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The second approach to optimizing microsomal stability in
2022-05-12

The second approach to optimizing microsomal stability in this series involved the strategic positioning of steric bulk along the tether as a means of encumbering the access of oxidative enzymes to the methylene bridge. This approach has been employed in other P2-P4 macrocyclic inhibitors of NS3/4A
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Of special interest is that riociguat and NO donors decrease
2022-05-12

Of special interest is that riociguat and NO donors decreased the phosphorylation of many proteins in human platelets. This aspect is presently under further investigation but a few comments can be made already here. Of the extensive spectrum and diversity of human protein kinases and protein phosph
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Oxaliplatin br Materials and methods br Results br Discussio
2022-05-12

Materials and methods Results Discussion Recently, we characterized the interaction of the PH domains of various Lbc family RhoGEFs with the activated small GTPase, RhoA, and demonstrated that this could serve as a positive feedback mechanism for robust activation of RhoA (Medina et al., 20
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br Introduction Atherosclerosis is a
2022-05-12

Introduction Atherosclerosis is a chronic inflammatory disease characterized by lipid and leukocyte accumulation within the arterial wall. Homocysteine (Hcy) is a thiol-containing amino HBC derivative derived from the metabolism of dietary methionine. Epidemiological studies have shown that elev
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br AUTHOR CONTRIBUTIONS br ACKNOWLEDGMENTS br
2022-05-11

AUTHOR CONTRIBUTIONS ACKNOWLEDGMENTS Introduction Chronic neuropathic pain is a common symptom in patients with human immunodeficiency virus (HIV)-1 infection. Glycoprotein 120 (gp120) is an HIV-1 protein that can cause pain behaviors in animal models (Hao, 2013, Nasirinezhad et al., 2015,
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To further explain the energy differences between Group A
2022-05-11

. To further explain the energy differences between Group-A and Group-B, the average distances between ligands and the zinc cation were obtained from the last 1ns trajectory. It turns out that the members of group A were within the coordination distance of the zinc ion, whereas those of group B stay
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br Experimental procedure br Acknowledgments This research w
2022-05-11

Experimental procedure Acknowledgments This research was supported by funds provided by NIH/NIAAA grant P01 AA020683 and the Waggoner Center for Alcohol and Addiction Research. Introduction Acute mesenteric ischemia (AMI) is still associated with a high mortality rate, and currently, an ea
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Several reports have shown that the ICD
2022-05-11

Several reports have shown that the ICD of CLRs is involved in the desensitization process of this superfamily. The analysis of our chimeric constructs between GlyRα1 and GLIC revealed differences in desensitization properties. In contrast, other ion channel properties such as channel block and ion
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GlyRs are members of the superfamily
2022-05-11

GlyRs are members of the superfamily of Cys-loop receptors (CLRs) [3]. They form postsynaptic pentameric receptor complexes of α1 and β subunits anchored via the scaffolding protein gephyrin [4]. GlyRs are composed of several domains with the large N-terminal extracellular domain (ECD) important for
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br Acknowledgements We thank LetPub www
2022-05-11

Acknowledgements We thank LetPub (www.letpub.com) for its linguistic assistance during the preparation of this manuscript. This work was funded by National Natural Science Foundation of Beijing (No. 7122187), and Special fund for clinical research of Chinese Medical Association (No. 13040700455).
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In order to discover novel small molecule compounds with the
2022-05-11

In order to discover novel small-molecule compounds with the activity of GLUT4 translocation, we conducted a cell-based phenotype screening in L6-GLUT4-myc myoblasts by measuring appearance of GLUT4 on the plasma membrane (GLUT4 translocation activity). Evaluation of total 183,400 compounds gave sev
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br Methods br Results br Discussion Among three main signali
2022-05-11

Methods Results Discussion Among three main signaling pathways activated by bFGF, the MAPK pathway was found to be involved in the upregulation of GR levels. So far, there have been a few candidates that could connect activated ERK to the upregulation of GR. One likely candidate is the zinc
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br Conclusions We have shown that despite the development of
2022-05-11

Conclusions We have shown that despite the development of severe insulin intolerance and marked alterations in whole body substrate oxidation that Gcgr−/− mice are protected against olanzapine-induced hyperglycemia. Our data provides evidence that this protective effect is likely due in large par
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The HH Gli pathway has been demonstrated
2022-05-11

The HH-Gli pathway has been demonstrated to play an extensive role in skeletal development. India Hedgehog, derived from hypertrophic chondrocytes, and Parathyroid Hormone-like related Protein (PTHrP), derived from peri-articular chondrocytes, form a negative feedback loop to inhibit chondrocyte hyp
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Previous researches about ghrelin focused primarily on
2022-05-11

Previous researches about ghrelin focused primarily on gastrointestinal functions [30], energy balance [31], weight [32], and more recently on anxiety [33], [34], [35] and depression [36]. Here, we provided the first demonstration that chronic peripheral or central ghrelin treatment to CUMS rodents
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