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The co crystal structure of
2025-01-04
The co-crystal structure of ()-blebbistatin ()- bound to myosin II (PDB: ) was used to scout for possible favorable interactions with the residues lining the binding pocket. Looking at A, we hypothesized that -oriented hydrophilic moieties (e.g. hydroxymethyl) on C of the blebbistatin scaffold might
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There are profound differences between acute and
2025-01-04
There are profound differences between acute and chronic pain when dramatic changes occur in peripheral nociceptors and central nociceptive pathways and the pain system is sensitised thereby leading to exaggerated responses to noxious stimuli (hyperalgesia) and responses to non-noxious stimuli (allo
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br Acknowledgments br Introduction Hypospadias is a common
2024-12-31
Acknowledgments Introduction Hypospadias is a common congenital malformation in males, in which the urethral orifice is found on the ventral side of the penis as a result of incomplete fusion of urethral folds. The mean prevalence in per 10,000 live births from 1910 to 2013 were: Europe 19.9,
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mek inhibitors The molecular mechanisms that mediate the pla
2024-12-30
The molecular mechanisms that mediate the plasticity of the NMJ are not well understood. PGC-1α is a master regulator of the NMJ gene expression program 23, 24, and thus AMPK might indirectly regulate the NMJ via its broad influence on the coactivator. Cerveró et al.[6] recently provided more direct
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Sixth significant progress has been
2024-12-30
Sixth, significant progress has been made during the last few years regarding the molecular mechanisms underlying the activation of AMPK and this should aid to develop more potent and specific compounds. Information from crystallographic structures combined with computer-based drug design hold promi
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These findings suggest that eventually more
2024-12-30
These findings suggest that eventually more than one 12/15-lipoxygenase isoform may play a role in human atherosclerosis. Humans have two 12-lipoxygenases and two 15-lipoxygenases which show different expression patterns, substrate specificities and stereo-selective metabolism [1]. However, in Isoch
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br Materials and methods br Results br Discussion
2024-12-30
Materials and methods Results Discussion Intracellular metabolic pathways of sugar, such as glycolysis and TCA cycle, provide material and energy for the synthesis of other substances, including amino acids. Thus, the content of sugars and their metabolic pathways are important for amino Ba
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AAT enzyme activity was readily detected in crude cell free
2024-12-30
AAT enzyme activity was readily detected in crude cell-free extracts obtained from berry tissues of all accessions but displayed different substrate selectivities (Fig. 2). Cell-free extracts derived from ‘Muscat Hamburg’ berries showed the highest AAT activity with all alcoholic substrates tested,
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br Introduction There are greater than five million American
2024-12-30
Introduction There are greater than five million Americans living with Alzheimer's dementia and more than 35 million people worldwide [1], and without a way to stop or slow the progression, there will be nearly a tripling of individuals affected by 2050 (13.8 million) [1]. The urgency to develop
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The macrophage is the major cell type responsible for choles
2024-12-30
The macrophage is the major cell type responsible for cholesterol uptake and metabolism associated with the initiation and progression of atherosclerosis in focal areas of the arterial subendothelial space. In advanced atherosclerotic lesions of cardiovascular disease, cholesterol-induced macrophage
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Active SI behavior was dose dependently affected by
2024-12-30
Active SI behavior was dose-dependently affected by PACAP treatment (F3,25 = 14.42, p affected gfp mrna 1 week later (F3,20 = 8.93, p in the time to complete the task (F4,76 = 3.53, p hypothesis that PACAP causes disruptions in posterror adjustments that are similar to disruptions seen in humans wi
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br Functional consequences of ADK regulation on astrocyte fu
2024-12-30
Functional consequences of ADK regulation on astrocyte function As outlined above (see introduction), ADK critically regulates the extracellular adenosine levels in Danazol (Boison, 2006, Etherington et al., 2009). Changes in the levels of adenosine, as a result of the regulation of ADK expressi
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A high throughput small molecule ACK
2024-12-30
A high-throughput small molecule ACK1 biochemical inhibition screen was performed in-house and led to the identification of 1μM inhibitor furanopyrimidine (). Further binding studies found porcine receptor to be both ATP-competitive and reversible. Early structure-activity relationship (SAR) work
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br Experimental section br Conflicts of
2024-12-30
Experimental section Conflicts of interest Acknowledgments This work was partly supported by INSA-Rouen, Rouen University, CNRS, Labex SynOrg (ANR-11-LABX-0029), Région Haute-Normandie. Introduction A key component of the integrated management of key pests such as codling moth (Cydia po
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4-IPP receptor Bioactive peptides contain amino acids
2024-12-30
Bioactive peptides contain 2–20 amino acids with possible bioactivities including antihypertensive, antioxidant, antimicrobial, anticancer, and opioid activity [9], [10], [11]. There has been a great interest in antihypertensive peptides for their efficiency in lowering blood pressure. The antihyper