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br Acknowledgments br Free fatty acids
2022-01-28

Acknowledgments Free fatty acids (FFAs) are not only essential nutritional components, but they also function as signaling molecules. Recently, a G protein-coupled receptor (GPCR) de-orphanizing strategy successfully identified multiple receptors for FFAs, which function on the cell surface and
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EAATs can transport glutamate aspartate cysteic
2022-01-28

EAATs can transport glutamate, aspartate, cysteic acid, and serine-o-sulfate (Bjorn-Yoshimoto and Underhill, 2016). All EAATs work as symporters co-transporting 2 or 3 molecules of Na+ and a proton with each molecule of glutamate (or aspartate). In addition, a K+ ion is counter-transported ending in
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ATN Ac PHSCN NH is a
2022-01-27

ATN-161 (Ac-PHSCN-NH2) is a small peptide antagonist of integrin α5β1, a recently developed anticancer drug that interacts with the N-terminus of the β1 region of integrin α5β1 to lock integrin α5β1 in its non-activated conformation (Wang et al., 2016). The drug has been tested in Phase 2 clinical t
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In tumor cells HK II induction
2022-01-27

In tumor cells HK-II induction is mediated by Akt/mTOR pathway [6], [11]. HK-II dynamically shuttles between the mitochondria and cytoplasm under different metabolic conditions. In cardiomyocytes, Akt enhances HK-II binding to mitochondria, setting the heart at a state resistant to ischemic injury [
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KU-0060648 The study by Pigna and
2022-01-27

The study by Pigna and collaborators provides an elegant demonstration why class IIa HDAC inhibition may not be suitable to protect the neuromuscular function in ALS, consistent with a recent study that showed only a transient protection of motor performance after treatment of the same ALS model wit
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PDEs block GUCY C associated
2022-01-27

PDEs block GUCY2C-associated second messenger signaling by degrading cyclic nucleotides, whereas inhibition of PDEs activity prevents cyclic nucleotide degradation (Fig. 1). Several researchers have described the pathophysiological roles of various PDEs in numerous tumor cell types, including CRC Ad
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The manuscript provides mechanistic insights into the suppre
2022-01-27

The manuscript provides mechanistic insights into the suppression of EGFR, BCRP, PKM2, and other cancer biomarkers in response to pharmacological inhibition of GPR55 with MNF and CID (Fig. 7). Firstly, inactivation of ERK has been previously demonstrated following treatment of PANC-1 PD0332991 Iseth
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br Conclusions Beta cell specific expression in human islets
2022-01-27

Conclusions Beta cell-specific expression in human islets of DGCR2, GBF1, GPR44 and SerpinB10 has not previously been described, although the proteins have partly been characterized in other contexts not related to beta talazoparib or diabetes. DGCR2, GPR44 and SerpinB10 were negative in all oth
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Because of its excellent GPR potency good
2022-01-27

Because of its excellent GPR119 potency, good hERG selectivity and favorable rat t, MK-2461 australia was scaled-up and further profiled. The synthetic protocols described in , were both suitable for a multi-gram scale synthesis of compound . An off-target screen was performed against an extensiv
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Being a facultative intracellular pathogen C
2022-01-27

Being a facultative intracellular pathogen, C. pseudotuberculosis is exposed to oxygen and nitrogen species (ROS and RNS, respectively) reactive environment within macrophages (Nathan and Shiloh, 2000), apart from species endogenously generated by metabolic processes. These molecules interact with D
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Overall ABC transporters are hypothesised to prevent the pen
2022-01-27

Overall, ABC transporters are hypothesised to prevent the penetration of AEDs and other pharmacological compounds into the brain, being a hurdle for therapeutic delivery in neurological diseases. DRE is thought to be in part related to an increased expression of efflux transporters in the BBB, altho
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Glial cells have emerged as
2022-01-27

Glial cells have emerged as important protagonists of the central nervous system (CNS) physiology (Chen and Swanson, 2003; Kettenmann and Verkhratsky, 2008; Parpura and Verkhratsky, 2012). As widely described in the literature, astrocytes regulate glutamatergic synapses by clearance of glutamate in
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In addition to the increase of extracellular glutamate ICH c
2022-01-27

In addition to the increase of extracellular glutamate, ICH can also increase the levels of reactive oxygen species (ROS) and oxidative stress. Although the products of red blood cell lysis and plasma components, as well as the excitotoxic effect of glutamate have been to increase oxidative damage (
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A number of anti diabetic drugs are
2022-01-26

A number of anti-diabetic drugs are available that inhibit α-glucosidase activity, including acarbose, voglibose and miglitol [6,7]. These inhibitors, however, also exhibit undesirable side effects, such as adverse gastrointestinal symptoms and liver toxicity [8,9]. For diabetics, it would therefore
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br Acknowledgements This work was supported by the
2022-01-26

Acknowledgements This work was supported by the National Institutes of Health [grant number GM024417]. Introduction In mammals, glucose is the major energy substrate supporting conceptus development after Minocycline HCl receptor formation [1,2]. While the equine morula uses similar amounts o
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