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br Development of lorlatinib from crizotinib to
2024-11-28
Development of lorlatinib from crizotinib (1) to a clinical candidate (6) Xalkori (1, PF-02341066, crizotinib), was the first-in-class ALK inhibitor approved by the Unites States Food and Drug Administration (FDA) in 2011 as a first-line treatment for ALK+- NSCLC patients. This section describes
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Pituitary adenylate cyclase activating polypeptide
2024-11-27
Pituitary adenylate cyclase-activating polypeptide (PACAP) is a member of the secretin/growth hormone-releasing hormone (GHRH)/vasoactive intestinal peptide (VIP) family, with potent anti-inflammatory and potent cytoprotective properties [[6], [7], [8], [9], [10], [11], [12], [13]]. PACAP exists as
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Toxicity is the main reason for
2024-11-27
Toxicity is the main reason for the failure at all stages of the new drug development process. The major part of safety-related attrition occurs at preclinical phases while predicting preclinical safety liabilities earlier in the drug development process. This strategy enables the design and/or sele
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Search sphere This sphere includes the acetylcholine binding
2024-11-27
Search sphere 1: This sphere includes the Eribulin mesylate binding site between the α–γ subunits. The center point of the search area was located at x=35.26, y=77.67, z=137.74 and the initial search radius was set to 27Å which assures that the corresponding area outside the channel pore of the two
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A promising target that is involved
2024-11-27
A promising target that is involved in the biosynthesis of the precursor LTA4 is the 5-LO-activating protein (FLAP), which in vivo is seemingly indispensable for LT formation [8], [9]. FLAP, a member of the MAPEG family (membrane-associated proteins in eicosanoid and glutathione metabolism), is an i
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br Conclusions br Conflicts of interest br Acknowledgements
2024-11-27
Conclusions Conflicts of interest Acknowledgements This work was supported by Ege University Research Fund [BAP, 14-ECZ-030, 2016]. Introduction The interest in the effects of endocrine disrupting chemicals (EDCs) in the aquatic environment continues to increase over the past decade, sp
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The SKOV and SKOV TR cells were exposed
2024-11-27
The SKOV3 and SKOV3TR Atazanavir were exposed to stepwise increased concentration of paclitaxel with or without a different concentration of autophagy inhibitor (3-MA or HCQ) to further evaluate whether suppression of autophagy affected the growth and drug sensitivity of ovarian cancer cells in vitr
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In the present study we
2024-11-27
In the present study we sought to decipher the role of ATP-citrate lyase and of the mitochondrial NADH-dependent Mae in the oleaginous yeast Y. lipolytica. Indeed, although this yeast is one of the major models for lipid metabolism, the function of these enzymes is still not clear. As the study of t
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This project was funded by the
2024-11-27
This project was funded by the University of the Philippines Diliman through the Natural Sciences Research Institute with grant No. CHE-09-2-02. Introduction There is compelling evidence for an anti-inflammatory effect of 12- and 15-lipoxygenases through the generation of lipid mediators involve
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Oocytes from the African clawed
2024-11-27
Oocytes from the African clawed frog Xenopus laevis have been widely used as an expression system to study the modulation of NMDA receptors by metabotropic receptors, such as metabotropic glutamate receptors [12], μ opioid receptors [13], insulin receptors [14] and serotonin receptors [15]. No data
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We found a protective effect of the GTCC haplotype against
2024-11-27
We found a protective effect of the GTCC haplotype against ED, which is reflected by its association with increased IIEF in patients with clinical ED. Further studies are required to determine the functional implications of these genetic markers combined in specific haplotypes blocks. Indeed, we fou
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In addition to calpain I activity cathepsin activities have
2024-11-27
In addition to calpain I activity, cathepsin activities have been proven to be linked to apoptotic signaling. Cathepsin B and cathepsin D are two of the most abundant and well-investigated lysosome acid-dependent proteases that are involved in the apoptotic regulation (Ferri & Kroemer, 2001). Cathep
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Recently whey products have been added to
2024-11-27
Recently, whey products have been added to nutritional beverages to boost their antioxidant capacity. Supplementation of a lemon drink with 1% WP hydrolyzed by subtilisin increased the antioxidant activity of the beverage from 0.75 to 7.79 mmol of TE/L (Athira et al., 2014). In addition, a flavored
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br Materials and methods br Conflict of
2024-11-26
Materials and methods Conflict of interest Acknowledgments We thank Christine Heiner (Department of Surgery, University of Pittsburgh) for her critical reading of the manuscript. This work was supported by grants from the US National Institutes of Health (R01GM115366, R01CA160417, and R01CA
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br Introduction There are greater
2024-11-26
Introduction There are greater than five million Americans living with Alzheimer's dementia and more than 35 million people worldwide [1], and without a way to stop or slow the progression, there will be nearly a tripling of individuals affected by 2050 (13.8 million) [1]. The urgency to develop
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