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Matthew et al synthesized and carried out SAR
2024-08-05

Matthew et al. synthesized and carried out SAR studies of imidazo-[1,2-a]-pyrazine as Aurora kinase inhibitors with enhanced kinase selectivity and found that cmk 39 showed optimal potency on Aurora-A and Aurora-B with IC50 value of 4 nM and 13 nM while on phosphorylation histone H3 (pHH3), EC50 wa
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HBX 41108 synthesis br Disclaimer Statement br Acknowledgmen
2024-08-05

Disclaimer Statement Acknowledgments Introduction Metabolic changes are a common feature of cancerous tissues. Mutations in oncogenes and tumor suppressor genes cause alterations to multiple intracellular signaling pathways that rewire tumor cell metabolism and re-engineer it to allow enhan
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This study evaluated the anti
2024-08-05

This study evaluated the anti-tumor influences of LA against HepG2 Stattic in vivro, and investigated the molecular mechanisms of inducing apoptosis. Overall, our studies suggested that LA is a promising anti-cancer drug and a possible novel therapeutic agent directed toward the mitochondrial-mediat
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Oxaprozin Recently two distinct small molecule
2024-08-05

Recently, two distinct small-molecule inhibitors of PHGDH were identified using high-throughput screens, both of which inhibit de novo serine biosynthesis and show selective toxicity to cancer Oxaprozin with high SSP flux [50,51]. The inhibitor NCT-503, which has an IC50 of 2.5μM, reduces the growth
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According to average serum fat content of g
2024-08-05

According to average serum fat content of 6.9 g/L (Phillips et al., 1989) and serum dioxin level from individuals exposed to dioxins as the result of accidents in Seveso (Needham et al., 1997), Taiwan (Guo et al., 2004) and Vietnam (The Tai et al., 2011) the median serum concentration of TCDD would
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We stimulated HNEpC cells with
2024-08-05

We stimulated HNEpC cells with LPS found that the secretion of inflammatory cytokines and the expression of AHR was increased significantly, and miR124 was reduced. It has been found that LPS as a foreign substance can bind to the TLR family of proteins to activate intracellular AHR signaling [[19],
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The relatively high concentration of HT used in this
2024-08-03

The relatively high concentration of 5-HT used in this study (100 µM) is consistent with the concentrations used in other published ex vivo studies (Ropert and Guy, 1991, Passani et al., 1994, Shen and Andrade, 1998). In our paradigm 5-HT was focally applied at the surface of the slice via a fast pe
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Desipramine hydrochloride synthesis Song et al reported seri
2024-08-03

Song et al. reported series of 1,2,3-triazolylsalicylamide derivatives and screened over kinase panel and found compound 31 as most potent which inhibited Aurora-A, specifically with IC50 of 0.37 μM. Compound 31 was about 10-fold more active for Aurora-A than for Aurora-B (IC50 = 3.58 μM reported se
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Sodium valproate PGR regulation of epithelium stroma crossta
2024-08-03

PGR regulation of epithelium–stroma crosstalk is proven by numerous studies that utilize genetically engineered mouse models. Before embryo implantation, epithelial PGR mediates the progesterone signal to transcriptionally increase the Ihh levels 13, 15. Epithelial IHH then activates the stromal hed
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Neuropathic animals display increased sensitivity
2024-08-03

Neuropathic animals display increased sensitivity to the anti-nociceptive effect of baclofen and whilst the number and affinity of GABAB corticosterone in the dorsal horn are not altered (Smith et al., 1994; Zemoura et al., 2016), GABAB receptors subunits (B1 and B2) are both down-regulated in senso
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On the other hand our study permits
2024-08-03

On the other hand, our study permits to draw general conclusions about the complex functional pattern of C4HT, C8HT and C12HT, in comparison with the parent molecule HT and two reference compounds like Trolox and vitamin E. Table 1 summarizes the results obtained in the present investigation (for th
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Recently the FDA approved the first blood
2024-08-03

Recently, the FDA approved the first blood-based test for the detection of EGFR mutations in non-small cell lung cancer patients (http://www.fda.gov) (Voelker, 2016). This allows detection of specific, recurrent mutations, which can help the selection of the patients that could benefit from Erlotini
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Cell surface metalloproteases coordinate signaling
2024-08-02

Cell surface metalloproteases coordinate signaling during development, tissue homeostasis, and disease. A disintegrin and metalloprotease 17 (ADAM17) is a well-characterized member among ADAM family, which mediates the cleavage of various cell surface proteins (Black, 2002, Black et al., 1997, Dello
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Through systematic deletion of AhR in specific cell
2024-08-02

Through systematic TH-302 of AhR in specific cell types, Di Meglio et al. (2014) revealed that AhR in keratinocytes and fibroblasts are key to the exacerbated psoriatic phenotype induced by IMQ in AhR-deficient mice. This emphasizes the crosstalk between keratinocytes and the immune system to regul
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IU1 Adiponectin also works on AdipoR
2024-08-02

Adiponectin also works on AdipoR1, inducing extracellular Ca2+ influx necessary for activation of Ca2+/calmodulin-dependent protein kinase kinase (CaMKK)β, AMPK (Fig. 1). This step is then followed by activation of SirT1 and increased expression and decreased acetylation of PPARγ coactivator (PGC)-1
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