Results 191 to 200 of about 88,568 (304)

Microscopy and spectroscopy approaches to study GPCR structure and function

open access: yesBritish Journal of Pharmacology, Volume 182, Issue 14, Page 3090-3108, July 2025.
Abstract The GPCR signalling cascade is a key pathway responsible for the signal transduction of a multitude of physical and chemical stimuli, including light, odorants, neurotransmitters and hormones. Understanding the structural and functional properties of the GPCR cascade requires direct observation of signalling processes in high spatial and ...
Tomáš Fessl   +2 more
wiley   +1 more source

G protein‐coupled receptor‐mediated autophagy in health and disease

open access: yesBritish Journal of Pharmacology, Volume 182, Issue 14, Page 3151-3162, July 2025.
G protein‐coupled receptors (GPCRs) constitute the largest and most diverse superfamily of mammalian transmembrane proteins. These receptors are involved in a wide range of physiological functions and are targets for more than a third of available drugs in the market. Autophagy is a cellular process involved in degrading damaged proteins and organelles
Devrim Öz‐Arslan   +2 more
wiley   +1 more source

Phosphorylation of Src by phosphoinositide 3-kinase regulates beta-adrenergic receptor-mediated EGFR transactivation [PDF]

open access: green, 2016
Lewis J. Watson   +7 more
openalex   +1 more source

Altered desensitization and internalization patterns of rodent versus human glucose‐dependent insulinotropic polypeptide (GIP) receptors. An important drug discovery challenge

open access: yesBritish Journal of Pharmacology, Volume 182, Issue 14, Page 3353-3370, July 2025.
Abstract Background and Purpose The gut hormone glucose‐dependent insulinotropic polypeptide (GIP) signals via the GIP receptor (GIPR), resulting in postprandial potentiation of glucose‐stimulated insulin secretion. The translation of results from rodent studies to human studies has been challenged by the unexpected effects of GIPR‐targeting compounds.
Lærke Smidt Gasbjerg   +18 more
wiley   +1 more source

The path to the G protein‐coupled receptor structural landscape: Major milestones and future directions

open access: yesBritish Journal of Pharmacology, Volume 182, Issue 14, Page 3225-3248, July 2025.
G protein‐coupled receptors (GPCRs) play a crucial role in cell function by transducing signals from the extracellular environment to the inside of the cell. They mediate the effects of various stimuli, including hormones, neurotransmitters, ions, photons, food tastants and odorants, and are renowned drug targets.
Małgorzata M. Kogut‐Günthel   +11 more
wiley   +1 more source

Ketotic Hypoglycaemia Following Sleeve Gastrectomy

open access: yesClinical Endocrinology, Volume 103, Issue 1, Page 45-49, July 2025.
ABSTRACT Post‐bariatric surgery hypoglycaemia is typically mediated by hyperinsulinaemia, although the exact mechanisms are incompletely understood. Two cases of non‐insulin mediated, ketotic hypoglycaemia following sleeve gastrectomy are presented. After fasting for 40 and 65 h, respectively, both patients developed symptomatic hypoglycaemia, with ...
Jinwen He   +3 more
wiley   +1 more source

Targeted protein degradation of PDE4 shortforms by a novel proteolysis targeting chimera

open access: yesThe FEBS Journal, Volume 292, Issue 13, Page 3360-3377, July 2025.
Here, we report KTX207, a previously undescribed cereblon‐based PDE4 PROTAC that can specifically target PDE4D shortform for degradation. We showed that KTX207 could improve selectivity, potency and enable a long‐lasting effect when used at a sub‐nanomolar concentration.
Yuan Yan Sin   +16 more
wiley   +1 more source

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