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Based on their different sources the APN inhibitors APNIs
2024-05-27
Based on their different sources, the APN inhibitors (APNIs) can be divided into the natural products and synthetic compounds. Bestatin (1, Fig. 1), isolated from the Streptomyces oliuoreticuli by Umezawa et al., is the first reported and only marketed natural dipeptidomimetic inhibitor of APN. Afte
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In this report we introduce a new method for
2024-05-27
In this report, we introduce a new method for identifying aminopeptidases. Because single substrates can be insufficient for enzyme identification, we used an entire library of substrates to obtain more information about enzyme activity and to directly detect aminopeptidases. Moreover, substrates ca
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For the first series we decided
2024-05-27
For the first series we decided to verify the effects induced, on the ALR2 inhibitory properties, of an additional steric hindrance on the carbon in α position with respect to the carboxylic group, by introducing a methyl group (R2=Me). Therefore, we synthesized a series of new α-alanine derivatives
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Corticosterone induced inhibition of OCT mediated
2024-05-27
Corticosterone-induced inhibition of OCT-mediated transport is rapid and appears to involve direct interaction of the steroid with the transporter at a specific site. Volk et al. (2003) studied OCT2-mediated transport by measuring substrate-induced currents using patch clamp of Xenopus oocytes exoge
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There are two ways to transport
2024-05-27
There are two ways to transport FFAs into cells. First by passive diffusion. Second as the putative long-chain fatty calcium sensing receptor transporters are proposed, CD36 the plasma membrane-associated fatty acid-binding protein (FABPpm) and fatty acid transport proteins (FATP) [11], where CD36
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A previous study reported that the serotonergic mechanism
2024-05-27
A previous study reported that the serotonergic mechanism was involved in the psychological stress-induced alteration in synaptic plasticity in the rat hippocampal CA1 field (Matsumoto et al., 2004). Sumitaka Inoue et al. (Inoue et al., 2014) reported that pretreatment with a 5-HT1A receptor partial
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Ethanol can affect biological systems directly or also
2024-05-27
Ethanol can affect biological systems directly, or also through the interactions between these systems, which become important in the actions promoted by alcohol consumption. Its metabolites acetaldehyde and acetate play a key role in the Bikinin receptor mediating some effects of ethanol (Israel et
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br Acknowledgment br Introduction Vascular smooth muscle cel
2024-05-27
Acknowledgment Introduction Vascular smooth muscle cells (VSMC) exhibit the capacity to switch between a differentiated (contractile) and a dedifferentiated (synthetic) phenotype [1]. Synthetic VSMC express a lower amount of contractile proteins such as Smooth muscle 22α (sm22α) and α-Smooth m
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br Experimental Procedures br Acknowledgments br Introductio
2024-05-27
Experimental Procedures Acknowledgments Introduction Synapses are fundamental units for efficient communication between neurons and their target cells. Despite significant progress in understanding the structure of matured synapses, less is known about the mechanisms by which neurotransmitt
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The UV vis and fluorescence spectra have
2024-05-27
The UV–vis and fluorescence spectra have been used to study the interaction between small chemical molecules and biomolecules (Punith and Seetharamappa, 2012). The UV glatiramer acetate synthesis peak of the protein changes with the microenvironment of the chromophore. That is, the peaks may show a
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The H N mutation in exon has not
2024-05-27
The H373N mutation in exon 6 has not previously been reported [3], [4], [5], [6]; thus, this mutation appears to be a novel mutation. The functional expression study demonstrated that the H373N mutation results in almost complete loss of enzymatic activity. Thus, it is highly likely that the H373N m
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Having established the structural requirements for potency
2024-05-25
Having established the structural requirements for potency in both the biochemical and biomarker (CRA) assays, we evaluated key compounds in the metabolic stability assay. Disappointingly, we found that all compounds had high intrinsic clearances in mouse microsomes. To ascertain whether the in vitr
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Skeletal pain associated with bone fracture is another
2024-05-25
Skeletal pain associated with bone fracture is another area of critical need for a novel pain medication. NSAIDs and opiates are the two major therapies currently used to manage bone fracture pain. However, both of these therapies lead to significant unwanted side effects. Using the osteotomy model
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br Materials and methods br Results Dried leaves used were
2024-05-25
Materials and methods Results Dried KC7F2 used were 48.46 g C. benghalensis, 857.98 g T. zebrina and 25.09 g T. fluminensis. The samples gave 12.9% C. benghalensis, 0.078% T. zebrina and 3.06% T. fluminensis methanol extracts. The methanol extracts were evaluated for their lipoxygenase inhib
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The tumor suppressor function of
2024-05-25
The tumor-suppressor function of 15-LOX-2 in normal prostate epithelial cells may be explained by the induction of replicative senescence [14,15]. Thus, 15-LOX-2 is overexpressed in age-dependent prostatic hyperplasia, but cell senescence may hinder progression to malignant transformation. Notwithst
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