Results 121 to 130 of about 79,392 (254)
Compartmentalisation in cAMP signalling: A phase separation perspective
British Journal of Pharmacology, EarlyView.Cells rely on precise spatiotemporal control of signalling pathways to ensure functional specificity. The compartmentalisation of cyclic AMP (cAMP) and protein kinase A (PKA) signalling enables distinct cellular responses within a crowded cytoplasmic space.
Milda Folkmanaite, Manuela Zaccolo
wiley +1 more source
Non‐canonical PKG1 regulation in cardiovascular health and disease
British Journal of Pharmacology, EarlyView.It is well established that the cyclic GMP‐dependent protein kinase I (PKG1) is canonically activated by cyclic guanosine monophosphate (cGMP), enabling its regulation of vascular tone, cardiac function and smooth muscle homeostasis. However, diverse non‐canonical stimuli of PKG1 have also been identified.
Jie Su, Joseph Robert Burgoyne
wiley +1 more source
PDE4D and PDE3B orchestrate distinct cAMP microdomains in 3T3‐L1 adipocytes
British Journal of Pharmacology, EarlyView.Basal conditions: •Ins/PDE3B lowers cytoplasmic cAMP (cyt‐cAMP) without affecting plasma membrane cAMP (pm‐cAMP). •Insulin decreases lipid droplet cAMP (LD‐cAMP) independent of PDE3B. •FGF1/PDE4D modestly reduces both cyt‐ and pm‐cAMP, while PDE4D alone can modulate LD‐cAMP. ISO stimulation: •Ins/PDE3B has minimal impact on cyt‐cAMP.
Johannes Krier +9 more
wiley +1 more source
British Journal of Pharmacology, EarlyView.Abstract Background and Purpose Guanylate cyclase‐C (GC‐C) is the receptor for endogenous (uro)guanylin peptides, bacterial toxins and pharmacological analogues. Receptor activation leads to intestinal fluid loss, but also activates an antiproliferative pathway and is a promising target in colorectal cancer therapy.
Renjie Xiu +4 more
wiley +1 more source
Covalent drug discovery: Progress against key targets, emerging strategies and lessons learnt
British Journal of Pharmacology, EarlyView.Abstract Covalent drug discovery is currently experiencing a boom in industrial and academic interest. To date, at least 75 covalent drugs have received regulatory approval, targeting both traditional target classes and more challenging proteins for which other approaches failed. In many cases, unique aspects of covalent targeting are essential for the
Charles P. Brown +2 more
wiley +1 more source
Targeting protein–protein interactions with reversible covalent modalities: Non‐cysteine chemistries
British Journal of Pharmacology, EarlyView.Abstract Protein–protein interactions (PPIs) are central to diverse cellular functions, and represent a rapidly expanding class of therapeutic targets. Advancements in covalent drug design have enabled small‐molecule drugs to overcome challenges associated with engaging these targets, such as limited durations of action and difficult‐to‐drug (expansive,
Ruchira Basu, Steven Fletcher
wiley +1 more source
Protein Kinase A in neurological disorders
Journal of Neurodevelopmental DisordersCyclic adenosine 3’, 5’ monophosphate (cAMP)-dependent Protein Kinase A (PKA) is a multi-functional serine/threonine kinase that regulates a wide variety of physiological processes including gene transcription, metabolism, and synaptic plasticity ...
Alexander G. P. Glebov-McCloud +3 more
doaj +1 more source
Caloric restriction controls stationary phase survival through Protein Kinase A (PKA) and cytosolic pH. [PDF]
Aging Cell, 2019 Dolz-Edo L +3 more
europepmc +1 more source
Impact of incretin analogues on lipid and lipoprotein metabolism in obesity and diabetes
British Journal of Pharmacology, EarlyView.Abstract Incretin‐based therapies have gained momentum as a key strategy for reducing cardiovascular risk in individuals with obesity and/or type 2 diabetes (T2D). It remains unclear whether the cardiovascular benefits reflect a direct reduction in atherogenic lipoproteins—namely, low‐density lipoproteins (LDL), very low‐density lipoproteins (VLDL) and
Andrea Baragetti, Giuseppe Danilo Norata
wiley +1 more source