Results 141 to 150 of about 115,342,253 (257)

Differential segment‐specific signalling pathways for guanylate cyclase C‐activated anion secretion in murine ileocolon

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, Johannes Reiner, Franz Hofmann, Azam Salari, Ursula Seidler   +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, Alan Armstrong, David J. Mann   +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

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

Atrial natriuretic peptide counteracts aldosterone secretion by preventing acute angiotensin II‐induced cAMP signalling

British Journal of Pharmacology, EarlyView.
Background and Purpose Aldosterone plays a key role in blood pressure and volume regulation. Enhanced aldosterone secretion contributes to cardiovascular and renal diseases. Therefore, inhibitors of aldosterone receptors and synthase are essential drugs for the treatment of hypertension and heart failure.
Sanika Mohagaonkar, Egor B. Skryabin, Bettina M. Buchholz, Michaela Kuhn, Celso E. Gomez‐Sanchez, Stepan Gambaryan, Viacheslav O. Nikolaev   +6 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

Inhibition of late sodium current prevents pathological hyperactivation of calcium/calmodulin‐dependent protein kinase IIδ in a murine model of acute doxorubicin‐related cardiotoxicity

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Doxorubicin (DOX) is a highly effective anthracycline, whose clinical application for cancer is limited by cardiotoxicity. The mechanisms underlying doxorubicin‐induced toxic cardiomyopathy (DICM) involve electrophysiological remodelling with intracellular Na+ overload because of increased late INa and hyperactivation of
Anna‐Lena Feder, Anna‐Maria Pfützenreuter, Lea Maria Funke, Maria Johanna Baier, Daniel Tarnowski, Laura Stengel, Lars Siegfried Maier, Can Martin Sag   +7 more
wiley   +1 more source

Alamandine/MrgD pathway modulates gut–bone marrow axis in ageing

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Ageing is associated with colon epithelial barrier disruption and up‐regulation of myelopoiesis in the bone marrow (BM). Alamandine (Ala) and MrgD are novel members of the renin angiotensin system (RAS). This study tested the hypothesis that Ala restores the colon epithelial barrier integrity in ageing via modulating gut–
Kishore Chittimalli, Henryata E. Rozario, Victor Martinez, Zachary L. McAdams, Stephen A. Adkins, Aaron C. Ericsson, Yagna P. R. Jarajapu   +6 more
wiley   +1 more source

Phloroglucinol inhibits human ureteral contractions via activation of cAMP‐PKA pathway

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Phloroglucinol is used to treat renal colic, especially when non‐steroidal anti‐inflammatory drugs are contraindicated. This study aimed to clarify its mechanism by examining effects on human ureteral contractility and underlying signalling pathways. Experimental Approach Urinary levels of neurokinin A (NKA), substance P
Hanwen Liu, Ruize Xu, Zihan Guan, Lei Liu, Guangda Lv, Weibo Chen, Jiliang Wen, Jianing Liu, Jieke Yan, Fangxin Gong, Pan Xiao, Xiulin Zhang, Lei Zhang   +12 more
wiley   +1 more source