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October 2022 Cholesterol-Dependent Dynamics of the Serotonin1A Receptor Utilizing Single Particle Tracking To explore the role of cholesterol in lateral dynamics of GPCRs, we utilized single particle tracking

We used TIRF microscopy and a statistical method to track and classify the motion of different receptor

To explore the role of cholesterol in lateral dynamics of GPCRs, we utilized single particle tracking

October 2022 Dimerization of β2-adrenergic receptor is responsible for the constitutive activity subjected to inverse agonism "Dimerization of beta 2-adrenergic receptor (β2-AR) has been observed across various physiologies. However, the function of dimeric β2-AR is still elusive. Here, we revealed that dimerization of β2-AR is responsible for the constitutive activity of β2-AR generating inverse agonism. Using a co-immunoimmobilization assay, we found that transient β2-AR dimers exist in a resting state, and the dimer was disrupted by the inverse agonists. A Gαs preferentially interacts with dimeric β2-AR, but not monomeric β2-AR, in a resting state, resulting in the production of a resting cAMP level. The formation of β2-AR dimers requires cholesterol on the plasma membrane. The cholesterol did not interfere with the agonist-induced activation of monomeric β2-AR, unlike the inverse agonists, implying that the cholesterol is a specific factor regulating the dimerization of β2-AR. Our model not only shows the function of dimeric β2-AR but also provides a molecular insight into the mechanism of the inverse agonism of β2-AR." Read more at the source #DrGPCR #GPCR #IndustryNews Subscribe to the Dr. GPCR Newsletter

August 2022 "Genetically encoded fluorescent biosensors allow intracellular signaling dynamics to be tracked By combining fiber photometry with FRET-based biosensors, we were able to track GPCR-dependent signaling

September 2022 "Yeast use the G-protein–coupled receptor signaling pathway to detect and track the mating

mediated signal transduction.[47] The 2000 Nobel Prize in Physiology or Medicine went to Eric Richard Kandel Dopamine exerts its action in the human nervous system via dopamine receptors and human trace amine-associated proteins, particularly kinases and phosphatases, that are involved in synaptic transmission[55,56] Kandel Kandel – Facts - NobelPrize.org. https://www.nobelprize.org/prizes/medicine/2000/kandel/facts/. 52.

Retrograde trans-synaptic rabies virus tracing revealed that postsynaptic cAMP signaling is required

AlphaFold accelerated discovery of psychotropic agonists targeting the trace amine-associated receptor

GPCR-Expressing Cell Membrane for Targeted Extraction Using Minimum Organic Solvent: An Investigative Study of Trace

and Taste Single-cell transcriptomic atlas of enteroendocrine cells along the murine gastrointestinal tract

advancing diabetes and obesity management, driving the obesity market toward $66 billion by 2030 and on track

Tracking N- and C-termini of C. elegans polycystin-1 reveals their distinct targeting requirements and

Hansell et al. 2011); and it may interfere with other chemokine receptors which share the ligands and

In the GI tract OR ligands drive an intracellular cascade that results in enhanced serotonin release