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br Therapeutic advantages and clinical implications of
2024-10-19
Therapeutic advantages and clinical implications of caffeine treatment in ROP The demonstration of the role of the adenosine receptor in development of ROP and protection by caffeine suggests two potential therapeutic strategies with high translational potential: a) modification of caffeine treat
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Among the enzymes involved in adenosine metabolism adenosine
2024-10-19
Among the enzymes involved in adenosine metabolism, adenosine kinase plays an important role in regulating formation and release of endogenous adenosine in cardiomyocytes as well as vascular endothelial cells Decking et al., 1997, Kowaluk et al., 1998, Smolenski et al., 1994. Inhibition of adenosine
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br Conflict of interest br Financial
2024-10-19
Conflict of interest Financial support Acknowledgments This work was supported by the Japanese Millennium project. We thank all members of the Center for Genomic Medicine of RIKEN and Dainippon-Sumitomo Pharma Co., Ltd. for supporting this study. We are also grateful to members of the Hiros
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The reaction of LOX with unlabeled AA generated products fro
2024-10-19
The reaction of 5-LOX with unlabeled AA generated products from hydrogen abstraction at C7 (95% 5-HETE) with minor products derived from abstraction at C10 (5% 8-HETE). With 7,7--AA the selectivity remained skewed towards C7 hydrogen abstraction (59%) compared to C10 hydrogen abstraction products (4
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Thus one possible target for
2024-10-19
Thus one possible target for CRPC treatment is the enzyme 17,20-lyase, which plays a crucial role in androgen biosynthesis. This is because inhibition of 17,20-lyase would be expected to decrease serum androgen levels secreted not only by the testes but also by the adrenal glands.7, 8, 9 In recent
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PF also a dual Aurora A and Aurora B inhibitor
2024-10-19
PF-03814735, also a dual Aurora-A and Aurora-B inhibitor, was administered in a phase I dose escalation study in a 3-weekly LY335979 for 5 or 10 consecutive days [69], [70]. To date 25 patients have been included in 7 dose levels (5–100mg/day for 5 days). Using the 5-day schedule the MTD was define
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The acidification of endocytic compartments is closely relat
2024-10-19
The acidification of endocytic compartments is closely related to endocytic activity, although the mechanism linking acidification and membrane dynamics is largely unknown. In a recent RNA interference (RNAi)-based screen, V-ATPase depletion blocked the formation of clathrin-coated vesicles, an effe
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Phagosomes acquire some hydrolases early
2024-10-19
Phagosomes acquire some hydrolases early during their journey from the cell surface to lysosomes. An example for such hydrolase is cathepsin H which is most concentrated in the early phagosome at a pH of approximately 6.3 (Claus et al., 1998), the pH optimum of enzyme activity (Schwartz and Barrett,
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While it is known that circulating LDL
2024-10-19
While it is known that circulating LDL-C levels are largely regulated by either controlling the rate of hepatic production of its triglyceride-rich precursor VLDL particle or the rate of LDLR-mediated LDL particle clearance [58], it should be noted that important differences exist between rodents an
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br Discussion Herein we demonstrate that mice
2024-10-19
Discussion Herein, we demonstrate that mice deficient in L-12/15 LO are more sensitive to 3-NP-induced toxicity although a substantial individual variability in striatal lesion size in response to 3-NP in both genotypes was observed. This variability is not atypical; several studies demonstrate s
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Our research is the first to report that administration
2024-10-19
Our research is the first to report that administration of HMW-HA is an effective strategy to defend against PM2.5-induced disruption of pulmonary epithelial barrier and lung injury, and addresses that HMW-HA restricts PM2.5-induced epithelial apoptosis through reducing oxidative stress and followin
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However one should keep in mind that these
2024-10-19
However, one should keep in mind that these results may not reflect exactly in vivo antioxidant activity. Many other issues such as absorption, metabolism and physicochemical properties of different antioxidants must also be considered (Prior et al., 2007, Wu et al., 2004). Some research groups are
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br Angiogenesis as a critical event
2024-10-18
Angiogenesis as a critical event in diabetic retinopathy Angiogenesis refers to the abnormal proliferation of blood vessels during various pathological conditions. It acquires the stature of being one of the most detrimental events responsible for the progression of diabetic retinopathy. Angiogen
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estriol br Materials and methods br
2024-10-18
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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The lactam emerged as lead candidate
2024-10-18
The lactam (6) emerged as lead candidate due to its high selectivity, outstanding potency (against ALK or in clinically known ALK mutants), low in vitro clearance, and low efflux potential. The lactam (6) was selected for further profiling against the resistant ALK mutants. Preclinical rat pharmacok
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