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br Disp Mediated Hh Membrane Recycling Due to its cholestero
2021-12-10
Disp-Mediated Hh Membrane Recycling Due to its cholesterol modification, Drosophila Hh enriches on sphingolipid-rich apical membranes of polarized epithelial Pirinixic Acid 33., 38., 39.. Genetic studies examining Hh release from wing imaginal disc epithelia suggest that Hh must be endocytosed f
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br Conclusion and future perspectives In the
2021-12-10
Conclusion and future perspectives In the setting of myocardial I/R stress, HDAC activity is induced and contributes to myocardial injury. HDAC inhibition appears to protect the Clarithromycin from I/R injury by activating a variety of pro-survival molecular pathways. From a clinical relevance s
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For the SAR study human haspin kinase
2021-12-09
For the SAR study, human haspin kinase inhibitory activity of the various compounds was evaluated using the same assay utilized for the HTS, except in the presence of varying test compound concentrations. DYRK2 kinase inhibitory activity was measured by P-incorporation into Woodtide peptide substrat
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Administration of a fructose rich diet to normal rats induce
2021-12-09
Administration of a fructose-rich diet to normal rats induces insulin resistance and impaired glucose tolerance or diabetes, depending on treatment duration [23]. We have shown that development of these abnormalities as well as fat deposit in liver, are effectively prevented by co-administration of
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br The bile acid farnesoid
2021-12-09
The “bile acid” farnesoid X receptor (FXR) The Farnesoid X Receptor (FXR) is a ligand-activated nuclear receptor belonging to the Nuclear Receptor superfamily of transcription factors exploiting various crucial functions in mammalian physiology, including reproduction, development and metabolism
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The lack of biological activity
2021-12-09
The lack of biological activity of this family of compounds against T. cruzi is quite unexpected and cannot be attributable simply to the presence of a hydroxyl group at C-1. In fact, either compound 6 or risedronate (5), both bearing a hydroxyl group at C-1, are effective inhibitors of TcFPPS.21, 2
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MK cyclobutylpiperidin yl oxyphenyl methyl trifluoromethyl q
2021-12-09
MK-3134 (3-[4-(1-cyclobutylpiperidin-4-yl)oxyphenyl]-2-methyl-5-(trifluoromethyl)quinazolin-4-one) was synthesized by Merck, as the structurally constrained analogue of MK-0249 (Nagase et al., 2008). This H3R inverse agonist has MW 457.49, seven HBA, and MLogP 4.58, with one violation in terms of dr
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br Intracellular trafficking with concurrent signaling
2021-12-08
Intracellular trafficking with concurrent signaling of NPRA Our recent studies have shown internalization and concurrent signaling of NPRA in subcellular compartments; this had not been previously demonstrated [26,42]. Preparation of the enhanced GFP (eGFP)-tagged NPRA (eGFP-NPRA) construct has g
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Bupivacaine is one of the local anesthetics commonly used in
2021-12-08
Bupivacaine is one of the local anesthetics commonly used in spinal anesthesia. Previous studies had shown that bupivacaine induced neuronal apoptosis and axon degeneration among various neuronal populations in spinal cord, such as sciatic nerves and dorsal root CCG 203971 (DRG) neurons [5], [6], [
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A few research articles described that PLGA could
2021-12-08
A few research articles described that PLGA could alone improve physiological activities in certain illnesses by exerting therapeutic effects. These reported therapeutic activities of PLGA can be appended to the hydrolysis products of PLGA lactate, glycolate, and H+. We will recapitulate their respe
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The inhibition of NSAIDs towards GLOI provides
2021-12-08
The inhibition of NSAIDs towards GLOI provides a direction for the development of novel effective GLOI inhibitors. Although the inhibitory activity of indomethacin was determined and the interactions between it TH588 and GLOI were probed by NMR titration experiments, no detailed inhibitory mechanism
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br STAR Methods br Introduction Glycosylation is
2021-12-08
STAR★Methods Introduction Glycosylation is one of the most prevalent post-translational modifications of proteins. It not only plays major roles in folding, transport and localization of proteins [1], but also regulates various biological processes such as cell growth, viral replication and im
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The vast majority of clinical studies have shown that
2021-12-08
The vast majority of clinical studies have shown that chronic administration of GLP-1R agonists frequently lowers SBP/DBP in diabetic humans, which is consistent with preclinical studies, though the reported reductions are not as potent as those observed in their animal counterparts. In contrast, ac
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br GJs in the brain br Alterations
2021-12-08
GJs in the brain Alterations of GJs in epilepsy The role of GJ blockers and openers in epilepsy As previously known, GJ-mediated electrical coupling plays a role in the generation of highly synchronous electrical activity. The hypersynchronous neuronal activity is a significant feature of c
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Hypertriglyceridemia is associated with an overproduction an
2021-12-08
Hypertriglyceridemia is associated with an overproduction and secretion of triglyceride-rich lipoproteins (TRLs), due to increased liver lipid substrate availability (Adiels et al., 2005, Choi and Ginsberg, 2011), and/or reduced catabolism of TRLs and their remnants, due to reduced lipoprotein lipas
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