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Small kinase inhibitors have been developed to block AXL by
2024-10-08
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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We demonstrate a role for
2024-10-08
We demonstrate a role for low oxygen to regulate ATX mRNA in hepatocyte-derived HuH7 cathepsin inhibitors and human liver slices, consistent with reports of increased ATX expression in a variety of tumours that are frequently hypoxic. Importantly, we show a positive association between elevated ATX
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br Introduction Lipoxygenases LOXs are a heterogeneous
2024-10-08
Introduction Lipoxygenases (LOXs) are a heterogeneous family of enzymes that catalyze the peroxidation of polyunsaturated fatty acids (PUFAs). By oxidizing free PUFAs, they were shown to contribute to the generation of various bioactive lipid mediators. However, LOX-mediated oxidation of PUFAs es
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Citral or dimethyl octadien al
2024-10-08
Citral or 3,7-dimethyl-2,6-octadien-1-al is a mixture of two stereoisomeric monoterpene aldehydes (the trans isomer geranial, citral A (40–62%)) and the cis isomer neral, citral B (25–38%) and serves one of the main constituent of essential oils of C. citratusis used in cosmetic, food, fungicides, p
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The first evidence in supporting the hypothesis
2024-10-08
The first evidence in supporting the hypothesis that MAS receptors mediate the effects elicited by AT1 antagonists was provided by Iwai et al. (2012). The authors found that AT1 receptors triggers neointima formation after polyethylene-cuff placement around mouse femoral artery by reducing local AC
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The numbers and types of molecules needing
2024-10-03
The numbers and types of molecules needing to be transported across membranes are very large, and there is a corresponding very large and diverse number of transporters expressed throughout the body. Hundreds of proteins that have been assigned as having transporter function are broadly divided into
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HT modulates cortical and hippocampal pyramidal cell functio
2024-10-03
5-HT modulates cortical and hippocampal pyramidal cell function in a very complex manner, since most 5-HT receptor subtypes (excitatory as well as inhibitory) are expressed on pyramidal 2-nbdg as well as GABAergic interneurons that exert inhibitory control over pyramidal cells (Leiser et al., 2015,
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A highly attenuated B pertussis
2024-10-03
A highly attenuated B. pertussis strain, named BPZE1, has recently been described [10]. It produces enzymatically inactive pertussis toxin (PT), no dermonecrotic toxin and only trace amounts of tracheal cytotoxin. Markedly reduced lung pathology was observed in mice intranasally (i.n.) infected with
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The activation of P Rs
2024-10-03
The activation of P1Rs modulates the activity of many ion channels and receptors (Sebastião and Ribeiro, 2009) and the recent detection of P1Rs at the postsynaptic level of the adult NMJ (Garcia et al., 2014) makes potentially possible an adenosine-mediated modulation of the nicotinic Schisandrol B
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Our initial approach to identify
2024-10-03
Our initial approach to identify hits was two-pronged and included a high-throughput screening (HTS) campaign of the OSI Neochlorogenic acid library as well as a virtual screening (VS) campaign, utilizing a publically available crystal structure of ACK1 (PDB code: ). A tolerance for protein flexibi
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AMPK is an essential player in adiponectin signaling pathway
2024-09-30
AMPK is an essential player in adiponectin signaling pathway that regulates energy metabolism. The fact that suppression of AMPK activity by compound C largely diminished candesartan-mediated inhibition of NFκB via blocking AT1 also suggests that the AT1-mediated effect is at least partly resulted f
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In the previous study we demonstrated the importance
2024-09-30
In the previous study, we demonstrated the importance of the mPFC postsynaptic 5-HT1A receptor in the sustained antidepressant effects, because a sustained antidepressant effect was obtained with intra-mPFC injection, but not systemic injection of 8-OH-DPAT, a 5-HT1A receptor agonist (Fukumoto et al
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br Methods br Results and discussion
2024-09-30
Methods Results and discussion Conclusions Acknowledgements The authors thank Dr. Francois Alhenc-Gelas (then INSERM U367, Paris, France), who kindly provided the plasmid for truncated soluble recombinant human ACE – WTΔ, Dr. Elena Arablinskaya (Institute of Phtiziopulmonology, Moscow, R
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br Patients and Methods br Results br Discussion Gjerdrum et
2024-09-30
Patients and Methods Results Discussion Gjerdrum et al showed that Axl Poly(A) tailing kit for in vitro transcription is required to maintain the mesenchymal-like invasiveness of metastatic breast carcinoma cells, but Axl knockdown has no effect on the cell proliferation of MDA-MB-231 cell
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br Materials and methods br Results br Discussion Recent
2024-09-30
Materials and methods Results Discussion Recent studies have highlighted proteinase function and autophagy as novel targets for the treatment of liver fibrosis [7,14]. In this study, we demonstrated that catalpol protected the rat liver from CCl4-caused injury and fibrogenesis in vivo and
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