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Glucose uptake a critical metabolic control
2022-07-16

Glucose uptake, a critical metabolic control point in glycolysis, is mediated by the GLUT (SLC2) family of integral membrane transporters (Mueckler and Thorens, 2013). GLUT1 (SLC2A1), one of the most well-studied members of the SLC2 family, exhibits a wide tissue distribution; cell surface expressio
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Although the ramifications of non additive SAR are
2022-07-16

Although the ramifications of non-additive SAR are context-dependent, the knowledge that perturbations in one region of a chemical series are not synergistic with perturbations in another region of the same chemical series is clearly pertinent to any medicinal chemistry effort. In our experience, no
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It must be noted that while the accumulated evidence
2022-07-16

It must be noted that while the accumulated evidence on molecular mechanisms has resulted in well-established experimental methods to externally act on single-cell characteristics and networks, safe and efficient external methods to modify multicellular states are still a matter of basic research. C
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br During cardiac ischaemia a decrease in GJ
2022-07-16

During cardiac ischaemia, a decrease in GJ coupling is observed, which results in slower conduction of electrical impulses and a higher risk of arrhythmias.[13], [20] In Huntington’s disease an increase in the XL228 of 5 Cxs was observed in the astrocytes in the brain, suggesting an adaptive prote
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N Alkylated quinolinium dyes are the
2022-07-16

N-Alkylated quinolinium dyes are the common fluorescence molecules used in fluorescence sensing and cell imaging because of their attractive optical properties as well as high DNA binding affinities.13, 14, 15, 16, 17, 18, 19, 20 Moreover, the quinolinium moiety usually plays the role of donor in va
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In this study it was demonstrated that
2022-07-16

In this study it was demonstrated that also in mice chronically exposed to CS, lung inflammation persists after SC and is associated with a progressive alveolar loss and remodeling of respiratory tract, characterized by the onset of bronchial and bronchiolar GCM and peribronchiolar fibrosis. Persist
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The typical pharmacophore for GPR agonists
2022-07-16

The typical pharmacophore for GPR40 agonists contains four parts: head (acid moiety), central (phenyl ring), linker and tail (aromatic carbocyclic or heterocyclic ring) [20]. On the other hand, the chemical features that are required for the PPARγ agonists include hydrogen bond donors and acceptors
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During the activation of the coagulation cascade
2022-07-15

During the activation of the coagulation cascade, factor Xa (FXa) forms a complex with activated factor V and calcium N1-Methylguanosine-5'-Triphosphate on the surface of platelet membrane (so called prothrombinase complex) and converts prothrombin to thrombin [5], [6]. Selective FXa inhibitors do
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Parkinson s disease is another neurodegenerative disorder af
2022-07-15

Parkinson's disease is another neurodegenerative disorder affecting H3Rs. The most common clinical symptoms of this disease are rigidity, bradykinesia, rest tremor, loss of postural reflexes, and gain impairment owing to progressive degeneration of the dopaminergic neurons in the nigro-striatal neur
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br Materials and methods br Results Estimations of OMP
2022-07-15

Materials and methods Results Estimations of OMP generated by the proposed mechanism (Fig. 1) were first performed for the range of 0.001–2 mM of Cathepsin S inhibitor concentration in the cytosol. It was assumed that only 5% of all VDACs in MOM form the ANT-VDAC1-HKI contact sites, and that
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In addition to acting as the gatekeeper
2022-07-15

In addition to acting as the gatekeeper for the metabolic and antioxidant roles of glucose, HKs have also been found to regulate mPTP opening directly. First described in the cancer field, the high-affinity HK isoforms HK1 and HK2 are strongly anti-apoptotic when bound to the outer mitochondrial mem
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br Multiple sclerosis MS is an immune mediated
2022-07-15

Multiple sclerosis MS is an immune-mediated disease of the human CNS with a pathological signature featuring immunocyte infiltration, altered cytokine production, oligodendroglial degeneration, astrogliosis, microglial activation, multifocal demyelination and axonal degeneration (Schipper, 2004b)
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It has been known for some
2022-07-15

It has been known for some time that an oral salt load given to mammals induces a much greater natriuresis than the intravenous administration of an equivalent amount of saline (Carey et al., 1976, Singer et al., 1998). In addition, oral administration of salt to rats has been reported to augmented
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Introduction Epigenetic alterations play an important role i
2022-07-15

Introduction Epigenetic alterations play an important role in carcinogenesis. Aberrant promoter CpG island hypermethylation causes transcriptional gene silencing [1], and has been documented for a number of genes in prostate cancer (PCA) [2]. Histone modifications are also important regulators of t
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br Other Functions of HCA Receptors HCA receptors in
2022-07-15

Other Functions of HCA Receptors HCA receptors, in particular HCA1, are expressed in various primary tumor GNE-317 77, 78, 79. This is of interest, as most solid tumors show increased glucose uptake and lactate formation even under normoxic conditions, with lactate concentrations in the tumor mi
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