
functions of lipids are building blocks for membrane biogenesis. However, lipids are also …

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 …

[HTML][HTML] Illuminating G-protein-coupling selectivity of GPCRs

A Inoue, F Raimondi, FMN Kadji, G Singh, T Kishi… - Cell, 2019 - cell.com
Heterotrimetic G proteins consist of four subfamilies (G s, G i/o, G q/11, and G 12/13) that
mediate signaling via G-protein-coupled receptors (GPCRs), principally by receptors binding …

A genetically encoded fluorescent sensor for rapid and specific in vivo detection of norepinephrine

J Feng, C Zhang, JE Lischinsky, M Jing, J Zhou… - Neuron, 2019 - cell.com
Norepinephrine (NE) is a key biogenic monoamine neurotransmitter involved in a wide
range of physiological processes. However, its precise dynamics and regulation remain …

Lysophospholipid mediators in health and disease

K Kano, J Aoki, T Hla - Annual Review of Pathology …, 2022 - annualreviews.org
Lysophospholipids, exemplified by lysophosphatidic acid (LPA) and sphingosine 1-
phosphate (S1P), are produced by the metabolism and perturbation of biological …

[HTML][HTML] Membrane phosphoinositides regulate GPCR-β-arrestin complex assembly and dynamics

J Janetzko, R Kise, B Barsi-Rhyne, DH Siepe… - Cell, 2022 - cell.com
Binding of arrestin to phosphorylated G protein-coupled receptors (GPCRs) is crucial for
modulating signaling. Once internalized, some GPCRs remain complexed with β-arrestins …

Biased allosteric modulators: new frontiers in GPCR drug discovery

LM Slosky, MG Caron, LS Barak - Trends in Pharmacological Sciences, 2021 - cell.com
G protein-coupled receptors (GPCRs) are the largest class of cell surface receptors in the
genome and the most successful family of targets of FDA-approved drugs. New frontiers in …

Heterotrimeric Gq proteins act as a switch for GRK5/6 selectivity underlying β-arrestin transducer bias

K Kawakami, M Yanagawa, S Hiratsuka… - Nature …, 2022 - nature.com
Signaling-biased ligands acting on G-protein-coupled receptors (GPCRs) differentially
activate heterotrimeric G proteins and β-arrestins. Although a wealth of structural knowledge …

The experimental power of FR900359 to study Gq-regulated biological processes

R Schrage, AL Schmitz, E Gaffal, S Annala… - Nature …, 2015 - nature.com
Despite the discovery of heterotrimeric αβγ G proteins∼ 25 years ago, their selective
perturbation by cell-permeable inhibitors remains a fundamental challenge. Here we report …

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 …