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Through activation of the CD
2024-10-16
Through activation of the CD46–GOPC pathway, attenuated/vaccinal MeVs rapidly induce a transient phase of autophagy which then diminishes with no signs of negative regulation and precedes a second autophagy phase related to viral protein synthesis [115]. In sharp contrast, virulent MeVs do not inter
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br Results and discussion br Conclusion A series of
2024-10-16
Results and discussion Conclusion A series of aminobenzothiazole derivatives were investigated as possible Aurora B kinase inhibitors. Bioisosteric replacement of the heterocyclic core of the lead compound was performed regarding the docking analysis. Replacement of the oxygen netilmicin austr
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The activity of an enzyme may be regulated allosterically as
2024-10-16
The activity of an enzyme may be regulated allosterically as well as transcriptionally. We have consistently studied REMS deprivation (REMSD) associated NA mediated allosteric regulation of Na-K ATPase activity in neurons and glia in vivo and in vitro (Amar and Mallick, 2015; Amar et al., 2016; Bask
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br ASK in multiple sclerosis and optic neuritis Multiple scl
2024-10-16
ASK1 in multiple sclerosis and optic neuritis Multiple sclerosis (MS), a chronic inflammatory demyelinating disease of the central nervous system (CNS), is the most common neurological disease among young adults in the United States and Europe (Dutta and Trapp, 2011). Although MS primarily affect
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Molecular docking quantitative structure activity relationsh
2024-10-16
Molecular docking, quantitative structure–activity relationship (QSAR) and high-throughput virtual screening (HTVS) studies have a very widespread use in computer-assisted drug design.25, 26, 27, 28 Suvannang et al. used the published X-ray crystallographic data to examine known aromatase inhibitors
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Our previous studies and others have identified that the
2024-10-16
Our previous studies and others have identified that the inhalational anesthetic isoflurane induces neuronal apoptosis via [Ca2+]i overload through the opening of synaptic voltage-dependent calcium channels (VDCCs) and the excessive Ca2+ release from the endoplasmic reticulum (Zhao et al., 2011; Zha
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Several strategies have been employed to
2024-10-16
Several strategies have been employed to design and engineer peptide biosensors of kinase activity, which are quite different from the strategies developed to generate genetically encoded KARs. In all cases, doxercalciferol induces changes in the spectral properties of the fluorophore(s) incorporat
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The androgen receptor gene AR is located on the X
2024-10-15
The androgen receptor gene (AR) is located on the X-chromosome and consists of eight exons in humans (Brown et al., 1989; Kuiper et al., 1989). The similar gene structure in mice, monotremes and marsupials indicates AR is highly conserved in mammals (Choong et al., 1998; Faber et al., 1991; He et al
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BI-7273 br Introduction Quenchbody Q body immunoassay is a n
2024-10-15
Introduction Quenchbody (Q-body) immunoassay is a novel biosensing technology that uses the quenching of fluorescence by intrinsic tryptophan (Trp) residues in antibody variable regions when dye(s) are conjugated to an antibody or antibody fragments in appropriate position, and de-quenching while
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Imaging QTL studies may have several potential
2024-10-15
Imaging QTL studies may have several potential advantages over case-control studies, including increased power . Imaging endophenotypes of disease in QTL studies can separate patients and normal subjects more accurately and therefore limit the confound of including asymptomatic subjects in the contr
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GSK2126458 Regarding A Rs and A ARs basal
2024-10-15
Regarding A1Rs and A2ARs, basal conditions generate a low tone of endogenous adenosine and cause A1R activation, in contrast to situations of increased adenosine where A2AR activation becomes dominant. When adenosine concentrations rise, e.g. during hypoxia, also time appears likely important in reg
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A selected set of these
2024-10-15
A selected set of these new derivatives was then used for functional assays at the human A1AR showing, as expected, an antagonist profile with IC50 values at nanomolar level. The same molecules showed also to be efficacious as nanomolar antagonists in a functional assay aimed at analyzing their abil
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A key step in the ADAR reaction is the
2024-10-15
A key step in the ADAR reaction is the formation of the adenosine covalent hydrate with a tetrahedral center at C6. The nucleoside analog 8-azanebularine (box in Fig. 6), with its relatively high propensity to form a covalent hydrate, is useful as an adenosine replacement in ADAR2 substrates to trap
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To better understand the pathophysiology of ASDs we would
2024-10-15
To better understand the pathophysiology of ASDs, we would need comprehensive information on a) the functions of ASD-associated proteins in the brain, b) how mutations affect the expression level and function of these proteins, c) how mutations affect their function in neurons, and d) how changed ne
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In conclusion two novel series of furo
2024-10-15
In conclusion, two novel series of furo[2,3-]pyrimidin4-amines and 7-pyrrolo[2,3-]pyrimidin-4-amines which exhibit potent in vitro inhibitor activity against ACK1 have been identified and evaluated. 1,3-Dithiolane-substituted pyrrolopyrimidine displays excellent ACK1 cellular inhibition, good kinas
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