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ML-291 Elimination of the Q R bridge significantly affected
2022-03-24

Elimination of the Q234–R244 bridge significantly affected the protein ML-291 but had little effect on its activity at a permissive temperature, which may seem contrary to the known functional importance of this motif in Fpg. However, since the mutants fully or partially retained the bound zinc (Ta
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Herein we report the discovery of
2022-03-24

Herein, we report the discovery of AM-3189 (). AM-3189 maintains the in vivo efficacy of AMG 837 while displaying a superior pharmacokinetic profile and minimal CNS exposure. As we reported previously, activity on the GPR40 receptor varies significantly with substitution at the β-carbon relative to
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Epidemiological studies revealed that vitamin D deficiency w
2022-03-24

Epidemiological studies revealed that vitamin D deficiency was associated with a wide range of neuropsychiatric disorders and neurodegenerative diseases, in particular, Alzheimer's and Parkinson's disease (Annweiler et al., 2013; Knekt et al., 2010), dementia and cognitive function impairment (Balio
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The developed method was used to quantify RBC membrane trans
2022-03-24

The developed method was used to quantify RBC membrane transport of the anomers of three monofluorinated analogs of glucose in a modified medium designed to provide stable metabolic properties of the cells over the lifetime of the experiment. This allowed us to evaluate the specific interaction (spe
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The MeO CFO phen yl group was then
2022-03-24

The 1-MeO-4-CFO-phen-2-yl group was then selected for the C-3 position when we investigated the aryl substituents at the C-6 position of indazole. As shown in , C-6 position seems to be more tolerant than the C-3 position, as all the aryl groups examined exhibited potent hGCGR activity. Interestingl
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Magtanong et al observed that caspase dependent
2022-03-23

Magtanong et al. (2019) observed that caspase-dependent apoptotic lipotoxicity of saturated fatty acids is suppressed by exogenous MUFAs. This may explain the ability of MUFAs to prevent atherosclerosis, in contrast to the pathogenicity of saturated fatty acids. Moreover, MUFAs may promote while PUF
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In accordance with our study the blockage
2022-03-23

In accordance with our study, the blockage of Fas/FasL pathway and overexpression of miR-204-5p was associated with reduced BUN, Scr, and MDA, as well as elevated SOD and GSH-Px. A recent study has reported the ectopic expression of BUN and Scr in RIRI animals, which marked the dysfunction of kidney
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br Introduction Currently HIV infection
2022-03-23

Introduction Currently, HIV-1 infection treatment guidelines adopted in USA and EU provide for the simultaneous administration of three antiretroviral drugs (HAART “Highly Active Anti-Retroviral Therapy”) in severely compromised patients [[1], [2], [3]]. Coupling at least two different mechanisms
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The even bigger surprise was
2022-03-23

The even bigger surprise was the second feature of both structures. Interestingly, binding of the MRG domain hardly altered the conformation of the SET domain compared with its apo state (An et al., 2011). What did change, however, is the conformation of the ASH1L auto-inhibitory loop (Figure 1). De
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br Histamine H R The cloning of the H R
2022-03-23

Histamine H4R The cloning of the H3R (Lovenberg et al., 1999) provided a template for the search of other Glyoxalase I inhibitor receptors, and resulted in the most recent discovery of histamine H4R. This concluded with six independent groups that have reported the cloning of the H4R (Leurs et a
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br Author contributions br Declaration
2022-03-23

Author contributions Declaration of conflict of interest Acknowledgements We are grateful to the Director, National Institute of Immunology for his support. The work was partially supported by J.C. Bose Fellowship to SSM. We acknowledge the help from staff of Small Animal Facility of Nation
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In hypoxic breast cancer cells BNIP mediated autophagy activ
2022-03-23

In hypoxic breast cancer cells, BNIP3-mediated autophagy activation and elevation of amino Phosphatase Inhibitor Cocktail 2 (100X in ddH2O) levels were notable. BNIP3, a BCL-2 family protein, is known to be transcriptionally regulated by HIF-1α and to be involved in cancer cell death in hypoxic con
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The increased levels of proinflammatory cytokines in BALF ar
2022-03-23

The increased levels of proinflammatory cytokines in BALF are noted during ALI/ARDS, and the persistent elevation of these mediators may exaggerate systemic or focal inflammatory reaction with a worse outcome. These cytokines, particularly TNF-α and IL-6, play essential roles in ALI [16,17]. The ove
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br Acknowledgements This work has
2022-03-23

Acknowledgements This work has been supported by TSTAR USDA and Florida Citrus Advanced Technology Program Grants to D.B., C.P and R.S. One of us (D.B.) is an established scientist fellow at the Oak Ridge Institute for Science and Education (ORISE). This research was supported in part by an appoi
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br GSK The GSK family is highly conserved throughout
2022-03-23

GSK-3 The GSK-3 family is highly conserved throughout evolution and is encoded by two genes, GSK-3α and GSK-3β, which are located in chromosomes 19q13.2 and 3q13.3 in human, respectively. Both GSK-3α and GSK-3β proteins exist in a variety of tissues with the highest levels found in C527 synthesis
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