Results 131 to 140 of about 122,133 (302)

Non‐canonical PKG1 regulation in cardiovascular health and disease

open access: yesBritish 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

A quad‐cistronic fluorescent biosensor system for real‐time detection of subcellular Ca2+ signals

open access: yesBritish Journal of Pharmacology, EarlyView.
Background and Purpose The calcium ion (Ca2+) is a versatile cellular messenger regulating a variety of biological processes. Compounds modulating subcellular Ca2+ signals hold substantial pharmacological potential. Advances in fluorescent biosensors have revolutionised Ca2+ imaging.
Anna Lischnig   +7 more
wiley   +1 more source

Impact of incretin analogues on lipid and lipoprotein metabolism in obesity and diabetes

open access: yesBritish 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

open access: yesBritish 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   +6 more
wiley   +1 more source

Isolation of the calmodulin N-methyltransferase and characterization of its interaction with calmodulin [PDF]

open access: yes, 1996
The methyltransferase that catalyzes the trimethylation of lysine 115 in calmodulin has been purified from sheep brain. The enzyme is a monomer with an apparent molecular weight of 38,000 based on gel filtration chromatography and SDS-polyacrylamide ...
Han, Chang-Hoon
core   +1 more source

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

open access: yesBritish 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   +6 more
wiley   +1 more source

Functional screen for subtype specificity of voltage sensor–targeted Kv7 potentiators

open access: yesBritish Journal of Pharmacology, EarlyView.
Background and Purpose Voltage‐gated Kv7 (potassium channel subfamily Q [KCNQ]) potassium channels are powerful modulators of neuronal excitability. ICA‐069673 is a N‐aryl benzamide drug that targets the voltage‐sensing domain (VSD) of Kv7.2 with strong selectivity over Kv7.3 or Kv7.5, but the molecular basis of this selectivity remains poorly ...
Richard Kanyo   +6 more
wiley   +1 more source

Peripheral κ opioid receptor in pain and inflammation: From molecular signalling and gene expression to drug discovery

open access: yesBritish Journal of Pharmacology, EarlyView.
The κ opioid receptor (κ receptor, KOR) is a G protein‐coupled receptor with well established roles in analgesia and immune modulation. Although historically studied primarily in the central nervous system (CNS), growing evidence indicates that κ signalling in peripheral tissues plays an important role in regulating pain, inflammation and immune ...
Rumsha Khan   +3 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

open access: yesBritish 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   +7 more
wiley   +1 more source

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

open access: yesBritish 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   +11 more
wiley   +1 more source

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