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Herein we describe the development of second generation
2021-12-24
Herein, we describe the development of second generation GSM compounds aimed at improving critical physicochemical properties while maintaining the potent activity of the parent AGSM. Ligand design focused on identifying heterocyclic replacements for the hydrophobic D-ring as a means to improve ADME
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Galanin a amino acid peptide was first isolated in
2021-12-24
Galanin, a 29/30-amino-acid peptide, was first isolated in 1983 from porcine intestine by Tatemoto and collaborators [70]. It is widely distributed throughout the central and peripheral nervous systems as well as other tissues. It is involved in a wide range of physiological functions, such as modul
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About of human primary melanomas and of melanoma metastases
2021-12-24
About 67% of human primary melanomas and 56% of melanoma metastases display cytoplasmic or nuclear β-catenin accumulation (Xue et al., 2016). Of note, active β-catenin stimulates emergence of metastasizing melanoma in mice harboring BrafV600E or NrasQ61K hyperplasia (Damsky et al., 2011, Delmas et a
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br Application of TIRFM to
2021-12-24
Application of TIRFM to visualizing exocytosis TIRFM was first used to visualize exocytosis from large secretory granules from chromaffin ABT 702 dihydrochloride receptor (Steyer et al., 1997). Before that, visualization of secretory organelle was strictly limited to a few exceptions, such as mas
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br Methods br Results br Discussion The aim
2021-12-24
Methods Results Discussion The aim of this study was to investigate whether serum lectin-binding activity is associated with development of HCC in HCV-positive individuals. Using ELISA-based assays of lectin-binding activity, we demonstrated that both age and gender influence the circulatin
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Under most circumstances NO is
2021-12-24
Under most circumstances, NO is a potent endogenous vasodilator. Therefore, its involvement in an endothelium-dependent contraction seems paradoxical, to say the least. Soluble guanylyl cyclase (sGC) is the major downstream target of NO; its inhibition results in the lack of vasoconstrictor response
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GSTP catalyzed reduction of Prdx enhances its peroxidase act
2021-12-24
GSTP1-1 catalyzed reduction of Prdx6 enhances its peroxidase activity. Using standard NADPH/GR/GSH-coupled assays we used cell lysates from the transiently transfected leukotriene to measure the influence of GSTP1 allelic variation on peroxidase activity. Specificity for detection of Prdx6 activity
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br FFA GPR was deorphanised as the second receptor
2021-12-24
FFA4 GPR120 was deorphanised as the second receptor for long-chain fatty acids in 2005 [5]. Initial focus highlighted expression in the lower gut, the capacity of unsaturated fatty acids to promote release of the incretin glucagon-like peptide-1 (GLP-1) from the enteroendocrine cell line STC-1, a
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protein kinase inhibitor Generally speaking the regulation o
2021-12-24
Generally speaking, the regulation of GnIH on gonadotropins synthesis and release, although controversial, could be direct and/or indirect via GnRH, among others peptides. In this sense, different scenarios have been reported in vertebrates. In mammalian and avian species, GnIH fibers reach the medi
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Recent research reveals that human alkyladenine
2021-12-24
Recent research reveals that human alkyladenine DNA glycosylase (hAAG) is an important protein enzyme which can specifically recognize and excise a variety of alkylated purines and deoxyinosine from DNA [12]. hAAG plays pivotal roles in maintaining genomic integrity, and it is involved in 1-Oleoyl l
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br Dysregulation of glutamate transporter expression and fun
2021-12-24
Dysregulation of glutamate transporter expression and function Aberrant glutamate transporter function and expression are associated with various neurological disorders. Therefore, understanding the underlying mechanisms of EAAT1/2 expression may provide therapeutic targets for treating neurologi
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Introduction Glucose is the most important energy carrier of
2021-12-24
Introduction Glucose is the most important energy carrier of the brain. Glucose transporter type 1 (Glut1) is located at the blood–brain barrier and assures the energy-independent, facilitative transport of glucose into the brain [1]. Twelve transmembrane segments of the protein and an intracellula
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UNC 3230 Although it is well documented that FAAH
2021-12-23
Although it is well documented that FAAH substrates can elicit analgesic effects [for review see [47,48] and that systemic poly I:C administration induces mechanical allodynia in rats [14], to our knowledge this is the first study to demonstrate that enhancing FAAH substrate levels can modulate TLR3
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Similar to Rac Cdc and RhoA
2021-12-23
Similar to Rac1, Cdc42, and RhoA, expression of Rnd3 is also increased under hypoxic conditions, involving Hif1α mediated transcriptional activity. Here, downregulation of Rnd3 abolishes hypoxia-induced cell migration via a mechanism involving the chemokine receptor C-X-C motif chemokine receptor 4
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br Conclusion GST expression was detected in
2021-12-23
Conclusion GST expression was detected in the Hemicornea construct and the commonly used animal cornea models at both the protein and functional levels. The results are summarized in Table 1. However, the construct exhibited lower levels of activity of GST, a marker of phase II enzymatic activity
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