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Therapeutic options targeting intrahepatic resistance are ve
2021-01-20

Therapeutic options targeting intrahepatic resistance are very limited. Theoretically, the NO-cGMP pathway may be influenced at several sites. Yet, most strategies did not reach clinical practice or yielded disappointing results, such as activators of soluble guanylate cyclase [14], NO releasing der
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The reaction of chitosan with DVS should take
2021-01-20

The reaction of chitosan with DVS should take place primarily through a nucleophilic attack of the vinyl sulfone groups to the amino groups in chitosan [39,50], although its hydroxyl groups can also be involved, as it happens when using agarose [35]. These reactions create very stable secondary amin
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Fmoc-Gly-OPfp receptor A robust meta analysis of randomized
2021-01-20

A robust meta-analysis of 22 randomized clinical trials found that application of ischemic preconditioning strategies reduce ventricular arrhythmias [3]. Additionally, it was demonstrated that remote ischemic perconditioning (perRIC) induces immediate cardioprotection during ongoing ischemia by atte
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Since the initial identification of DNA ligase inhibitors by
2021-01-19

Since the initial identification of DNA ligase inhibitors by a structure-based approach [[18], [26]], there have been several reports describing LigI inhibitors using computer modelling and derivatives of the original DNA ligase inhibitors [[49], [50], [51]]. While these studies have shown that the
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br Materials and methods br
2021-01-19

Materials and methods Results Because of the specific binding of DGKε to an arachidonoyl group, there was a particular interest to evaluate the behavior of 2-AG with this isoform of DGK. The substrate specificity and kinetic constants for DGKε has been recently reported [13]. Using the preferr
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br Conclusion The present work
2021-01-19

Conclusion The present work describes the synthesis of 18 naphthoquinonolyl-1,2,3-triazole compounds based on natural product modification with antiplasmodial activity. Lapachol derivatives disclosed higher activity than the natural product. Six of these final modified lapachol 1,2,3-triazole com
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Primary human GBM neurospheres expressed high levels of the
2021-01-19

Primary human GBM neurospheres expressed high levels of the metabolic enzyme fatty acyl-CoA synthetase VL3 (ACSVL3) that were associated with CSCs self-renewal and tumorigenic capacity. ACSVL3 knockdown significantly decreased ALDH levels, indicating its contribution to cell metabolism and maintenan
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br Results br Discussion GPCRs recognize a
2021-01-19

Results Discussion GPCRs recognize a broad range of molecules with a vast chemical ret pathway through different mechanisms. Our understanding of the recognition of lipid mediators by GPCRs primarily comes from the structural studies of receptors for lysophospholipids and endocannabinoids inc
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The pyrrolo benzodiazepines PBDs are a family
2021-01-19

The pyrrolo[2,1-][1,4]benzodiazepines (PBDs) are a family of antitumour antibiotics that includes the natural products anthramycin and DC-81. They exert their cytotoxicity by covalently bonding to the exocyclic C2–NH group of guanine residues in the minor groove of DNA through their N10–C11 imine fu
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An increased CK activity was
2021-01-19

An increased CK2 activity was found in septal neuronal Cy3 azide dissected from rat embryos after hypoglycemia [36]. These data indicated that CK2 activity is not only regulated by insulin but also by the glucose concentration. One essential step in insulin action is the binding of the hormone to
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Cell swelling stimulates the release of certain amino
2021-01-19

Cell swelling stimulates the release of certain amino acids, in particular the non-protein amino WP 1130 receptor taurine, via a pathway which has the characteristics of a channel rather than a carrier [54], [69]. Indeed, on the basis of pharmacological inhibition, it was suggested that volume-activ
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As plants can only take
2021-01-19

As plants can only take up P in an inorganic orthophosphate form, it was expected that the proportion of orthophosphate P in the OA would be a good indication of the availability of the P in the OA. While the P speciation of the COMP sample could not be determined by deconvolution due to the broadne
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br Introduction Ewing s sarcoma ES is a mesenchymal
2021-01-19

Introduction Ewing’s sarcoma (ES) is a mesenchymal tumor characterized by small, round, blue cells, and is poorly differentiated and highly malignant [1]. While ES typically arises in bone and soft tissue, rare primary extraosseous manifestations of ES have been reported throughout the body [2].
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Cantharidin is a natural element extracted from blister beet
2021-01-19

Cantharidin is a natural element extracted from blister beetles, and has been proven to be effective in cancer [16]. NCTD, the demethylated analog of cantharidin, has been synthesized and been shown to have an equal anti-cancer effect with fewer side effects than cantharidin [39]. It was confirmed t
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For most enolases fluoride acts as
2021-01-19

For most enolases, fluoride acts as an inhibitor, while Mg2+ is the most important metal activator. In yeast systems, metal cations and fluoride bind to enolase at the active center of the enzyme, forming a complex. The complex blocks the binding of substrates to the enzyme in yeast systems, thereby
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