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Recent findings of us suggest that compounds
2022-04-01
Recent findings of us suggest that compounds that inhibit both FAAH and TRPV1 may be more efficacious in pain relief than those targeting only one such protein. As continuation of our efforts to identify new molecules able to target simultaneously both FAAH and TRPV1 receptors, we hypothesized that
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br Results br Discussion In this
2022-04-01
Results Discussion In this study, six new T30695 variants were synthesized with the acyclic R or S glycerol linker instead of 795 unit at 4, 8 or 12 T residue. Based on our previous studies on TBA-GQ, this type of modification should provoke local changes in GQ conformations in the final T3069
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Consistent with a similar study
2022-04-01
Consistent with a similar study, we found economic status to be very important to domestic funding of HIV. Upper-middle-income and high-income countries are more likely to have fiscal space for health and be less reliant on external sources. Moreover, richer countries often attract larger cofinancin
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The rationale for developing HDACi as anticancer
2022-03-31
The rationale for developing HDACi as anticancer agents was based on their ability to induce the hyperacetylation of histones and nonhistone proteins, resulting in increased differentiation, apoptosis, and Temozolomide arrest of cancer cells 1, 2, 3. HDACi have been used in the treatment of hematolo
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br Experimental br Acknowledgment br Introduction Hepatitis
2022-03-31
Experimental Acknowledgment Introduction Hepatitis C virus (HCV) belongs to Flaviviridae, is a blood-borne pathogen which infects about 180 million individuals throughout the world; most of the cases lead to end stage liver diseases, fibrosis, cirrhosis and hepatocellular carcinoma (Choo et
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topotecan Elevated methylglyoxal levels also contribute to
2022-03-31
Elevated methylglyoxal levels also contribute to carbonyl stress, cytotoxicity, DNA damage, apoptosis and cell death. These mechanisms may be important for normal aging of the nervous system as well as for the development of neurodegenerative diseases such as Alzheimer's and Parkinson's disease wher
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Cortisol is a natural glucocorticoid hormone produced by the
2022-03-31
Cortisol is a natural glucocorticoid hormone produced by the adrenal cortex. Its secretion is stimulated by the sympathetic nervous system, and its main function is to mobilize energy to protect the homeostasis of vital biochemical processes during physical and psychological stress [14]. Chronic lev
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Nanaomycin A To help resolve the question of simple binding
2022-03-31
To help resolve the question of simple binding versus transport, we reasoned that if quercetin is transported by GLUT1, we should be able to block its uptake by other GLUT1 inhibitors. We initially investigated the effects of two newly identified GLUT1 inhibitors, BAY-876 and WZB-117. WZB-117 was fi
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br Acknowledgments This work was supported by a grant CIHR
2022-03-31
Acknowledgments This work was supported by a grant CIHR-NSFC China-Canada Joint Health Research from the National Science Foundation of China (Grant Number 81061120525) and the Canadian Institutes for Health Research (Grant number CCI-109605). The authors thank two anonymous reviewers for helpful
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With the exception of R none of
2022-03-30
With the exception of R5.40310, none of the other residues would appear to be in a position to mediate direct agonist interactions in the active state GLP-1R structures. ECL2 within the GLP-1R is important for affinity and efficacy of both extended and processed GLP-1 peptides [24]. Though distal fr
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Though regulation of ghrelin interaction with GHSR has not b
2022-03-30
Though regulation of ghrelin interaction with GHSR has not been described previously, a precedent for a similar regulatory mechanism exists in the form of the interaction between Agouti-Related Protein (AgRP) and melanocortin receptor subtypes MC3R and MC4R (Ollmann, 1997). AgRP is produced by hypot
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Introduction br Channel activity Since initial reports of
2022-03-30
Introduction Channel activity Since initial reports of the Ca2+-activated K+ permeability of erythrocytes (see Gardos, 1958), several ‘criteria’ have been established to certify K+ fluxes as being due to the Gárdos channel. For example, the requirement for Ca2+ at the intracellular face of the c
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pkc inhibitor Also a large number of small molecules are
2022-03-30
Also a large number of small molecules are potent G-quadruplex ligands that exhibit anti-proliferative activity in cells [39,48]. Several small molecules, for example cyclic naphthalene diimide derivative [43], cationic porphyrins [2,[49], [50], [51], [52]] and pentaheteroaryls [53], quinacridines [
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br FXR FGF in the control of
2022-03-30
FXR–FGF15/19 in the control of BAs synthesis The nuclear receptor FXR is the master regulator of BAs homeostasis, modulating their synthesis, GANT61 and uptake [15]. FXR decreases BA de novo hepatic biosynthesis by reducing the expression of CYP7A1. At the canalicular membrane, newly-synthesized
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Emerging evidence has shown that
2022-03-30
Emerging evidence has shown that pharmacological FXR agonism attenuates chronic alcohol treatment-induced liver injury and steatosis [18], [19], while whole-body FXR knockout worsens alcohol-induced liver injury [19]. This suggests that FXR plays an important role in ALD development. However, defici
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