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In recent years several DPP IV inhibitors
2022-06-20
In recent years, several DPP-IV inhibitors have already been approved, such as sitagliptin, vildagliptin, saxagliptin, tenegliptin, alogliptin and linagliptin, etc. Among them, linagliptin (1, Fig. 1) is a non-peptide mimetic Z-IETD-FMK with a unique xanthine scaffold developed through high-throughp
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br Methods and materials br Acknowledgements
2022-06-20
Methods and materials Acknowledgements The authors thank the NIH AIDS Reagent Program for providing the materials and reagents. The HIV-1 1084i envelope gene was a generous gift from Dr. Charles Wood. This work was supported in part by grants to S.-H. X. from the Bill and Melinda Gates Foundat
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Naringin has been shown to have
2022-06-20
Naringin has been shown to have significant anti-inflammation, anti-oxidative stress, glucolipid metabolic regulation, and myocardial protection effects (Gopinath et al., 2011, Gopinath and Sudhandiran, 2012), suggesting that it may mitigate ADC by inhibiting P2X7 receptors. In the present study, na
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br Materials and methods br Results br Discussion The redox
2022-06-20
Materials and methods Results Discussion The redox domain that spans the region between amino Telaprevir synthesis positions 35 and 127 of the major human AP endonuclease, APE1, regulates the sequence-specific DNA binding of various transcription factors [[52], [85]]. The existent crystal
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Results indicated that superfusion of orexin alone
2022-06-20
Results indicated that superfusion of orexin alone, glutamate alone or orexin-glutamate co-administration significantly increases the spontaneous discharge rate of LC neurons in both morphine dependent and non-dependent rats (Fig. 2, Fig. 3). However, co-application of orexin and glutamate resulted
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br Experimental section br Introduction Fasting hyperglycaem
2022-06-20
Experimental section Introduction Fasting hyperglycaemia in all forms of diabetes mellitus occurs primarily as a result of upsurge in hepatic glucose synthesis (HGS) [1], [2]. Two specific enzymes, glucokinase (GK) and glucose-6 phosphatase (Glu-6-Pase) play crucial role in hepatic glucose pro
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During the tests in vitro
2022-06-20
During the tests in vitro, SHP289-04 showed the beneficial effect on both two important aspects. In human liver carcinoma cell line HepG2, it was found to improve glucose consumption significantly. Otherwise, in pancreas cell line NIT1, it could only promote insulin secretion significantly at high g
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br Results br Discussion Using
2022-06-20
Results Discussion Using a novel viral vector for norepinephrine-targeted gene deletion, we have shown that glucocorticoid receptor SYBR Safe DNA Gel Stain from locus coeruleus norepinephrine neurons reduces social interaction specifically in female mice. This effect is not attributable to ch
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Fatty acid amide hydrolase FAAH is a membrane bound
2022-06-18
Fatty tachykinins amide hydrolase (FAAH) is a membrane-bound enzyme which releases arachidonic acid and ethanolamine by breaking amide bond of AEA. It also controls the cellular uptake of AEA, by creating and maintaining an inward concentration gradient leading to AEA-facilitated diffusion via a sp
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One limitation of our study was that all
2022-06-18
One limitation of our study was that all control dogs had histologic evidence of mild GI inflammation according to established WSAVA guidelines (Washabau et al., 2010), despite being apparently healthy purpose-bred research dogs housed in a controlled environment with no history of vomiting, diarrhe
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The synthetic pathway of the target compounds and is present
2022-06-18
The synthetic pathway of the target compounds , , , and is presented in . The intermediate was synthesized according to a reported method. The intermediate was prepared by mixing UA with an equimolar concentration of KCO, a catalytic amount of KI, and more than two equivalents of 1,2-dibromoethane o
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Substrate affinity and specificity can be enhanced by dockin
2022-06-18
Substrate affinity and specificity can be enhanced by docking interactions, in which regions distal to the site of BOP reagent bind to grooves, pockets, or surfaces outside of the kinase catalytic cleft 1, 2, 5, 6. Like catalytic site interactions, docking interactions can involve recognition of sh
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In normal tissues the expression patterns of
2022-06-17
In normal tissues, the expression patterns of GPR120 and GPR40 are not uniform. GPR120 is highly expressed in adipocytes, lung and intestinal tract, while GPR40 is shown to be expressed in pancreatic islet AH 7614 and intestinal tract [7], [20]. It is considered that the distribution of the GPR120
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N6-Methyl-dATP T lymphocytes play an important role in cellu
2022-06-17
T lymphocytes play an important role in cellular and humoral immunity and immune responses (Shin and Iwasaki, 2013; Schenkel and Masopust, 2014). T N6-Methyl-dATP mature after complex selection and differentiation in the thymus. They can express various membrane proteins, such as CD3, CD4, and CD8 m
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Molecular properties as well as
2022-06-17
Molecular properties as well as metabolic stability in rat and human liver microsomes for the most active nitro (), nitrile (), methylsulfone (), and sulfonamides () analogues were measured (). All these derivatives possessed excellent membrane permeability as measured in the Pampa assay and further
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