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P Benzoxaborole substituted macrocyclic compounds based on I
2021-11-06

P4-Benzoxaborole-substituted macrocyclic compounds based on ITMN-191 scaffold were prepared using a general scheme as shown in . ITMN-191 was prepared by following a patent procedure. The P4 BOC group was removed by treatment with TFA in dichloromethane to give amine . The coupling of the amine to 6
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The discovery that the physiological functions
2021-11-05

The discovery that the physiological functions of LPI are associated with the activation of specific GPR55 membrane receptor [4] has launched a new era of research on this lysophospholipid. However, the activation of membrane receptors by lysophospholipids is extremely complex due to the multitude o
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In order to consolidate our genetic funding we performed sev
2021-11-05

In order to consolidate our genetic funding, we performed several in silico analysis regarding the p.R85W mutation. The high conservation of R85 residue in all species suggests that it has an important role in glucokinase function. Pathogenic effect of the p.R85W is supported by in silico prediction
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The effect of GCK NES mutations on enzyme kinetics
2021-11-05

The effect of GCK-NES mutations on enzyme kinetics and protein stability might account for the hyperglycaemia that characterizes MODY2 patients, since reduced GCK activity would increase the threshold for glucose stimulated insulin release in beta-cells [31,37,49]. However, a more in depth functiona
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In conclusion enhanced glucagon action of the
2021-11-05

In conclusion, enhanced glucagon action of the beta cell results in improved beta cell function after glucose stimulation, but simultaneously dissociated responses to both glucose-dependent and non-glucose secretagogues evolve. This shows that the glucagon receptor is complexly involved in beta cell
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br Discussion According to the generally accepted notion whi
2021-11-05

Discussion According to the generally accepted notion which originated from the study of ATP-depleted Butyrolactone 3 the changes in Ca2+ homeostasis induced by ATP depletion and leading to the activation of the Gárdos effect are due to the inhibition of Ca2+ pumping, and the subsequent entry of
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GSIs were shown to effectively
2021-11-05

GSIs were shown to effectively decrease Aβ levels at doses close to or higher than their IC50 values in cell culture models. Surprisingly, they also slightly increase Aβ levels at low doses, (significantly below the IC50) also known as “Aβ rise”, due to various mechanisms including inhibition of cel
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br Acknowledgements br Introduction Galanin
2021-11-05

Acknowledgements Introduction Galanin shows widespread distribution in the central nervous system (CNS) and peripheral nervous system (PNS) as well as in the immune, endocrine and endothelial vascular systems (Lang et al., 2007). Galanin controls diverse physiological processes such as arousal
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Here we investigated on epigenetic regulatory mechanisms of
2021-11-05

Here, we investigated on epigenetic regulatory mechanisms of ALX/FPR2 expression. Epigenetic changes, that include phosphorylation, acetylation, methylation and ubiquitination of DNA and histone proteins, occur in a variety of diseases [21] and are being recognized as key targets for personalized me
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br STAR Methods br Introduction Arsenite is
2021-11-05

STAR★Methods Introduction Arsenite is a well-recognized toxic metalloid that commonly presents in the natural environment. Chronic exposure to arsenite can lead to a wide range of adverse health effects to human, including cancers, cardiovascular diseases, diabetes, skin lesion and neurodegene
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br Acknowledgments We apologize for
2021-11-05

Acknowledgments We apologize for the omission of primary citations owing to space limitations. This work was supported by grants from National Natural Science Foundation of China (81772801 and 81472455 to C.D.), the Key Program of Zhejiang Provincial Natural Science Foundation (LZ17H160002 to C.D
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Management of HIV treatment with HIV
2021-11-05

Management of HIV-1 treatment with HIV PIs can be complicated due to wide inter-patient variability in Rosiglitazone levels. In certain scenarios, therapeutic drug monitoring (TDM) has been recommended as a useful approach to individualize therapy for HIV-infected patients [[9], [10], [11], [12]].
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Histamine receptors were largely linked with
2021-11-05

Histamine receptors were largely linked with allergic and inflammatory reactions before the recognition of the histamine H3R in 1983 that proved its function as auto- as well as heteroreceptor at pre- and postsynaptic membranes and demonstrated its intense regulating influence on release of numerous
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Histamine functions as a key neurotransmitter in multiple
2021-11-05

Histamine functions as a key neurotransmitter in multiple circuits to control various behaviors. In Drosophila photoreceptor, histamine is produced de novo by histidine decarboxylase (Burg et al., 1993); meanwhile, maintaining normal histamine content also depends on the histamine recycling pathway
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br Autophagy and HBV induced HCC Researchers have
2021-11-04

Autophagy and HBV-induced HCC Researchers have demonstrated downregulation of autophagy in HBV transgenic liver tumors of mouse models and in human HBV-induced HCC specimens. Kotsafti and his colleagues declared that the expression level of BECN1 mRNA in HCC specimens was considerably lower than
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