[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 …
functions of lipids are building blocks for membrane biogenesis. However, lipids are also …
Biased signalling: from simple switches to allosteric microprocessors
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 …
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
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 …
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
Norepinephrine (NE) is a key biogenic monoamine neurotransmitter involved in a wide
range of physiological processes. However, its precise dynamics and regulation remain …
range of physiological processes. However, its precise dynamics and regulation remain …
Lysophospholipid mediators in health and disease
Lysophospholipids, exemplified by lysophosphatidic acid (LPA) and sphingosine 1-
phosphate (S1P), are produced by the metabolism and perturbation of biological …
phosphate (S1P), are produced by the metabolism and perturbation of biological …
[HTML][HTML] Membrane phosphoinositides regulate GPCR-β-arrestin complex assembly and dynamics
Binding of arrestin to phosphorylated G protein-coupled receptors (GPCRs) is crucial for
modulating signaling. Once internalized, some GPCRs remain complexed with β-arrestins …
modulating signaling. Once internalized, some GPCRs remain complexed with β-arrestins …
Biased allosteric modulators: new frontiers in GPCR drug discovery
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 …
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 …
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 …
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 …
active states that go on to interact with cellular signaling proteins to form a range of different …