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Through the analysis of various synthetic
2022-08-18
Through the analysis of various synthetic GPR40 agonists as reported in literature, we found that a number of these compounds contained a phenylpropanoic 3065 receptor motif which was inspired from naturally occurring medium to long chain fatty acids. For instance, in the early period of discoverin
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br Introduction Before planning population
2022-08-18
Introduction Before planning population-based genetic analysis or GWAS, it is important to annotate the sequence of the gene because these sequences represent the major sites such as promoter and transcription factor cgk synthesis which may ultimately affect the expression of the gene. Similarly,
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br Conflict of interests br
2022-08-18
Conflict of interests Acknowledgements This work was supported by the National Institutes of Health grants HD058577 and ES01678 to Kirill Kiselyov. We thank Sreeram Ravi for technical support. We also thank Mike Myers at the University of Pittsburgh Cancer Institute Flow Cytometry Facility.
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To validate the effects of the G a HMT
2022-08-18
To validate the effects of the G9a HMT inhibitors on HMEC-1 WM-8014 and transcriptional responses we generated knockdown cells for G9a using an shRNA approach. Upon transduction of HMEC-1 and doxycycline activation of the shRNA, both G9a HMT mRNA and protein expression were effectively decreased (Fi
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Introduction Soluble guanylyl cyclase sGC
2022-08-17
Introduction Soluble guanylyl cyclase (sGC) is a key protein in the regulation of multiple physiological functions in mammalian physiology [1,2]. Upon stimulation by nitric oxide (NO) [3], sGC generates cyclic guanosine monophosphate (cGMP) from guanosine-5′ triphosphate and activates protein kinas
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It is interesting to note that
2022-08-17
It is interesting to note that the long and short forms of GPR120 exist at different basal levels of phosphorylation, with the short form demonstrating a greater degree of constitutive activity [12]. Importantly, Burns and Moniri [12] showed that, upon activation, the long and short isoforms of GPR1
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We hypothesized that modulating redox stress by altering end
2022-08-17
We hypothesized that modulating redox stress by altering endogenous antioxidant content (overexpression of catalase) and/or via dietary intervention will improve energy metabolism, adipose tissue function, and overall glucose and lipid homeostasis. To better understand the interplay between redox re
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Generally replacement of the aryl group
2022-08-17
Generally, replacement of the aryl group was well tolerated, with tetrahydropyran () and hydroxyl () functionality providing potency equivalent to and . These substitutions had no effect on selectivity versus GlyT2 and taurine transporter (TauT)—no activity was observed at micromolar concentrations.
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Here we performed TEM and AFM imaging to study APE
2022-08-17
Here, we performed TEM and AFM imaging to study APE1–DNA interactions. The results showed that APE1 can dynamically polymerize on DNA in an apparently sequence-independent manner. We propose that this protein polymerization allows for scanning of the structural properties of DNA with short residence
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In the present study both experimental
2022-08-17
In the present study, both experimental and theoretical studies were performed to explore the inhibitory mechanisms of indomethacin and its analogues towards GLOI. A remarkable correlation (=0.974) was derived for the four structurally similar NSAIDs and two curcumins between the experimental bindin
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Indirubin The glycine receptor is an ionotropic neurotransmi
2022-08-17
The glycine receptor is an ionotropic neurotransmitter receptor coupled to a chloride ion channel. Glycine receptors are typically described as inhibitory and distributed in the spinal cord and brainstem, though mRNA transcription labelling studies in rats show expression in the hippocampus, cingula
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br Vesicular glutamate transporters VGLUTs br Conclusions Du
2022-08-17
Vesicular glutamate transporters (VGLUTs) Conclusions Due to the molecular cloning of EAAT and VGLUT subtypes, a better understanding of the functional properties of these carriers has been elucidated over the last few years. In the case of the EAATs, specific blockers, such as trans-2,4-PDC,
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Through the analysis of various synthetic GPR agonists
2022-08-17
Through the analysis of various synthetic GPR40 agonists as reported in literature, we found that a number of these compounds contained a phenylpropanoic NSC74859 motif which was inspired from naturally occurring medium to long chain fatty acids. For instance, in the early period of discovering TAK
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dapagliflozin br Redox regulation in the brain Reactive oxyg
2022-08-17
Redox regulation in the brain Reactive oxygen species are generated in dapagliflozin by the mitochondrial respiratory chain, which occurs on the inner mitochondrial membrane (Murphy, 2009, Jensen, 1966, Dickinson and Chang, 2011). Interestingly, although most cancer cells are thought to primarily
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Recent studies revealed that synthetic oligomeric A
2022-08-17
Recent studies revealed that synthetic oligomeric Aβ1-42 decreased GLT-1 expression and promoted mislocalization of GLT-1 from the cell surface of primary astrocytes, leading to glutamate dyshomeostasis in synapses (Abdul et al., 2009, Scimemi et al., 2013). To address the cause for reduction of ast
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