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Despite these efforts to prevent oxidative metabolic degrada
2023-10-20
Despite these efforts to prevent oxidative metabolic degradation, and showed only marginal improvements in metabolic stability and still exhibited high plasma clearances as shown in . High molecular weight as well as relative high log values could be contributing factors to the poor PK profiles of a
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Since pyrrolopyrimidine dithiolanes and both displayed parti
2023-10-20
Since pyrrolopyrimidine dithiolanes and both displayed particularly excellent levels of ACK1 inhibition, these analogs were viewed as potential candidates for further investigation in tumor xenograft experiments. While in vitro metabolic studies indicated that pyrrolidine was predicted to be sign
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br Experimental section br Results and discussion br Conclus
2023-10-20
Experimental section Results and discussion Conclusion In the present study, 3a,8a-dihydroxy-8-oxo-1,3,3a,8a-tetrahydroindeno[1,2-d]imidazol-2(1H)-iminium chloride (3) has been synthesized and characterized by spectral studies and single crystal X-ray crystallography. DFT calculations have
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Application of the broad acting HTR antagonist methiothepin
2023-10-20
Application of the broad-acting 5-HTR antagonist methiothepin (Bard et al., 1996, Hoyer et al., 1994, Peroutka, 1990) converted the TBS-induced response of both thalamocortical and intracortical A1 synapses from LTP to LTD, an effect that was mimicked by the selective 5-HT2R antagonist ketanserin (L
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br Introduction Stroke is a
2023-10-20
Introduction Stroke is a devastating condition that causes cognitive and motor dysfunction, neurodegenerative diseases and even acute death, and is a leading cause of mortality and morbidity worldwide (Chen et al., 2014a, Wang et al., 2016). Thus, exploration or identification of novel therapeuti
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NOXA a BH only protein
2023-10-20
NOXA, a BH3-only protein, is best known as a selective inhibitor of MCL-1, which is a highly expressed pro-survival protein in many human malignancies [30]. In addition, NOXA was recently proven to act as a direct activator via directly binding to BAX to induce apoptosis [31]. Given that its levels
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Aurora A the polar kinase is located at the
2023-10-20
Aurora A the ’polar kinase’ is located at the centrosome and is required for its maturation, division, for the mitotic spindle assembly and entry into mitosis., Mutation or transcriptional silencing of Aurora A impairs centrosome maturation and separation, leads to mono/multipolar spindles, to dela
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Additionally we used the predicted Cyp a b amino
2023-10-20
Additionally, we used the predicted Cyp19a1b amino PYR-41 mg sequence from a number of bony fish species to infer their genetic relatedness and found that R. quelen occupies an ancient position within the Siluriformes group. A phylogenetic tree was constructed and it included both full-length and p
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br Acknowledgements This work was supported in part
2023-10-20
Acknowledgements This work was supported, in part, by NIH grant R01-GM071760. Introduction The MADS box genes encode a eukaryotic family of transcriptional regulators involved in diverse and important biological functions. This class of proteins has been identified in yeasts, plants, insects,
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R406 Introduction It has long been
2023-10-20
Introduction It has long been recognized that angiogenesis is critical to the growth, progression, and metastasis of many solid tumor types [1], and thus, drugs targeting the angiogenic pathway have been a topic of clinical investigation in the oncology community for many years. Angiogenesis is reg
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br Material and methods br Results br Discussion
2023-10-19
Material and methods Results Discussion In order to find new and improved ways of treating type 2 diabetes (T2D) and other related conditions it is vital that investigators gain a more in-depth understanding of the effects that anti-diabetic treatments, such as TZDs, have on molecules impli
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br Animal models of NAFLD Human research has greatly
2023-10-19
Animal models of NAFLD Human research has greatly shaped our understanding of non-alcoholic fatty liver disease, but several limitations exist in studying the disease processes in humans, such as variations in environmental exposure, pre-existing genetic risk factors, racial and ethnic difference
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When arachidonic acid is used
2023-10-19
When arachidonic SLIGKV-NH2 is used as a substrate, the platelet-type 12S-lipoxygenase produces predominantly the 12S-hydroperoxy derivative. In contrast, the leukocyte-type 12S-lipoxygenases generate substantial amounts of the 15-lipoxygenase product in addition to the 12S-hydroperoxy derivative.
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Asparagine synthetase ASNS is a glutamine amidotransferase t
2023-10-19
Asparagine synthetase (ASNS) is a glutamine amidotransferase that catalyzes ATP-dependent synthesis of asparagine and glutamate from aspartate and glutamine. Upregulation of ASNS expression renders leukemia cells resistant to l-asparaginase treatment, and ASNS is essential for cell survival in the a
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APN accounts for of total plasma proteins in
2023-10-19
APN accounts for 0.01% of total plasma proteins in humans; this proportion increases with age to a small extent (Barb et al., 2007). Normal APN levels in the circulation range 3–30μg/mL (Aprahamian and Sam, 2011). APN levels are lower in men than women due to the presence of testosterone and even mo
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