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The general synthetic routes leading to
2022-05-04
The general synthetic routes, leading to aspartate and 2,3-diaminopropionate analogs, are shown in . As outlined in , aspartic tlr4 analogs – were synthesized through standard carbodiimide-mediated coupling between an amine and an appropriately protected aspartic acid. It is worth mentioning that s
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ci-1033 The unique mechanism of EAAT anion channel
2022-05-04
The unique mechanism of EAAT anion channel gating results in neuronal or glial anion conductances that follow changes in substrate concentrations and thus allow feedback control of glutamate release (Wersinger et al., 2006) or modification of GABAergic postsynaptic currents by glutamatergic signals
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br Experimental section br Acknowledgments
2022-05-04
Experimental section Acknowledgments MIN6 hiv protease inhibitor were kindly provided by Dr. Junichi Miyazaki, Osaka University. This research was supported in part by the Ministry of Education, Culture, Sports, Science and Technology of Japan (JP16H05099 and JP18H04609 to K.H., and JP16H0657
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Although most of the incretin effects on glucose metabolism
2022-05-04
Although most of the incretin effects on [D-Lys3]-GHRP-6 metabolism can be secondary to their action on insulin/glucagon secretion, some evidence strongly suggests that they could also act directly on liver glucose utilization and production [4], [13], [22], [27], [34], [44]. Supporting this concep
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Ghrelin readily crosses the blood brain barrier
2022-05-04
Ghrelin readily crosses the blood GGsTop sale barrier (Banks et al., 2002, Banks et al., 2008), and recent studies have identified central nervous system sites of action for ghrelin-mediated appetite and hyperphagia (Alvarez-Crespo et al., 2012, King et al., 2011, Schele et al., 2016, Skibicka et a
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br Acknowledgements We apologize to our distinguished collea
2022-05-04
Acknowledgements We apologize to our distinguished colleagues whose work has not been cited owing to space limitations. This work was funded by the Italian Association for Cancer Research (AIRC, Milan, Italy, IG 14732 to A.M.); Italian Ministry of University and Education (Finanziamenti per la Ri
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The overall very satisfactory potency profile
2022-05-04
The overall very satisfactory potency profile of compounds 7a–l suggests that 1,3,4-thiadiazole-2-carboxamide moiety was a suitable periphery group to add to the 3-phenylpropanoic Fmoc-Leu-OH core in order to improve affinity to FFA1. The agonist activity in this series appears to be particularly s
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br Acknowledgements br Introduction Muscle
2022-04-29
Acknowledgements Introduction Muscle FBPase is very sensitive to AMP inhibition and in the presence of physiological concentrations of this effector in muscle fibres FBPase should be almost completely inactive [1], [2]. Recently, we have presented evidence that, in vitro, muscle aldolase binds
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In the Medicines for Malaria Venture
2022-04-29
In 2011 the Medicines for Malaria Venture (MMV) distributed the Open-Access Malaria Box to accelerate antimalarial drug discovery (Spangenberg et al., 2013). The Malaria Box consists of 400 structurally diverse compounds, curated from >20,000 hits generated from large-scale screens, that inhibit the
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The membrane metalloendopeptidase MME gene
2022-04-29
The membrane metalloendopeptidase (MME) gene is located at human chromosome 3q21-27. It encodes a 100-kD type II transmembrane glycoprotein, a widely expressed membrane metalloendopeptidase that degrades a number of substrates. The active site of the enzyme faces the extracellular space. MME is wide
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br Venous thromboembolism VTE is a rare but
2022-04-29
Venous thromboembolism (VTE) is a rare but potentially life-threatening complication of total joint arthroplasty (TJA) . With modern chemoprophylaxis, the incidence of VTE after primary total hip (THA) or total knee (TKA) arthroplasty is commonly estimated between 0.5% and 1%, and VTE is now consi
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Current guidelines for thromboprophylaxis recommend the use
2022-04-29
Current guidelines for thromboprophylaxis recommend the use of vitamin K antagonists (eg, warfarin), low-molecular-weight heparin (LMWH), or indirect inhibitor of factor Xa . Aspirin is also used for thromboprophylaxis in patients undergoing orthopedic procedures , . The efficacy and safety of LMWH
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br Introduction Over one million people
2022-04-29
Introduction Over one million people are currently living with HIV in the United States (CDC, 2016). Through advances in HIV medications, the use of antiretroviral therapy has led to people living longer with HIV (Palella et al., 2006). In attempts to mitigate the effects of the psychological and
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The VirScan assay has several
2022-04-29
The VirScan assay has several advantages over alternative multiplex serological assays for peptide discovery. These advantages include quantitative assessment of antibody binding to peptides that span all open reading frames in the HIV genome, including both structural and regulatory proteins; repre
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aminopeptidase inhibitor With the aim to identify
2022-04-29
With the aim to identify potential novel targets in CVD, we applied proteome analyses on vascular tissue of these frequently used mouse models of atherosclerotic disease in the presence and/or absence of diabetes. Potential targets for intervention identified with this approach were validated in hum
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