G. Ladds

ER-mitochondria distance is a critical parameter for efficient mitochondrial Ca2+ uptake and oxidative metabolism.

The paper shows that an optimal ER-mitochondria distance of ~20 nm is critical for efficient Ca2+ transfer and mitochondrial oxidative metabolism, with reduced distances observed in Parkinson's disease astrocytes.

Agonist efficacy at the B2AR is driven by agonist-induced differences in receptor affinity for the Gs protein, not ligand binding kinetics.

This study shows that agonist efficacy at the {beta}2AR is determined by differences in receptor affinity for Gs protein, not ligand binding kinetics.

Cancer-Associated Mutations Enhance The Sensitivity Of The Trupath GαQ/11 System

The paper modifies Gq and G11 biosensors to enhance sensitivity for detecting Gq/11 activation in GPCRs, including those with cancer-associated mutations.

RAMPs regulate signalling bias and internalisation of the GIPR

This study shows RAMPs modulate GIPR signaling and internalization, with RAMP3 reducing cAMP production and promoting surface retention, while RAMP1/2 decrease Gq/11/15 activation, and RAMP1 is essential for normal glucose regulation.

CGRP-receptor family reveals endogenous GPCR agonist bias and its significance in primary human cardiovascular cells

The paper demonstrates endogenous agonist bias at the calcitonin-like receptor in primary human cardiovascular cells, showing physiological consequences through RAMP switching.

Deciphering the Agonist Binding Mechanism to the Adenosine A1 Receptor

The paper uses molecular dynamics simulations and mutagenesis to study agonist binding to the A1 receptor, identifying new residues and binding modes of CPA-related ligands.

A Multisite Model of Allosterism for the Adenosine A1 Receptor

The paper models allosteric behavior of the adenosine A1 receptor using simulations of PAMs and agonists to explain their functional selectivity and binding properties.

Pharmacological Characterisation of Novel Adenosine Receptor A3R Antagonists

This study characterizes a selective A3R antagonist, K18, and identifies its binding mode through molecular dynamics simulations and mutagenesis.

Selective activation of Gαob by an adenosine A1 receptor agonist elicits analgesia without cardiorespiratory depression

The paper identifies BnOCPA as an A1R agonist that selectively activates Gαob, providing analgesia without cardiorespiratory depression.

Proposed model of the Dictyostelium cAMP receptors bound to cAMP

The paper presents homology models of cAMP receptors from Dictyostelium discoideum, highlighting structural features that may explain differential cAMP binding affinities and activation mechanisms.

GLP-1R is downregulated in beta cells of NOD mice and T1D patients

This study shows that GLP-1R is downregulated in beta cells of NOD mice and T1D patients, likely due to accelerated degradation, and suggests a role in autoimmune inflammation.

Elevated intracellular cAMP concentration mediates growth suppression in glioma cells

The paper shows that increasing intracellular cAMP levels via AC activation or PDE inhibition suppresses glioma cell growth, with different mechanisms depending on the PDE inhibitor used.

BCL11A interacts with SOX2 to control the expression of epigenetic regulators in lung squamous cell carcinoma

This study identifies BCL11A as an oncogene in lung squamous cell carcinoma, showing its interaction with SOX2 to regulate epigenetic factors and demonstrating potential therapeutic targets.