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In recent years several DPP IV
2021-12-09
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 URMC-099 with a unique xanthine scaffold developed through high-throughput
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Of the patients that presented a CD dip
2021-12-09
Of the 11 patients that presented a CD4 dip with no cause identified other than HIV-infection, 9 had CD4 counts >200 cells/μL in the next measurement and all experienced the event during the first 24 months of follow-up. Intra-laboratory measurements and individual patient physiologic factors also i
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To shed more light on
2021-12-09
To shed more light on the binding of benzophenanthridine to GlyT1, we studied how the replacement of certain residues around the sanguinarine sensitive cysteine 475 previously identified (Jursky et al., 2012) affects GlyT1 inhibition of by these alkaloids. Based on these results we propose a putativ
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br Acknowledgments br Free fatty acids FFAs are not only
2021-12-09
Acknowledgments Free fatty acids (FFAs) are not only essential nutritional components, but they also function as signaling molecules. Recently, a G protein-coupled receptor (GPCR) de-orphanizing strategy successfully identified multiple receptors for FFAs, which function on the cell surface and
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br Materials and methods br Results br Discussion Ajuba
2021-12-09
Materials and methods Results Discussion Ajuba was originally identified as an adaptor protein which communicates cell adhesive events with nuclear responses to remodel the epithelium (Langer et al., 2008; Marie et al., 2003). Recently, increasing evidence has shown that Ajuba functions as
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Multiple mechanisms have been suggested by which
2021-12-09
Multiple mechanisms have been suggested by which glucagon can increase energy expenditure although none have been conclusively proven to be responsible. Both enhanced gluconeogenesis and enhanced protein turnover secondary to hyperglucagonaemia have been suggested as the reason for the increased met
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Many studies support that Gli transcription factors are not
2021-12-09
Many studies support that Gli transcription factors are not solely regulated by Hh/smo signaling but are also influenced by crosstalk with other pathways, such as RAS, PI3K/AKT, transforming growth factor-b/SMAD, PKC, or extracellular signal-regulated kinase pathways which are downstream and indepen
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Recent studies have elucidated a profound role for FFA
2021-12-09
Recent studies have elucidated a profound role for FFA4 in modulation of metabolism and energy utilization as well as endocrine and immune function, and as a consequence, have thrust FFA4 to the forefront of drug discovery efforts. For example, activation of FFA4 by fatty α-Bungarotoxin receptor or
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br STAR Methods br Introduction Arsenite is a well
2021-12-09
STAR★Methods Introduction Arsenite is a well-recognized toxic metalloid that commonly presents in the natural environment. Chronic exposure to arsenite can lead to a wide range of adverse health effects to human, including cancers, cardiovascular diseases, diabetes, skin lesion and neurodegene
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MMV s distinct mode of
2021-12-09
MMV019313's distinct mode of inhibition addresses key impediments in the development of PfFPPS/GGPPS inhibitors as antimalarial drugs. First, it is the first non-bisphosphonate inhibitor of Plasmodium FPPS/GGPPS with drug-like physicochemical properties satisfying the “Rule of 5” (Van Voorhis et al.
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In humans mutations in KDM A KDM B and KDM
2021-12-09
In humans, mutations in KDM5A, KDM5B, and KDM5C are found in patients with ID, implicating KDM5-regulated transcription in the development or activity of neuronal tissues (Vallianatos and Iwase, 2015). KDM5D is Y-linked, and its role in cognition remains uncharacterized. Mutations in KDM5C are the m
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br Recently MST emerged as a critical regulator of leukocyte
2021-12-09
Recently, MST1 emerged as a critical regulator of leukocyte function and autoimmunity in humans. Five independent groups reported on autosomal recessive nonsense mutations in the gene STK4 (which encodes for MST1) in human patients with a novel primary immunodeficiency disease (PID), now called ST
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The rationale for developing HDACi as anticancer
2021-12-08
The rationale for developing HDACi as anticancer agents was based on their ability to induce the hyperacetylation of histones and nonhistone proteins, resulting in increased differentiation, apoptosis, and Forskolin arrest of cancer cells 1, 2, 3. HDACi have been used in the treatment of hematologi
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740 Y-P receptor Further our study provides the first eviden
2021-12-08
Further, our study provides the first evidence that zaprinast and kynurenic 740 Y-P receptor administration not only prevented the development of thermal and mechanical hypersensitivity but also enhanced morphine antinociceptive properties. Morphine is considered to be one of the most effective ana
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Several investigators including ourselves have previously
2021-12-08
Several investigators including ourselves have previously shown, that allogeneic HLA-DPB1 class II-alleles are powerful leukemia rejection SB 747651A dihydrochloride for CD4 T-cell therapy following allogeneic hematopoietic stem cell transplantation (Herr et al., 2017, Rutten et al., 2008, Stevanovi
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