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The Ala to Leu substitution
2021-11-10

The Ala116 to Leu110 substitution would reduce the size of the active-site cavity disfavoring the production of longer allylic compounds as a result of steric hindrance, according to the observations of Poulter and co-workers [29], [30]. However, this explanation appears to be unlikely since several
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In enzyme assays it is convenient to
2021-11-10

In enzyme assays, it is convenient to quantify the product formed in the enzyme reaction, where a decrease in the concentration of product indicates enzyme inhibition [35], [36], [37], [38]. In the present study, substrates were carefully chosen so that they are specific to each enzyme. Known natura
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Recent studies are beginning to explore this complex interpl
2021-11-10

Recent studies are beginning to explore this complex interplay of pathways. For example, intracellular trafficking of poly(lactic-co-glycolic acid)(PLGA) based nanoparticles was studied in detail using 30 different Rab proteins as markers for intracellular transport vesicles (involved in exocytosis,
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br Acknowledgments This study was financially supported by N
2021-11-10

Acknowledgments This study was financially supported by National Science Center Poland grant No DEC-2011/02/A/NZ4/00031 (KKK), Jagiellonian University Medical College (Poland) grants: K/ZDS/007130 (SM) and K/ZDS/007131 (SM), COST Action CA15135 (DŁ, HS, KKK) and DFG INST 208/664-1 FUGG (HS). Than
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Based on the role of NMDA receptors in initiation and
2021-11-09

Based on the role of NMDA receptors in initiation and propagation of epileptic seizures and on potentiation of NMDA function by glycine, it has been hypothesized that glycine will have proconvulsant activity (Foster and Kemp, 1989). Indeed, there is some evidence that human epileptogenic foci, remov
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Diabetes induced damage results in peripheral nerve
2021-11-09

Diabetes-induced damage results in peripheral nerve pathology that 77 receptor correlates with clinical signs and symptoms. Nerve injury that results in structural changes can be measured through clinical neurological assessment, quantitative sensory testing, nerve conduction studies, and periphera
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br Materials and methods br Results and discussion br Conclu
2021-11-09

Materials and methods Results and discussion Conclusions In summary, the Au@SiO2 based lateral flow sandwich immunoassay for fast detection of EBN-specific glycoprotein has been firstly established by using nanocomposites as signaling-labels and synthesized EBN-specific G007-LK as recogniti
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In addition to the increase of
2021-11-09

In addition to the increase of extracellular glutamate, ICH can also increase the levels of reactive oxygen species (ROS) and oxidative stress. Although the products of red blood cell lysis and plasma components, as well as the excitotoxic effect of glutamate have been to increase oxidative damage (
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To maintain low Glu concentrations in the synaptic
2021-11-09

To maintain low Glu concentrations in the synaptic cleft below the affinity of its receptors, this amino 3'-O-(2-nitrobenzyl)-2'-dATP is rapidly removed from the extracellular space by a family of sodium-dependent high-affinity transport systems located mainly in the plasma membrane of perisynaptic
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cpmt mg br Introduction Glucokinase GCK hexokinase IV is a m
2021-11-09

Introduction Glucokinase (GCK, hexokinase IV) is a monomeric enzyme that catalyzes the ATP-dependent conversion of glucose to glucose 6-phosphate, the first and rate-limiting step of glycolysis in the liver and pancreas [1,2]. GCK was first discovered in the early 1960's, and shortly thereafter i
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The effect of the selected compounds on NF kB
2021-11-09

The effect of the selected compounds on NF-kB transrepression was assessed using the well-studied HeLa B2 cell line that expresses endogenous GR and NF-kB family members and responds properly to glucocorticoids and pro-inflammatory cytokines (such as TNF). Our data revealed that the two hit compound
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As glucagon stimulated hepatic glucose
2021-11-09

As glucagon-stimulated hepatic Cy5 EGFP production is a key component of the normal response to hypoglycemia, the potential of a GCGr antagonist to delay or prevent recovery from a hypoglycemic state is a critical safety issue that must be addressed. Studies of the effects on time to recovery from
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In sharp contrast to these genetically
2021-11-09

In sharp contrast to these genetically altered animals, there are two types of living fish that appear to lack Band 3 in their red blood cells. These are the Lamprey [45] and the Hagfish [46,47]. While these fish normally occupy their respective niches, the presumed compensatory mechanisms, as with
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Hydantoin in region F bridging the phenoxybenzene
2021-11-09

Hydantoin in region F bridging the phenoxybenzene and benzimidazole moieties was replaced by cyclic building blocks, diketopiperazine (25) and imidazolidinone (26), and linear bonds, amide (27) and urea (28). Analogs 25–28 possessing the linkers other than hydantoin were not tolerated in LBD of FXR,
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In terms of cytotoxicity studies under two dimensional
2021-11-09

In terms of cytotoxicity studies under two-dimensional cell culture conditions, only two of the above-mentioned publications with liposomal formulations of tyrosine kinase inhibitors reported viability data as compared to respective free drugs. On the one hand, liposomal gefitinib exerted strongly r
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