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A pyrimidine class of compounds is of enormous interest with
2022-05-09
A pyrimidine class of compounds is of enormous interest within anti-HIV drug discovery process for several decades, as pyrimidine based DABOs class [7], DAPYs class [8] are well known as NNRTIs as well as NRTIs. However, the overall role of a pyrimidine class of heterocycles in anti-HIV drug discove
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Benzene metabolism occurs primarily in the liver
2022-05-09
Benzene metabolism occurs primarily in the liver where benzene is converted into phenol, catechol, hydroquinone (HQ). HQ is further converted to 1,4-benzoquinone (1,4-BQ) in the bone marrow which is the primary organ of benzene toxicity (Bolton et al., 2000). 1,4-BQ is an important benzene metabolit
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The data presented here support a
2022-05-09
The data presented here support a dynamic and complex interplay among labile heme, BACH1 and HO-1. It appears also that metabolites of heme degradation may participate in the mechanistic regulation of the various factors examined. Our results point to the possibility that the HO-1 pathway restricts
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P Benzoxaborole substituted macrocyclic compounds based
2022-05-09
P4-Benzoxaborole-substituted macrocyclic compounds based on ITMN-191 scaffold were prepared using a general scheme as shown in . ITMN-191 was prepared by following a patent procedure. The P4 BOC group was removed by treatment with TFA in dichloromethane to give amine . The coupling of the amine to 6
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Biological evaluations of the compounds were done
2022-05-09
Biological evaluations of the compounds were done both using HCV protease and replicon assays. Results are shown in . The protease inhibitory IC’s were determined using a FRET assay with HCV NS3/4A 1a protease domain. The replicon EC’s were determined using a replicon luciferase cell-based assay. Th
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br Activity dependent control of myelination
2022-05-07
Activity-dependent control of myelination and myelin maintenance Oligodendrocytes have intrinsic myelinating capacity and can myelinate fixed Liraglutide in addition to synthetic nanofibers and micropillars [21, 34, 35]. What prevents oligodendrocytes from myelinating dendrites or other cells in
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Human GPR hGPR was originally isolated in
2022-05-07
Human GPR55 (hGPR55) was originally isolated in 1999 as an orphan GPCR with high levels of expression in human striatum (Sawzdargo et al., 1999) (Genbank accession # NM_005683.3). hGPR55 was mapped to human chromosome 2q37, and in the human CNS it is predominantly localized to the caudate, putamen,
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br Discovery of GPR A The murine niacin receptor protein
2022-05-07
Discovery of GPR109A The murine niacin receptor, protein upregulated in macrophages by interferon-γ (PUMA-G), was identified as a G-protein-coupled receptor (GPCR) expressed in adipocytes and spleen [22], [23]. This finding suggested a role of this receptor in macrophage function [24]. In 2003, t
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br Specificity of CD T cells and their role in
2022-05-07
Specificity of CD4 T cells and their role in flavivirus neutralizing antibody responses CD4 T cells recognize peptides that are proteolytically processed from protein antigens and presented by MHC class II molecules on the surface of specialized antigen-presenting cells, such as dendritic cells o
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br Concluding Remarks br Outstanding Questions br Acknowledg
2022-05-07
Concluding Remarks Outstanding Questions Acknowledgments Research on DNA glycosylases in our laboratory is supported by the National Science Foundation (MCB-1517695). A.A.R. and N.P.B. are supported by the National Science Foundation Graduate Research Fellowship Program (DGE-1445197). In
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Several groups studied CTD mouse models which largely mimick
2022-05-07
Several groups studied CTD mouse models, which largely mimicked the symptoms (i.e. impaired cognition and autistic-like behaviour) of the human disease (Kurosawa et al., 2012; Baroncelli et al., 2016; Stockebrand, 2018). The CRT-1 knockout mice showed a drastic deterioration in the GABAergic system,
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We report on four affected
2022-05-07
We report on four affected children from two unrelated consanguineous AMD-070 with moderate to severe ID associated with epilepsy and variable neuropsychiatric features. Using whole-exome sequencing, we identified homozygous missense variants in SLC45A1 (OMIM: 605763), which codes for a neuronal gl
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br Acknowledgments This work was funded by NIH
2022-05-07
Acknowledgments This work was funded by NIH Grant 2R01 MH066958 (JGT) and NSF CAREER award IOS- 1053716 (NV). We thank Dr. Greti Aguilera for the generous gift of the GRE-Luciferase construct and Dr. Louis Muglia for the generous gift of the GR-GFP construct. Introduction Prostate cancer (PCa
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The fine interplay among post
2022-05-07
The fine interplay among post-translational modifications and intersection with other pathways, such as PI3K–AKT, has a crucial role in the regulation of GLI activity and in the generation of their repressor forms 40, 41, 42. In addition to β-TrCP, for example, other E3 ligases belonging to the real
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Amongst oxidants that we have studied PMS is
2022-05-07
Amongst oxidants that we have studied, PMS is unique in having a greater effect in deoxygenated cells. The resulting phenotype shows some similarities with the increased cation permeability shown by deoxygenated sickle aphidicolin [27]. It is interesting to consider why PMS has this effect. PMS fun
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