Allosteric Optical Control of a Class B G-Protein-Coupled Receptor

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Introduction: Regulation of endogenous glucose production (EGP) is essential for glucose homeostasis. It includes gluconeogenesis (GNG) from non-carbohydrate substrates and hepatic glycogenolysis. Both these pathways are dysregulated in acute stress, but t ...

Cells are attractive as carriers that can help to enhance control over the biodistribution of polymer nanomedicines. One strategy to use cells as carriers is based on the cell surface immobilization of the nanoparticle cargo. While a range of strategies ca ...

Over the last few decades, proteins and peptides have become increasingly more common as FDA-approved drugs, despite their inefficient delivery due to their inability to cross the plasma membrane. In this context, bacterial two-component systems, termed AB ...

Peptides have a number of attractive properties that make them an interesting modality for drug development, including their ability to bind challenging targets, their high target specificity, and their non-toxic metabolic products. However, a major limita ...

G protein-coupled receptors play essential roles in cellular processes such as neuronal signaling, vision, olfaction, tasting, and metabolism. As GPCRs are the most important drug targets, understanding their interactions with ligands is of utmost importan ...

The small molecule kinase inhibitor SBI-0206965 was originally described as a specific inhibitor of ULK1/2. More recently, it was reported to effectively inhibit AMPK and several studies now report its use as an AMPK inhibitor. Currently, we investigated t ...

Women with intrahepatic cholestasis of pregnancy (ICP), a disorder characterised by raised serum bile acids, are at increased risk of developing gestational diabetes mellitus and have impaired glucose tolerance whilst cholestatic. FXR and TGR5 are modulato ...

Pancreatic beta-cells secrete insulin to lower blood glucose, following a meal. Maintenance of beta-cell function is essential to preventing type 2 diabetes. In pancreatic beta-cells, mitochondrial matrix calcium is an activating signal for insulin secreti ...

Mitochondrial dysfunction is associated with aging-mediated inflammatory responses, leading to metabolic deterioration, development of insulin resistance, and type 2 diabetes. Growth differentiation factor 15 (GDF15) is an important mitokine generated in r ...

Allosteric Optical Control of a Class B G-Protein-Coupled Receptor

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Magnitude of gluconeogenesis and endogenous glucose production: are they predictable in clinical settings?

Covalent and Noncovalent Conjugation of Degradable Polymer Nanoparticles to T Lymphocytes

Harnessing the Membrane Translocation Properties of AB Toxins for Therapeutic Applications

Towards the Development of Orally Available Peptide Therapeutics

Enhancing the Signaling of GPCRs via Orthosteric Ions

The ULK1/2 and AMPK Inhibitor SBI-0206965 Blocks AICAR and Insulin-Stimulated Glucose Transport

Maternal glucose homeostasis is impaired in mouse models of gestational cholestasis

Targeting Mitochondrial Calcium Uptake with the Natural Flavonol Kaempferol, to Promote Metabolism/Secretion Coupling in Pancreatic beta-cells

Growth differentiation factor 15 protects against the aging-mediated systemic inflammatory response in humans and mice