Results 11 to 20 of about 183,080 (139)

Fluorescent‐target imaging and real‐time beam diagnostics at the High Energy Photon Source

open access: yesJournal of Synchrotron Radiation, EarlyView.
A fluorescent‐target imaging and real‐time beam diagnostic platform has been developed for the High Energy Photon Source (HEPS), integrating synchronized multi‐camera acquisition within the Experimental Physics and Industrial Control System (EPICS) areaDetector framework, online beam‐parameter extraction, and Mamba Data Worker enabled data management ...
Qun Zhang   +8 more
wiley   +1 more source

Biochemical and structural characterization of a tail‐spike protein with depolymerase activity identified in a marine podovirus

open access: yesActa Crystallographica Section D, EarlyView.
The marine tail‐spike protein Dpo31 degrades the exopolysaccharide of its host and has structural features similar to those of other members of this protein class, despite similarity not being detected at the sequence level.Marine phages are, through the infection of their bacterial hosts, key regulators of microbiome and carbon fluxes in the ocean ...
Serena Sirigu   +7 more
wiley   +1 more source

Notoginsenoside‐Fa mitigates vascular endothelial permeability via targeting SUGT1 to stabilize NLRP3 in a resting state

open access: yesBritish Journal of Pharmacology, EarlyView.
Background and Purpose Notoginsenoside‐Fa (Noto‐Fa) is an emerging active compound derived from notoginseng with promise in treating cardiovascular diseases. The development of cardiovascular diseases is intricately linked to the damage of vascular endothelium and it is widely acknowledged that numerous chronic inflammation pathways, especially the ...
Xiao‐Ying Yu   +9 more
wiley   +1 more source

Flecainide binding dynamics in voltage‐gated sodium channels: A comparative isoform analysis of the state‐dependent block

open access: yesBritish Journal of Pharmacology, EarlyView.
Background and Purpose Local anaesthetics and class I anti‐arrhythmic drugs block voltage‐gated Na+ channels, but the molecular basis for the isoform differences in drug sensitivity remains unclear. Understanding these mechanisms is essential for optimizing therapeutic efficacy and safety.
Tatsuo Munakata   +4 more
wiley   +1 more source

Targeting the noncatalytic activity of GSK3β modulates neuronal excitability in medium spiny neurons via Nav1.6 interactions

open access: yesBritish Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Kinases phosphorylate ion channels, but their noncatalytic roles via protein–protein interactions (PPI) are less understood. Here, we identified the peptidomimetic ZL141 to characterize the PPI between GSK3β and Nav1.6, revealing a noncatalytic role for GSK3β in regulating Nav1.6 currents and neuronal excitability ...
Aditya K. Singh   +19 more
wiley   +1 more source

Contact sensitisers activate keratinocytes and induce cytotoxicity via Transient Receptor Potential Ankyrin 1 in allergic contact dermatitis

open access: yesBritish Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Allergic contact dermatitis (ACD) is a frequent inflammatory skin disease with limited therapeutic options. While neuronal Transient Receptor Potential Ankyrin 1 (TRPA1) has been implicated in ACD, the role of keratinocyte TRPA1 remains unclear.
Areej Jaber   +8 more
wiley   +1 more source

Identification of drug repurposing candidates for the treatment of polycystic kidney disease

open access: yesBritish Journal of Pharmacology, EarlyView.
Background and Purpose Autosomal dominant polycystic kidney disease (ADPKD) is a leading cause of end‐stage renal disease with limited treatment options. Drug repurposing offers a promising strategy to find effective treatments. Experimental Approach We identified birinapant, bardoxolone methyl and salicylic acid as repurposing candidates for ADPKD and
Alina Meyer   +9 more
wiley   +1 more source

Agonist‐specific conformational dynamics at the β2‐adrenoceptor dictate allosteric modulation of Gαs signalling and bronchodilation

open access: yesBritish Journal of Pharmacology, EarlyView.
Abstract Background and Purpose β2‐adrenoceptor (β2AR) agonists are the cornerstone of asthma therapy and promote bronchodilation through Gαs signalling in airway smooth muscle (ASM), but their efficacy is limited by β‐arrestin‐mediated β2AR desensitization.
Sushrut D. Shah   +7 more
wiley   +1 more source

Optimization of novel compounds using computer‐aided drug design for treatment of cardiac arrhythmia

open access: yesBritish Journal of Pharmacology, EarlyView.
Background and Purpose Loss‐of‐function mutations of the voltage‐gated Kv7.1 (KCNQ/KCNE1) channels lead to cardiac arrhythmia such as long QT syndrome, characterized by a prolonged QT interval . One strategy to correct the prolonged QT interval is to design molecules that activate KCNQ1/KCNE1 channels and restore the QT interval.
Jessica Jowais   +4 more
wiley   +1 more source

Ketogenic Diet Alleviates Colorectal Cancer by Attenuating Macrophage M2 Polarisation Triggered by Oncometabolite MMA Derived From the Gut Microbiota

open access: yesCell Proliferation, EarlyView.
Proposed mechanism of the ketogenic diet‐microbiota‐MMA‐immune axis in CRC. (Part 1) A ketogenic diet remodels gut microbiota homeostasis by depleting MMA‐producing bacteria, thereby reducing the accumulation of the oncometabolite (MMA). (Part 2) At the molecular level, MMA acts as a ligand that binds to Rap1, activating the downstream MAPK/ERK ...
Yang Lu   +13 more
wiley   +1 more source

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