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Busulfan Introduction Breast cancer is the most common
2021-09-14
Introduction Breast cancer is the most common cancer among women worldwide, representing 30% of new cancer diagnoses. In addition, it is the second leading cause of cancer deaths among women [1]. With regard to the risk of breast cancer, proper diagnosis and stratification of tumors for individuali
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Most of the GSNOR inhibitors presented here were synthesized
2021-09-13
Most of the GSNOR inhibitors presented here were synthesized according to . The synthesis started from either commercially available ketones or the ketones prepared as described in the . In , condensation of ketone and 2-furanaldehyde provided intermediate in good yield. Furan ring opening of inte
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Previously we reported that the inhibition of PKC and PKC
2021-09-13
Previously, we reported that the inhibition of PKC-ζ and PKC-ε activity in hypertrophic adipocytes had deleterious effects on EPA-induced GPR120-mediated VEGF-A production [12]. However, the activation of PKC-θ, -ζ and -λ can also enhance the phosphorylation of IKK and p65, and facilitate the transl
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In addition to their functional activation of GPR A compound
2021-09-13
In addition to their functional activation of GPR109A, compounds of the pyrazolopyrimidine class also enhanced the binding of nicotinic lobeline to the receptor. For instance, increased the binding of H-nicotinic acid to the receptor (black curve) in a concentration-dependent manner, whereas unlabel
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About epilepsy no specific seizure type has been identified
2021-09-13
About epilepsy, no specific seizure type has been identified because GLUT1-DS is associated with a wide range of epilepsies: patients develop seizures in infancy and early childhood, which are, frequently, do not respond to anticonvulsant medication. In infants, seizures are described as brief, subt
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The widespread involvement of HH GLI in
2021-09-13
The widespread involvement of HH/GLI in human malignancies has initiated a remarkable effort to identify selective HPIs. As shown in Table 2.1, most of these small molecule inhibitors target the essential effector protein SMO, which should lead to pathway abrogation by eventually decreasing the GLIA
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We speculated modulation of redox
2021-09-13
We speculated modulation of redox balance in brain, by activation of GIP receptor pathway. QA is known to mediate production of ROS, lipid peroxidation by its interactions with Fe2+ and formation of QA-Fe2+ complex (Braidy et al., 2010, Rios and Santamaria, 1991, Stipek et al., 1997). QA induces NOS
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EPZ004777 australia Conversely we find that dysfunction
2021-09-13
Conversely, we find that dysfunction in lysosomal-autophagy system observed in human APP and PSEN1 mutant neurons can be reversed by β-secretase inhibition, which reduces the supply of APP-β-CTF to the late endosome and/or lysosome (Jiang et al., 2010). These data argue that accumulation and/or alte
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Clinical trials of all GSIs have ended prematurely
2021-09-13
Clinical trials of all GSIs have ended prematurely, raising the question on our understanding of their target, the γ-secretase/presenilin. Development of compounds to target γ-secretase and reduce Aβ production is complicated by the fact that γ-secretase/presenilin has critical biological function,
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Inflammatory pain is very common in the clinic A
2021-09-13
Inflammatory pain is very common in the clinic. A study demonstrated that galanin was upregulated after nerve injury or inflammation (Ma and Bisby, 1997). It has been reported that galanin plays an important role in the transmission of nociceptive information in the spinal cord of rats with inflamma
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Many investigators have noted structural similarities betwee
2021-09-13
Many investigators have noted structural similarities between certain flavonoids and benzodiazepines, such as diazepam, that are the most widely studied positive modulators of GABAA receptors. Benzodiazepines can act on these receptors via ‘two distinct and separable mechanisms’ (Walters, Hadley, Mo
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TXNIP interacts with various proteins including NLRP Yoshiha
2021-09-13
TXNIP interacts with various proteins, including NLRP3 (Yoshihara et al., 2014, Zhou et al., 2010). Emerging evidence suggests that TXNIP plays a role in ER stress-mediated cell death and in the NLRP3 inflammasome activation step (Abderrazak et al., 2015, Lerner et al., 2012, Oslowski et al., 2012,
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In the present studies we found
2021-09-13
In the present studies, we found that genistein did not antagonize fMLF-induced Ca2+ mobilization in FPR1-HL60 VO-Ohpic trihydrate and human neutrophils. Thus, the previously reported inhibitory effect of genistein on fMLF-stimulated degranulation, aggregation, and reactive oxygen species (ROS) prod
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Factor Xa FXa has emerged as a particularly promising
2021-09-13
Factor Xa (FXa) has emerged as a particularly promising target for the development of effective anticoagulant drugs because FXa acts at the convergence point of the extrinsic and intrinsic coagulation pathways. It efficiently catalyzes the conversion of prothrombin to thrombin with one molecule of F
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Mitochondrial is the main source for
2021-09-13
Mitochondrial is the main source for ROS and ATP generation, and the loss of mitochondrial membrane potential is involved in the alteration of mitochondrial metabolism and mitochondrial failure-induced cell death [33,34]. In this study, we showed that upregulated ZNF32 sustained mitochondrial membra
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