Results 121 to 130 of about 251,198 (269)

The potential for biased signalling in the P2Y receptor family of GPCRs

British Journal of Pharmacology, EarlyView.
The purinergic receptor family is primarily activated by nucleotides, and contains members of both the G protein coupled‐receptor (GPCR) superfamily (P1 and P2Y) and ligand‐gated ion channels (P2X). The P2Y receptors are widely expressed in the human body, and given the ubiquitous nature of nucleotides, purinergic signalling is involved with a plethora
Claudia M. Sisk, Simon Pitchford, Graham Ladds   +2 more
wiley   +1 more source

The nitty‐gritty of vascular permeability in cancer: targeting blood endothelium to control metastases

British Journal of Pharmacology, EarlyView.
Blood vascular permeability is a hallmark of cancer and acts as an active driver of metastatic dissemination. Metastasis accounts for the vast majority of cancer deaths, yet most work has focussed on tumour‐intrinsic traits and angiogenesis, while the specific contribution of endothelial barrier regulation to intravasation and extravasation remains ...
Pierre Boucher, Mérone Da Costa Oliveira, Adrien Levesque, Alexandre Rutault, Patrick Savoyaud, Nicolas Bréchot, Stéphane Germain   +6 more
wiley   +1 more source

Mechanistic principles of Rho GTPase patterning

Rho GTPases are regulators of morphogenesis in all eukaryotic cells. These peripheral membrane proteins spatially control actin cytoskeleton dynamics by locally concentrating at the plasma membrane in polarized activity patterns. However, the biochemical
Weiß, Yannic
core   +1 more source

Targeting KRAS for cancer therapy

British Journal of Pharmacology, EarlyView.
In recent years, therapeutics targeted against KRAS proto‐oncogene GTPase (KRAS)‐mutant cancers have seen significant progress. Herein we outline the biology and epidemiology of KRAS alterations at the lineage and allele levels, reviewing the clinical evidence for KRASG12C inhibition from the discovery of the recessive switch pocket to sotorasib ...
Jianlong Jia, Ruonan Liu, Tonia A. Adamide, Isis E. Fernandez, Georgios T. Stathopoulos   +4 more
wiley   +1 more source

CD93—An emerging vascular target in cancer therapy

British Journal of Pharmacology, EarlyView.
Abstract CD93 is a single‐pass transmembrane glycoprotein that belongs to the C‐type lectin domain group XIV family of proteins. Although it is known to be expressed in other cell types, namely, in some subsets of immune cells, CD93 is primarily expressed on endothelial cells, where it acts as a crucial regulator of angiogenesis.
Beatriz de Alves Pereira, Stefano Barbera, Roberta Lugano, Anna Dimberg   +3 more
wiley   +1 more source

Phosphoproteomics unveils the signaling dynamics in neuronal cells stimulated with insulin and insulin-like growth factors

Cell Communication and Signaling
Background Given the role of metabolism in brain health and disease, the investigation of the role of insulin (INS) and insulin-like growth factors (IGFs) as potential therapeutic strategies for neurodegenerative diseases is currently underway.
Mereena George Ushakumary, Ryan L. Sontag, Camilo Posso, Thomas L. Fillmore, Maisie E. Topping, Heather M. Olson, Philip L. De Jager, David A. Bennett, Zoe Arvanitakis, Vladislav A. Petyuk   +9 more
doaj   +1 more source

Inhibition of leucine‐rich kinase 2 (LRRK2) promotes peripheral axon regeneration via phosphorylation‐network remodelling

British Journal of Pharmacology, EarlyView.
Background and Purpose In contrast to neurons in the central nervous system, neurons in the peripheral nervous system can regenerate axons after injury via activation of a pro‐regenerative transcriptional programme. Pathogenic mutations in leucine‐rich repeat kinase 2 (LRRK2) are the most common genetic cause of Parkinson's disease, and several small ...
Eun‐Hae Jang, Eun Mo Yang, Gil Song, Seung Min Park, Harryn Choi, Jaeyong Kim, Chanil Kim, Yunho Gim, Hyuk‐Joo Jeon, Yewon Cho, Jong Bae Park, Eun‐Mi Hur   +11 more
wiley   +1 more source

Systematic profiling reveals broad G protein coupling and context‐dependent modulation of cyclic AMP by the orphan receptor GPR139

British Journal of Pharmacology, EarlyView.
Background and Purpose G protein‐coupled receptors (GPCRs) are major drug targets, yet many orphan receptors remain poorly characterized. GPR139 has been implicated in CNS disorders, including schizophrenia and depression, but its signalling mechanisms remain unclear.
Boris Trapkov, Hans Bräuner, Alexander Sebastian Hauser   +2 more
wiley   +1 more source

The lung is more than an organ of gas exchange: immunocompetency, platelets and implications for drug discovery

British Journal of Pharmacology, EarlyView.
Abstract The lungs have for a long time been recognised as having pharmacological significance as a specific organ to modulate the pharmacokinetics of endogenous substances needed to maintain homeostasis. The lungs are therefore the site of action of certain drugs that act on these homeostatic processes, resulting in systemic effects on the ...
Simon C. Pitchford
wiley   +1 more source

Long non‐coding RNAs at the crossroads of inflammation, cancer and angiogenesis: Molecular mechanisms and their potential as therapeutic targets

British Journal of Pharmacology, EarlyView.
Long non‐coding RNAs (lncRNAs), a broad class of non‐protein‐coding RNAs, are characterized as new regulators of gene expression at the epigenetic, transcriptional, and post‐transcriptional level. Thus, lncRNAs are involved in the regulation of physiological processes and the development of human diseases and cancer by modulating proinflammatory ...
Charlie Leboff, Pamela Calle‐Mendoza, Maria Hatziapostolou, Christos Polytarchou   +3 more
wiley   +1 more source