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br Research perspective In vitro and in vivo
2023-10-27
Research perspective In vitro and in vivo studies have demonstrated that increased LPA/ATX signaling contributes to cancer initiation and progression. Recent findings on the role of non-tumoral ATX in cancer progression and metastasis highlighted a new functional contribution for the microenviron
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GDC-0084 It is increasingly evident that many metabolic gene
2023-10-27
It is increasingly evident that many metabolic genes are associated with cancer progression of various tumor cells, including NSCLC. In particular, GLUT1 overexpression has been reported in NSCLC, and correlations between GLUT1 expression and a number of clinical parameters such as gender, smoking s
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Here we investigate the ATM
2023-10-27
Here, we investigate the ATM to ATR switch in normal human fibroblasts (82-6 cells) after irradiation with γ-rays, or high LET 56Fe and 28Si and moderate LET 16O particles. Our data provide important evidence of LET dependence on the transition of ATM to ATR as well as end resection at the sites of
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Although the interactions of PhLP with G and
2023-10-26
Although the interactions of PhLP with Gβγ and its other partners have been convincingly documented through in vitro studies, it is not clear how PhLP controls (±)-Baclofen signaling in vivo. C. elegans provides a powerful genetic model to analyze Phosducin function and study its interacting partne
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The apocrine sweat glands of the
2023-10-26
The apocrine sweat glands of the human axilla produce odor substances with pheromone functions whose nature corresponds to volatile steroids (Cowley and Brooksbank, 1991, Grosser et al., 2000, Sobel et al., 1999, Weller, 1998). These functions only begin with puberty, indicating that sex hormones st
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Tephrosia purpurea Linn pers Fabaceae a widely growing
2023-10-26
Tephrosia purpurea (Linn.) pers, (Fabaceae), a widely growing herbaceous perennial is reported to exhibit significant anti-hyperglycemic activity in animal models [7], [8], [9] as well as able to delay the development of diabetic complications [10], [11]. Recently, we have reported T. purpurea for i
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It has been reported that HT R involves in type
2023-10-26
It has been reported that 5-HT2R involves in type 2 diabetes mellitus and 5-HT-induced IR [22,23]. The present study also demonstrated that it is 5-HT2R rather than other 5-HT receptors, including 5-HT1BR and 5-HT7R, in the liver that mediates HFD-induced abnormality of hepatic lipid metabolism, and
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br Conflict of Interest br Transparency Document br Introduc
2023-10-26
Conflict of Interest Transparency Document Introduction Mitoxantrone (MXT) is an androstenedione chemotherapeutic agent that is used to treat acute nonlymphocytic leukemia, acute lymphoblastic leukemia, prostate cancer, metastatic breast cancer, and non-Hodgkin’s lymphoma [13], [14]. It is
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AdipoRon is an orally active synthetic small molecule
2023-10-26
AdipoRon is an orally active, synthetic small molecule that activates adiponectin receptor (AdipoR). It mimics the antidiabetic effects of adiponectin, exhibiting its effect through the activation of AMPK and PPARα pathways via AdipoR1 and AdipoR2, respectively (Fig. 2) [62]. AdipoR activation has r
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The identification of novel kinase inhibitor scaffolds is hi
2023-10-25
The identification of novel kinase inhibitor scaffolds is highly desirable in order to develop selective kinase inhibitors. Small-molecule inhibitors of Interleukin-2-inducible T-cell kinase (Itk) that are based on the 3-aminopyridin-2-one fragment 1 have been reported. Despite derivatisation of 1 y
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As shown in B the
2023-10-25
As shown in B, the recombinant human 15-LOX-1 (30nM) showed a time-dependent increase in fluorescent signal, and signal development was almost completed within 20min in the presence of 50μM arachidonic RHPS4 mg and 5μM DHR. For both purified enzyme and cell lysates, the enzyme activities disappeare
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Oocytes from the African clawed
2023-10-25
Oocytes from the African clawed frog Xenopus laevis have been widely used as an expression system to study the modulation of NMDA receptors by metabotropic receptors, such as metabotropic glutamate receptors [12], μ opioid receptors [13], insulin receptors [14] and serotonin receptors [15]. No data
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The structural analysis of the ASK activation segment which
2023-10-25
The structural analysis of the ASK1 activation segment, which was not phosphorylated in the crystal structure, showed interactions mimicking those found in activated kinases. In addition, the isolated unphosphorylated ASK1-CD is active and able to autophosphorylate itself at three sites, Thr813, Thr
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Molecular docking quantitative structure activity relationsh
2023-10-25
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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gsk-3 Beside estrogen several classes of compounds have
2023-10-25
Beside estrogen, several gsk-3 of compounds have shown significant neuroprotective efficacy when administered shortly after the induction of animal models of stroke, including glutamate (NMDA) receptor antagonists and zinc chelators [25], [26], [27]. Effects of these or other neuroprotective agents
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