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Over the past decade extensive
2023-12-19
Over the past decade, extensive research has been directed toward the discovery of Aurora-selective small-molecule inhibitors. As a result, a handful of Aurora inhibitors has been identified. Among them, 1 (VX-680) and 2 (SNS-314) have entered human clinical trials as pan-Aurora kinase inhibitors (F
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6-Aminonicotinamide Cancer cells manifest characteristic abn
2023-12-19
Cancer 6-Aminonicotinamide manifest characteristic abnormal growth properties accompanying clonal evolution of cells displaying progressively increasing genomic instability capable of invasion and metastasis to distant organ sites. With the emerging knowledge about the role of known oncogene and tum
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br Conclusion This is the first report
2023-12-19
Conclusion This is the first report to show that treatment of lung cancer cell lines, A549 and H1299, with ovatodiolid stimulates intracellular reactive oxygen species generation and induces DNA damage. Subsequently activates ATM/ATR and CHK1/2 signaling pathway, inhibits CDC25C and p21WAF1/CIP1,
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Limitations of this study include the use
2023-12-19
Limitations of this study include the use of HL-1 cardiomyocytes, which show different characteristics than primary cardiomyocytes [56]. Furthermore, sustained TAC in Ampkα1-deficient mice did not favorably influence cardiac function [33]. It must be kept in mind that global Ampkα1-deficiency may af
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Regarding progression free survival analyzing clinical trial
2023-12-19
Regarding progression free-survival, analyzing 12 clinical trials, we demonstrated that the use of antiangiogenic treatment results in a statistically longer PFS with a pooled HR of 0.76 (95% CI 0.65–0.89, pLP533401 hcl mg of improvement of PFS only is that after antiangiogenic therapy glioblastoma
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To elucidate this relationship we developed a
2023-12-19
To elucidate this relationship, we developed a spatial model of Ca-influx through N-methyl-D-aspartate receptor (NMDAR), CaMKII/PP1 activation, and AMPAR insertion in a realistic spine geometry. Using this model, we show that i) variables in membrane voltage mediated Ca-influx, particularly the numb
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Accumulating evidence indicates that experience
2023-12-19
Accumulating evidence indicates that experience-dependent alterations in glutamate transmission in the NAc, such as those produced by repeated exposure to cocaine, involve alterations in postsynaptic signaling mediated by AMPA-type receptors (Pierce and Wolf, 2013, Wolf and Ferrario, 2010). In the N
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CA-074 Me Through an extensive SAR optimization campaign
2023-12-19
Through an extensive SAR optimization campaign with the 4-((2-hydroxy-3-methoxybenzyl)amino)-benzenesulfonamide-based scaffold researchers have developed ML355 ((N-benzo[d]thiazol-2-yl)-4((2-hydroxy-3 methoxybenzyl)amino)benzenesulfonamide) [5]. ML355 is a nonreductive, noncompetitive, reversible 12
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Imatinib was first approved for the treatment of
2023-12-19
Imatinib was first approved for the treatment of Philadelphia chromosome positive chronic myelogenous leukemia in 2001 [25]. This first approved small molecule antagonist is quite unusual in that it provides a durable response that lasts for more than a decade in the majority of patients. Imatinib h
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We further analyzed selected hit compounds
2023-12-18
We further analyzed selected hit compounds for their ability to inhibit human AdK in intact cells. Human 1321N1 astrocytoma NS-398 were utilized which were found to express AdK. The whole cell assay was performed using a 96-well format. The standard AdK inhibitor 5-iodotubercidin was employed as a
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Since the localization of LO depends on
2023-12-18
Since the localization of 5-LO depends on phosphorylation, we also analyzed the phosphorylation profile of 5-LO-WT and all isoforms by Western blot using specific Rottlerin against the phosphorylation sites S271 and S523. Whereas phosphorylation at S271 activates the 5-LO, inhibits nuclear export a
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br LOX in esophageal cancer Various studies suggest
2023-12-18
5-LOX in esophageal cancer Various studies suggest that abnormal levels of AA metabolites play an essential role in human esophageal adenocarcinogenesis (EAC). The key AA derivatives of 5-LOX signaling molecules namely include, 5-HETE, LTB4, and cysteinyl LTs, which are well-known to initiate inf
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Drug resistance development often involves structurally un r
2023-12-18
Drug resistance development often involves structurally un-related drugs and, specifically both conventional and targeted agents. IGROV-1/Pt1 SEW 2871 are characterized by resistance to cisplatin and reduced sensitivity to inhibitors of EGF-R and MEK, the up-stream activator of ERK1/2, associated w
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Endoplasmic reticulum ER stress resulting
2023-12-18
Endoplasmic reticulum (ER) stress resulting from accumulation of misfolded proteins in ER lumen stimulates a chain of adaptive responses termed as the unfolded protein response (UPR). Glucose related protein (GRP78/BiP), key ER chaperone essential for the activation of the ER-transmembrane signaling
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In the current study SA was assessed to confirm the
2023-12-18
In the current study, SA was assessed to confirm the safety of CS addition to erythrocytes SA as well as SA elicits antioxidant action. It has been reported that, ROS induced desialylation by depletion of SA content from cell surfaces (Pawluczyk et al., 2014, Harisa, 2015). Therefore, significant de
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