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k j and d were then submitted
2021-11-02
15k, 15j and 14d, were then submitted to metabolic stability studies in human and mouse liver microsomes and permeability test with Caco-2 cells (Table 7). 15k, 15j and 14d all retained excellent permeability (Papp value greater than 15.2 × 10−6 cm/s) and displayed modestly improved metabolic stabil
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A oligomers increased ubiquitination of
2021-11-02
Aβ1-42 oligomers increased ubiquitination of GLT-1 in astrocytes. Previous studies found that astrocytic GLT-1 is internalized from the cell surface by ubiquitination of lysines located in the cytoplasmic C-terminus of the transporter (Gonzalez-Gonzalez et al., 2008, Martinez-Villarreal et al., 2012
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The widespread involvement of HH GLI
2021-11-02
The widespread involvement of HH/GLI in human malignancies has initiated a remarkable effort to identify selective HPIs. As shown in Table 2.1, most of these small molecule inhibitors target the essential effector protein SMO, which should lead to pathway abrogation by eventually decreasing the GLIA
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The presence of ghrelin s mRNA in the eye
2021-11-02
The presence of ghrelin's mRNA in the eye and the presence of ghrelin in the aqueous humor, along with a decrease of its levels in glaucoma, suggest a local role for this peptide in the ocular tissue [8], [16], [18]. There is no available data regarding the presence of GHSR-1 in the anterior segment
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br Ghrelin and energy balance To
2021-11-02
Ghrelin and Omeprazole balance To characterize the physiological role of ghrelin in energy homeostasis, ghsr−/− and ghrelin−/− mice were generated [33], [36], [41], [47]. Although ghrelin regulates the amplitude of episodic GH release, ghsr−/− mice were not dwarfs, and in fact appear identical to
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In conclusion starting from the weakly potent
2021-11-02
In conclusion, starting from the weakly potent GSM , exploration of various spacer groups between the triazole ring and the aromatic Nutlin-3a led to the discovery of a new series of potent gamma secretase modulators, with an improved drug-like profile—compared with the originally reported series ar
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All of the abovementioned effects
2021-11-02
All of the abovementioned effects of PUFAs signal their involvement in a cellular phenotype switching phenomenon, which is increasingly recognized as a potential target for future pharmacotherapies of atherosclerosis, especially for individuals who do not respond to the classical lipid-lowering stra
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On the other hand histone deacetylase inhibitors
2021-11-02
On the other hand, histone deacetylase inhibitors can accelerate inflammation resolution by promoting the externalization of AnxA1, a main ALX/FPR2 agonist, with concomitant inhibition of cytokine gene expression in mouse macrophages [30]. Thus, our present results provide an additional mechanism, i
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Thus both in Drosophila and mammals the Hippo pathway
2021-11-01
Thus, both in Drosophila and mammals, the Hippo pathway responds to cell–cell junctions via an apical NF2/Mer-containing complex. Indeed, Hippo signalling and NF2 are required for contact inhibition of growth in cell culture, which is thought to reflect an in vivo function as a sensor of tissue crow
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br Introduction Hexokinase HK is an
2021-11-01
Introduction Hexokinase (HK) is an enzyme that catalyses the transfer of phosphate from ATP to glucose in the first step of glucose metabolism (Wilson, 1995, Wilson, 2003). In mammalian, HK has four important isozymes which are designated as HK1, HK2, HK3 and HK4 (Wilson, 1995, Wilson, 2003). HK1
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br Conclusion br Funding br Availability of data and
2021-11-01
Conclusion Funding Availability of data and materials Authors' contributions Ethics approval and consent to participate Consent for publication Competing interests Introduction Hepatitis C virus (HCV) infection is a global public health problem. An estimated 71.1 million peop
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br The methyl aspartate receptor
2021-11-01
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 amino hydroxy methyl isoxazolepropionic acid AMPA
2021-11-01
The α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic SKF38393 HCl receptor (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
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In the present study co administration
2021-11-01
In the present study, co-administration of TM (AT1 receptor blocker) and PD (AT2 receptor blocker) were made in ischemic mice to explore the significance of AT2 receptors in cerebral ischemia while blocking central AT1 receptors. Also to prove that AT2 receptors should be free after ischemic injury
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Glucagon regulates the transition from
2021-11-01
Glucagon regulates the transition from hepatic glucose utilisation in the absorptive state to glucagon production in the post-absorptive state by acute stimulation of glycogenolysis and inhibition of glycolysis [1]. An important component of this response is the phosphorylation of liver PFK2/FBPase2
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