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Fosaprepitant Steroidal CYP inhibitors can further
2023-07-26

Steroidal CYP17 inhibitors can further be classified based on their mode of action, namely as mechanism-based inhibitors and type I and type II competitive inhibitors [129]. Recent studies investigated other biological targets than CYP17, and some new compounds have shown interesting dual activity a
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In conclusion we have designed
2023-07-26

In conclusion, we have designed and synthesized a series of 4-phenyl-thiazole analogues as potent ATX inhibitors. Total twenty-five compounds were synthesized and evaluated for their inhibitory activity on ATX using FS-3 and human plasma assays. Compound was found to be the most potent derivative p
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Zacopride hydrochloride br Materials and Methods br Author C
2023-07-26

Materials and Methods Author Contributions Conflicts of Interest Acknowledgments This study was funded by the NIH Common Fund (UH2TR000943) through the Office of Strategic Coordination/Office of the NIH Director, an NCI/NIH grant (1R21CA199050), the MD Anderson Cancer Center support gran
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br Acknowledgements We would like to thank Dr Thomas Blanpie
2023-07-26

Acknowledgements We would like to thank Dr. Thomas Blanpied, Sai Sachin Divakaruni, Dr. Helmut Kessels, Feline Lindhout, Dieudonnée van de Willige, and all members of the MacGillavry lab for discussions and critical reading of the manuscript. This work was supported by NWO (ALW-VENI 863.13.020, A
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Previously we have detected the expression of APJ receptor
2023-07-26

Previously, we have detected the expression of APJ receptor on stomach projecting histone demethylase inhibitor in DMV, in addition, icv administration of apelin-13 induced a remarkable c-Fos activation in those cells which were previously marked by a retrograde neuronal tracer fast blue (Birsen et
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The objectives of this study were to investigate the
2023-07-26

The objectives of this study were to investigate 1) the mRNA and protein expression of apelin and APJ in porcine ovarian follicles of different sizes, and their immunolocalization and concentrations in follicular fluid and ovarian follicle, and 2) the direct effect of recombinant human apelin-13 on
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It has been demonstrated that the hallmarks of
2023-07-26

It has been demonstrated that the hallmarks of pulmonary fibrosis are a loss of endothelial function and subsequent activation of the immune system, which is considered as a direct outcome affected by intracellular pro-inflammatory responses [26]. Thus, inhibition of early inflammation could be an i
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br Funding This work was supported
2023-07-26

Funding This work was supported by the National Natural Science Foundation of China (grant No. 81573664). Thanks to Jing-xian Yang from the Pharmacology Laboratory of Liaoning University of Traditional Chinese Medicine for support with technology and experimental equipment. Disclosure Confl
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The activity of MMPs is regulated
2023-07-26

The activity of MMPs is regulated at the level of gene transcription or by the enzymatic activation of latent enzymes. Inflammatory cytokines such as interleukin (IL)-1β, tumor necrosis factor (TNF)-α and IL-6 are elevated in synovial fluid, synovium and cartilage in patients with OA, and these cyto
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br Introduction The term antioxidant derives from
2023-07-26

Introduction The term antioxidant derives from the prevention of the oxygen consumption. In the late of 19th centuries, antioxidants were generally used in industrial processes such as against to metal corrosion, vulcanization of rubber. Later on, the use of antioxidants to prevent the rancidity
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br Conflict of interest br Acknowledgments This work was
2023-07-26

Conflict of interest Acknowledgments This work was financially supported by the Fund Project of Sichuan Provincial Department of Education (16ZB0053), the Scientific Research Foundation of Sichuan Agricultural University (No. 06021400) and the China Postdoctoral Science Foundation (No. 2015M58
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It has been proposed that a PrP pathogenic mechanism
2023-07-26

It has been proposed that a PrP pathogenic mechanism is a toxic gain of function secondary to the misfolding of mutated PrP. However, such a mechanism might not apply to all mutant PrP species, since some mutations had little effect on the stability and folding kinetics of PrP (Swietnicki et al., 19
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We found that decreased Ng
2023-07-26

We found that decreased Ng levels lead to a lower threshold for LTD induction at L4–L2/3 synapses. Previous studies in hippocampal slice culture have shown that LTD at individual synapses induces spine elimination at both the targeted synapse and selective neighboring synapses when spines are monito
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br Guava tea leaves inhibit leukocyte type lipoxygenase acti
2023-07-26

Guava tea leaves inhibit leukocyte-type 12-lipoxygenase activity Guava tea that is extracted from guava leaves contains a number of polyphenols, and is commonly taken as a dietary supplement. The extracts show a variety of beneficial effects such as antioxidative, anti-inflammatory and antiprolif
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These findings suggest that eventually more than one lipoxyg
2023-07-26

These findings suggest that eventually more than one 12/15-lipoxygenase isoform may play a role in human atherosclerosis. Humans have two 12-lipoxygenases and two 15-lipoxygenases which show different expression patterns, substrate specificities and stereo-selective metabolism [1]. However, in PI3K
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