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Transporters are important ta http
2022-06-13

Transporters are important targets for devising new therapies, optimizing existing therapies, and helping understand the toxicities of certain drugs. Given the well-documented role of transporters in restricting the distribution of drugs, modulating the relevant transporters could enhance the permea
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By regulation of synaptic glutamate concentration
2022-06-13

By regulation of synaptic glutamate concentration, glutamate transporters play an important role in limiting glutamate signaling and controlling the activation of glutamate receptors (Rimmele and Rosenberg, 2016). Reduced glutamate transport is thought to underlie the pathogenesis of numerous neurol
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Here we reported series of carbohydrate modified compounds c
2022-06-13

Here, we reported series of carbohydrate-modified compounds containing a dibromo substituted benzene ring which was derived from the red alga (). The conformation flexibility of Alda 1 and their polyol structures give them many unique biological properties as we have described earlier. More intere
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Piezo channels can be activated by
2022-06-13

Piezo channels can be activated by many mechanical stimuli . While some of these stimulations directly mimic physiological forces experienced by Imeglimin , such as shear stress applied in a microfluidic chamber, the most commonly used modes of stimulation consist of stretching the membrane by app
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To ensure the induction of CYP enzymes by several
2022-06-10

To ensure the induction of CYP enzymes by several inducers, specific monooxygenase activities of variously induced, uninduced and pooled liver microsomes were compared (Fig. 3). Although 3-MC, phenobarbital, acetone, and dexamethasone could induce CYP1A-, CYP2B-, CYP2E1-, and CYP3A-selective enzyme
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Based on the previous report that FXR
2022-06-10

Based on the previous report that FXR regulated PEPCK indirectly [20], we speculated that FXR may regulate gluconeogenesis by regulating some key transcription factors associated with gluconeogenesis. Finally, by using HS218 as a probe, we found that FXR binds to PGC-1α promoter and directly regulat
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Histamine Phosphate Despite their undisputed importance howe
2022-06-10

Despite their undisputed importance, however, FPR receptors are not in the limelight of GPCR-related research (for review [12] and references therein). We, therefore, draw attention to this GPCR receptor family, in order to re-initiate FPR-related research, particularly in the light of biased agonis
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Tail group SAR of the imidazole derived analogs
2022-06-10

Tail group SAR of the imidazole derived analogs is shown in . The previous SAR study from the discovery of AMG 837 revealed that a simple un-substituted meta-biphenyl tail group was less favorable in terms of potency. Efforts to introduce polarity to the tail group were not successful. When a methy
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br STAR Methods br Introduction Arsenite is a
2022-06-10

STAR★Methods Introduction Arsenite is a well-recognized toxic metalloid that commonly presents in the natural environment. Chronic exposure to arsenite can lead to a wide range of adverse health effects to human, including cancers, cardiovascular diseases, diabetes, skin lesion and neurodegene
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DAMPs are endogenous danger signals that can
2022-06-10

DAMPs are endogenous danger signals that can initiate and perpetuate a noninfectious Clindamycin HCl during cell death [23]. HMGB1 is a well-studied nuclear DAMP in various types of regulated necrosis and has been implicated in the pathogenesis of infection and sterile inflammation. Our current dat
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br Materials and methods br Results br Discussion
2022-06-10

Materials and methods Results Discussion ERK5 signaling and its regulation has gained focus in recent years specially in the subject of cardiovascular biology, where this kinase plays a key role in angiogenesis and maintenance of blood vessel integrity [18,20,34,35]. The signaling pathways
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br Introduction Thrombosis is one of the leading
2022-06-10

Introduction Thrombosis is one of the leading causes of deaths in the cardiovascular diseases such as myocardial infarction (MI), unstable N-3-oxo-dodecanoyl-L-Homoserine lactone and acute coronary syndrome (ACS) in developed countries [1], [2]. It is estimated that venous thromboembolism (VTE)
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FXa is a vitamin K dependent serine
2022-06-10

FXa is a vitamin K-dependent serine protease consisting of two chains linked by a disulfide bridge. The heavy chain contains 303 Daptomycin and the light chain has 139 amino acids. The catalytic triad comprised of Ser195, His57, and Asp102 exhibits the trypsin-like β-barrel structure [12]. The acti
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br What are the local exocytotic protein targets of
2022-06-10

What are the local exocytotic protein targets of PKC? A direct method for PKC to potentiate insulin release would be to phosphorylate and activate components of the exocytotic machinery. Bulk measurements show that potentiation occurs by enhancement of the calcium sensitivity of exocytosis [56],
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87114 synthesis br Conclusions and perspectives br
2022-06-10

Conclusions and perspectives Acknowledgements This work was supported by the National Natural Science Foundation of China (Grant Nos. 21802173, 21405182 and 21773315), the Natural Science Foundation of Guangdong Province (Grant Nos. 2018A030310301, 201710010019 and 2014A030313232, 201804020025
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