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A compound structurally similar to PF has been
2022-02-12

A levosimendan structurally similar to PF-03654746 has been developed by Pfizer (PF-03654764), with a minor change in the substituent attached to the cyclobutanecarboxamide moiety (Wager et al., 2011). This compound, with the chemical name trans-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)phenyl]
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br Hippo pathway signalling The
2022-02-12

Hippo pathway signalling The Hippo pathway is an evolutionarily conserved signal transduction pathway regulated by cell-cell contact, cell polarity, mechanical cues, ligands of G-protein coupled receptors, and cellular l-ascorbic acid status [10]. This pathway is linked to development, cell prol
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br Conclusion The mitochondrial and glycolytic energy metabo
2022-02-12

Conclusion The mitochondrial and glycolytic energy metabolism of the brain is coordinated by HKI binding to MOM, although the molecular mechanism of such a regulation is not yet clear. The Miglitol for HKI in MOM are VDACs [[5], [6], [7]], mainly the VDAC1 isoform [8]. Using a computational model
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Zalcitabine br Conclusion Whilst acknowledging that forensic
2022-02-12

Conclusion Whilst acknowledging that forensic science critically needs strategic investment across every domain [27], forensic science needs to bring both ‘hedgehog’ and ‘fox’ approaches together to address the roots of the major challenges the discipline faces. Addressing these challenges in a w
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When analyzing HIV AIDS patients in S o Paulo we
2022-02-12

When analyzing HIV/AIDS patients in São Paulo, we detected an association between HIV/HTLV-1/2 infection in black/pardo-colored individuals (OR 2.21, 95% CI 1.21–4.03). However, the majority of serum samples were from patients attending specialized services for hepatitis, other than HIV/AIDS or HTLV
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A similar symbiotic relationship has
2022-02-12

A similar symbiotic relationship has been reported in the brain, where increased gradients of lactate secreted by astrocytes enables neurons to import and use this nutrient, a process referred to the ‘neuron–astrocyte lactate shuttle’ [16]. Similarly, lactate-based metabolic coupling established by
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Lactate induced GPR activation was confirmed with a fluorime
2022-02-12

Lactate-induced GPR81 activation was confirmed with a fluorimetric imaging plate reader (FLIPR) assay, in which lactate induced a [Ca2+] flux in CHO cells stably expressing Gqi5 and HA-GPR81 but not vector control (Fig. 1C). The EC50 of lactate in the FLIPR assay was 4.3±0.73mM, a value well within
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Until now unfortunately no safe effective vaccine
2022-02-12

Until now, unfortunately, no safe, effective vaccine against HIV-1/AIDS has been found [16], [17]. Therefore, the development of safe, effective vaccines is a top priority in HIV/AIDS research field. Accordingly, to investigate the interactions between HIV vaccines or inhibitors and their correspond
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br The methyl aspartate receptor NMDAr hypofunction
2022-02-12

The -methyl--aspartate receptor (NMDAr) hypofunction hypothesis of schizophrenia correlates disease symptomology with glutamatergic neurotransmission dysfunction., , , Therefore, inhibition of glycine transporter 1 (GlyT1) to elevate synaptic levels of glycine and potentiate NMDAr signaling is a
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The aim of this study is to explore new
2022-02-12

The aim of this study is to explore new Glo-I inhibitors using the structure-based pharmacophore approach. Eighteen Glo-I co-crystallized structures have been explored to investigate their pharmacophoric features. Ninety two pharmacophoric models were generated. QSAR analysis followed by Ligand Prof
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br Conclusion Membrane transporters remain relatively unders
2022-02-12

Conclusion Membrane transporters remain relatively understudied in human disease, especially TBI (Cesar-Razquin et al., 2015), and considerably less is known in terms of expression, function and substrates of membrane transporters in pediatric patients. However, their importance in maintaining Ma
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Axons are the largest component of WM
2022-02-12

Axons are the largest component of WM by volume and are a significant repository of intracellular glutamate that can be releases under ischemic conditions [1,3,4,29,117]. We have recently shown that the principle route by which mature myelinated Adenosine-5'-diphosphate release glutamate during acu
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Next we focused on B part the phthalazine
2022-02-12

Next, we focused on B-part, the phthalazine ring. While both nitrogen atoms of the phthalazine ring were found to be important (data not shown), replacing the benzene ring of the phthalazine part was attempted, and shows the results of the substituted pyridazine rings with bearing 2-methoxy benzene
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The previous studies focused on the
2022-02-12

The previous studies focused on the regulation of GK activity by nutrients directly or nutritional hormones (Panserat et al., 2014), there was still a lack of studies paid attention to GK both in activity level and transcriptional level. Besides, the GK regulation by dietary SCH527123 has been defi
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In mammals a major physiological role of the GHSR gene
2022-02-12

In mammals, a major physiological role of the GHSR gene appears to be in regulating food intake and energy homeostasis by partaking in the neuronal mechanisms involving neuropeptide Y and agouti-related protein (Nakazato et al., 2001, Chen et al., 2017). In our study, determination of the abundance
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