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In HepG cells compound showed inhibition of
2024-11-23

In HepG2 cells, cdc42 inhibitor showed inhibition of total lipid syntheses with an IC of 8μM. A cell based Alamar Blue cytotoxicity assay was used in parallel to differentiate the effect on the inhibition of lipid synthesis versus potential cytotoxicity. Under identical incubation conditions, comp
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Given the recent discovery of regions of single
2024-11-23

Given the recent discovery of regions of single-stranded DNA in the nuclei of hypoxic cells, the role for ATR in the response to hypoxic stress seems clearer . Zou and Elledge demonstrated that both Ddc 2 (the homolog of ATRIP) and ATRIP have a lower affinity for double-strand breaks than they do f
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Having demonstrated that Gq coupled mGluR a was necessary
2024-11-23

Having demonstrated that Gq-coupled mGluR1a was necessary for estradiol-induced enhancement of CREB phosphorylation, we hypothesized that activation of a separate G-protein signaling pathway could explain the effect of estradiol on L-type calcium channel signaling (Boulware et al., 2005). Indeed, in
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Neural activity resulting from sensory experience is require
2024-11-23

Neural activity resulting from sensory experience is required for the refinement and maturation of neural circuits during cortical critical periods. This refinement is thought to be important for functional optimization of primary sensory cortices, enabling critical functions such as feature detecti
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Young et al described the role
2024-11-22

Young et al. [40] described the role of adenine monophosphate-activated protein kinase (AMPK) in the translocation of GLUT4 in the heart. The AMPK is activated during muscle contraction [74] by converting AMP to ATP. The adenosine analog, 5-aminoimidazole-4-carboxamide ribonucleotide (AICAR), is a c
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Introduction Epinephrine is an endocrine hormone mainly prod
2024-11-22

Introduction Epinephrine is an endocrine hormone mainly produced by adrenal medulla in response to stress (Tank and Lee Wong, 2015). This catecholamine exerts various major physiological effects, concerning notably the cardiovascular system, the respiratory system and the endocrine system, through
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Oxidative stress has recently been reported
2024-11-22

Oxidative stress has recently been reported as one of the important mechanisms of toxic effect of Cd2+[43]. The mechanism of Cd2+-induced oxidative stress involves an imbalance between generation and removal of ROS in tissues and cellular components, causing damage to membranes, DNA, and proteins [4
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br ACK inhibitors Since ACK activation is correlated with
2024-11-22

ACK1 inhibitors Since ACK1 activation is correlated with poor prognosis in various cancers, strong efforts are being directed by multiple groups towards developing highly potent and specific small molecule inhibitors targeting the ACK1 kinase. At least eight small molecule kinase inhibitors have
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br Acknowledgements br Introduction Autoantibodies directed
2024-11-22

Acknowledgements Introduction Autoantibodies directed at neurotransmitter receptors and ion channels are pathogenic and/or biomarkers in several autoimmune neurological diseases [1]. For example, autoantibodies directed against voltage-gated potassium channels, the P/Q-type (α1A) voltage-gated
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CYP A is one of
2024-11-22

CYP3A4 is one of the key metabolizing Sabutoclax of the cytochrome P450 (CYP) superfamily of heme-containing monooxygenases. As the CYP family of enzymes plays important roles not only in the xenobiotic metabolism and detoxification of a large number of drugs, but also in the biosynthesis of endoge
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Here we show that the co
2024-11-22

Here, we show that the co-activation of RTKs and non-RTKs is a common trait in treatment-naïve EGFR-mutation-positive NSCLC 67 7 and patients, with AXL and CDCP1 being commonly over-expressed. The combination of gefitinib or osimertinib with the Src/FAK/Janus kinase 2 (JAK2) inhibitor TPX-0005 (Zha
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Necrostatin 1 receptor Small kinase inhibitors have been dev
2024-11-22

Small kinase inhibitors have been developed to block AXL by interacting with the kinase cytoplasmic ATP binding site. Up to date, no AXL selective kinase inhibitors are marketed. As depicted in , some marketed kinase inhibitors such as Bosutinib and Cabozantinib or kinase inhibitors in clinical pha
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Previous studies have demonstrated ATR inhibition is effecti
2024-11-22

Previous studies have demonstrated ATR inhibition is effective for treating cancers combining with chemotherapies in lung adenocarcinoma, gastric cancer, HER2 positive breast cancer and chronic lymphocytic leukemia Alisol A sale to enhance chemotherapy sensitivity [[16], [17], [18],[20], [21], [22]
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c75 br Material and methods br Results br
2024-11-22

Material and methods Results Discussion This study explores the hypothesis that ASK1, via transcriptional upregulation by E2F1, molecularly defines AT that supports a dys-metabolic obese phenotype in humans. We demonstrate associations between increased visceral-AT ASK1 expression and multi
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Glycosylphosphatidylinositol GPI cell wall anchor synthesis
2024-11-21

Glycosylphosphatidylinositol (GPI) rilpivirine sale anchor synthesis pathway is another promising antifungal target. Novel inhibitors of Gwt1 and Mcd4, two enzymes in the GPI anchor pathway were identified by the chemical-genomics-based screening platform CaFT (Candida albicans fitness test) [89].
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