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br FXR FGF in the control of
2021-12-20
FXR–FGF15/19 in the control of BAs synthesis The nuclear receptor FXR is the master regulator of BAs homeostasis, modulating their synthesis, carboxypeptidase and uptake [15]. FXR decreases BA de novo hepatic biosynthesis by reducing the expression of CYP7A1. At the canalicular membrane, newly-s
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Considering the conformational preferences of the SRSRY sequ
2021-12-20
Considering the conformational preferences of the SRSRY sequence in the x-ray structures of soluble uPAR (SuPAR) [18], [19], [20], [50], [51], it is included in a quite flexible linker delimited by Cys76 and Cys95 residues. The SRSRY sequence adopts either α-turned or β-extended conformation. In any
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This excellent tolerability is especially
2021-12-20
This excellent tolerability is especially interesting in the light of the fact that intravenous administration of liposomal ponatinib was predicted to yield much higher plasma concentrations as compared to the orally administered free drug. In addition, liposomal drug dose in absolute numbers was te
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In the current study we
2021-12-20
In the current study, we report the properties of P. anserina mutants carrying mutations in a gene encoding the bi-functional enzyme 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase (PFK-2/FBPase-2). This enzyme catalyzes two opposite reactions (Pilkis et al., 1995, Rider et al., 2004): synthesi
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In conclusion the present study shows that
2021-12-20
In conclusion, the present study shows that the endothelin system is of importance in the cardiopulmonary vascular pathophysiology of porcine endotoxin shock. In this model, combination of a selective endothelin ETA and a selective endothelin ETB receptor antagonist markedly improved pulmonary circu
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In the pathogenesis of insulin resistance chronic activation
2021-12-18
In the pathogenesis of insulin resistance, chronic activation of inflammatory pathways plays an important role, and the macrophage/adipocyte inter-communication provides a key mechanism underlying the common disease states of decreased insulin sensitivity [10]. This involves the migration of macroph
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br Acknowledgements We thank the
2021-12-18
Acknowledgements We thank the support of the National Natural Science Foundation of China (NSFC) project 81501342 and support from the Disciplinary Group of Oncology and Immunology program of Xinxiang Medical University. Introduction First described as a new clinical entity in 1981, the Acqui
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rolipram The amino hydroxy methyl isoxazolepropionic acid AM
2021-12-18
The α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic rolipram (AMPA) receptors are related ionotropic glutamate receptors (iGluRs) that mediate fast excitatory neurotransmission, and are also typically heteromeric ion channels, composed of GluA2 subunits in conjugation with GluA1, GluA3, or GluA4 su
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MAPK are involved in a large variety
2021-12-18
MAPK are involved in a large variety of solid and hematolgical neoplasms and, indeed, several components of the MAPK network have already been proposed as targets in cancer therapy, such as p38, JNK, ERK1/2, MEK1/2, RAF, RAS, DUSP1 and ERK5 [11], [12]. Among them, alteration of the RAS-RAF-MEK1/2-ER
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In our study the changes in the and
2021-12-17
In our study, the changes in the α4 and δ subunit expression were accompanied by a significant increase in γ2 subunit expression in almost all analysed hippocampal structures in the fully kindled animals. In contrast, an acute injection of PTZ at a convulsive dose (55mg/kg) evoked a potent decrease
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VS strategies have been building momentum in G
2021-12-17
VS strategies have been building momentum in G4 drug discovery both as a low-cost enrichment step and as a lead development step in the discovery pipeline, which our laboratory has previously discussed [31]. Whereas traditional HTS methods rely on obtaining and screening hundreds or thousands of com
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The mechanisms underlying the inhibitory effects of n FAs
2021-12-17
The mechanisms underlying the inhibitory effects of n-3 FAs on neoplasia have not been completely elucidated. Until recently, the emphasis has been on the ability of n-3 FAs to compete for the pathways that lead to the synthesis of pro-inflammatory eicosanoids from arachidonic acid, an n-6 FA, there
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GLP is released in response to
2021-12-17
GLP-1 is released in response to ingestion of nutrients including carbohydrates, protein, and fat. Recent studies aimed at identifying the receptors involved in nutrient stimulated GLP-1 secretion have identified free fatty Bindarit mg receptor 4 (FFA4/GPR120) as a potential 7TM receptor involved in
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As concerns TRPV assays benzylic amides and
2021-12-17
As concerns TRPV1 assays, benzylic amides and benzylic reverse amides exhibited an overall superiority over their aryl counterparts and , and ureas and . A reversed trend was however observed with the 4-chlorostyryl and 4--butylphenyl moieties (compare compounds and ; , , and ; and ). The EC and IC
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Management of HIV treatment with HIV PIs can
2021-12-17
Management of HIV-1 treatment with HIV PIs can be complicated due to wide inter-patient variability in BI-847325 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]]. Seve
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