Results 131 to 140 of about 3,246,752 (251)

Contact Activation Is Alleviated by Testosterone Replacement Therapy in Klinefelter Syndrome: Evidence of Hormonal and Metabolic Modulation

open access: yesAndrology, EarlyView.
ABSTRACT Background Klinefelter syndrome is associated with a markedly increased risk of venous thrombosis. While hypogonadism and metabolic dysfunction are known contributors, the role of the contact activation system in Klinefelter syndrome remains unexplored.
Simon Chang   +4 more
wiley   +1 more source

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

Targeting protein–protein interactions with reversible covalent modalities: Non‐cysteine chemistries

open access: yesBritish 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

Investigating the Residue-Level Dynamics of the Thrombin-Thrombomodulin Interaction [PDF]

open access: yesBiophysical Journal, 2020
Riley B. Peacock   +2 more
openaire   +1 more source

Renal‐vascular axis: unmasking its role in vascular endothelial growth factor‐inhibitor vascular toxicity in cancer patients

open access: yesBritish Journal of Pharmacology, EarlyView.
Abstract Vascular toxicity is a growing concern in cancer patients receiving vascular endothelial growth factor inhibitor (VEGFi) therapy, posing a significant threat to patient prognosis. While the primary mechanism of VEGFi‐induced vascular toxicity is linked to redox‐sensitive reactions that disrupt vascular tone, leading to hypertension and ...
Grace Whelan, Karla B. Neves
wiley   +1 more source

Natural product‐derived TRPM7 channel inhibitors in neurological injury: Mechanisms, pharmacological potential and translational challenges

open access: yesBritish Journal of Pharmacology, EarlyView.
Disruption of intracellular ionic homeostasis is a convergent pathological feature across diverse neurological injuries and disorders, including ischaemic and haemorrhagic stroke, hypoxic–ischaemic brain injury, traumatic brain injury, epilepsy and brain tumour.
Xinyang Zhang   +5 more
wiley   +1 more source

Thrombin-induced reactive oxygen species generation in platelets: A novel role for protease-activated receptor 4 and GPIba.

open access: yes, 2015
BACKGROUND: Platelets are essential for maintaining haemostasis and play a key role in the pathogenesis of cardiovascular disease. Upon ligation of platelet receptors through subendothelial matrix proteins, intracellular reactive oxygen species (ROS) are
E. Gardiner (23305693)   +7 more
core  

A Biweekly GLP‐1R Agonist Designed With Drug‐Free Intervals for Enhanced Efficacy, Receptor Homeostasis and Gastrointestinal Tolerability

open access: yesDiabetes, Obesity and Metabolism, EarlyView.
ABSTRACT Aim To develop a next‐generation, longer‐acting, more‐clinical‐benefits agonist to achieve sustained efficacy with improved tolerability. Methods CT130 was designed from semaglutide. Binding affinity was validated via molecular dynamics and cellular assays.
Wei Ding   +4 more
wiley   +1 more source

RNF13 regulates the endolysosomal pathway through interaction with the small GTPase Arl8B

open access: yesThe FEBS Journal, EarlyView.
The E3 ubiquitin ligase RNF13 functions as a regulatory scaffold, organizing Arl8B‐dependent complexes and tuning downstream signaling that controls endolysosomal organization and trafficking. In this model, wild‐type RNF13 associates with Arl8B on endolysosomes, whereas Arl8B (E22D/F55A) or RNF13 (L244A) variants weaken complex assembly, potentially ...
Audrey M. Sénécal   +4 more
wiley   +1 more source

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