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The G protein coupled receptor GPR also called
2022-05-27
The G protein-coupled receptor, GPR40 (also called FFAR1) responds to medium and long chain unsaturated fatty acids, resulting in increase of insulin secretion during elevated glucose levels. The glucose dependency of insulin secretion makes this receptor a very good target for developing therapies
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Recently Bristol Myers Squibb and Merck reported their GPR a
2022-05-27
Recently, Bristol-Myers Squibb and Merck reported their GPR40 agonist research focused on the modification of α,β-position of phenylpropionic HQNO mg derivatives. For example, in recent published patent applications, Bristol-Myers Squibb claimed the pyrrolidine and dihydropyrazole GPR40 agonists wit
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Based on the above presumption
2022-05-27
Based on the above presumption, activation of Sox11 and FAK might be beneficial for alleviating the VILI. Previous studies have showed the relevance of Sox11 or FAK up-regulation with improvement of tissue injury. For example, over-expression of Sox11 protected and improved the tissue function or st
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Syt itself does not catalyze lipid mixing and membrane
2022-05-27
Syt1 itself does not catalyze lipid mixing and membrane fusion. Rather, the pairing of vesicular and target membrane SNAREs into complexes serves to pull bilayers together to drive fusion; Ca•syt1 accelerates these fusion reactions so that they occur on rapid timescales in a manner that is precisely
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br Conflict of interest br
2022-05-27
Conflict of interest Author contributions Introduction 2-Quinolones [quinoline-2(1H)-ones], while less prominent than the isomeric 4-quinolones, nevertheless enjoy significant attention as scaffolds in compounds exhibiting a variety of biological activities. These include: 4-aryl-6-chloroqu
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Betahistine N methyl pyridyl ethylamine is a
2022-05-27
Betahistine (N-methyl-2-(2-pyridyl)ethylamine) is a well-known dual H1 AMD-070 agonist/H3 receptor antagonist with structural resemblance to histamine. Though it has been approved long before the discovery of H3R to treat disorders of vestibular function as Menières-Disease, the evidence for this i
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While phosphorylation site motifs are typically described in
2022-05-27
While 4EGI-1 site motifs are typically described in terms of residues that promote phosphorylation, negatively selected residues can also be an important component of substrate recognition. Such ‘forbidden’ resides can act as a filter to prevent phosphorylation of a site by the ‘wrong’ kinase, whic
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br GSK The GSK family is highly conserved
2022-05-27
GSK-3 The GSK-3 family is highly conserved throughout evolution and is encoded by two genes, GSK-3α and GSK-3β, which are located in chromosomes 19q13.2 and 3q13.3 in human, respectively. Both GSK-3α and GSK-3β proteins exist in a variety of tissues with the highest levels found in Biotin-azide
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Our experimental results demonstrated http www apexbt com
2022-05-26
Our experimental results demonstrated marked variability in antioxidant defenses and oxidative damage in Crassostrea gigas between the visceral mass and the gill after the treatments by rifampicin and verapamil through determining the changes of the activity of SOD and POD and MT content. It has bee
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Pyoluteorin Here we report the first attempts to assess role
2022-05-26
Here we report the first attempts to assess roles of NTs and ABC transporters in transfer of ribavirin across the placental barrier using human placental villous fragments and microvillous plasma membrane (MVM) vesicles, in situ dually perfused rat term placenta, and cell-based models. Materials
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br Results and discussion br Conclusion
2022-05-26
Results and discussion Conclusion In conclusion, twenty-one 4-monocyclic aryl-5-carbamoyl-3-isoxazolols have been synthesized and evaluated for their antagonistic activities against housefly and common cutworm GABARs expressed in Xenopus oocytes. The TEVC results indicated that akt inhibitor s
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br The Farnesoid X receptor FXR identification and ligands
2022-05-26
The Farnesoid X receptor (FXR): identification and ligands The Farnesoid X receptor (FXR) belongs to a family of proteins called Nuclear Receptors (NRs). NRs are a class of ligand-activated transcription factors, which transactivate networks of target genes, thereby mediating a wide range of phys
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br Introduction Hepatocyte injury initiates
2022-05-26
Introduction Hepatocyte injury initiates and facilitates inflammation in the course of liver disease progression. Thus, understanding the regulatory basis for sensing and responding to damage-associated inflammatory processes in the liver’s parenchymal cells is a primary issue in liver pathophysi
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More recently Serna Marquez and colleagues investigated
2022-05-26
More recently, Serna-Marquez and colleagues investigated LA-induced migration and invasion of MDA-MB-231 breast cancer cells. In this study, LA was shown to induce AKT-2 phosphorylation and cell invasion and migration in MDA cells. LA-induced cell migration was inhibited by siRNA that selectively ta
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glasdegib br The signal of ferroptosis ROS generated by
2022-05-26
The signal of ferroptosis ROS generated by extracellular or intracellular stimuli play a fundamental role in cell and tissue injury in a variety of disease states [47]. Ferroptosis is generally considered as a type of ROS-dependent regulated necrosis [48]. Intracellular iron accumulation and lipi
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