• br Materials and methods br

  2023-12-20

  

  Materials and methods Results Discussion In the present study, we aimed to elucidate the contribution of adenosine receptors to vascular tone in mice with T1D. We showed that diabetes resulted in decreased A1 adenosine receptor-mediated contraction in the aorta, which was accompanied by inc

• Though we have proved that

  2023-12-20

  

  Though, we have proved that VA could suppress hepatic gluconeogenesis, the mechanisms of VA on gluconeogenesis in vivo and in vitro remain unclear. AMP-activated protein kinase (AMPK), which is called an energy receptor enzyme, is widely expressed in liver and other tissues [23]. AMPK has become ano

• HT modulates cortical and hippocampal pyramidal cell functio

  2023-12-19

  

  5-HT modulates cortical and hippocampal pyramidal cell function in a very complex manner, since most 5-HT receptor subtypes (excitatory as well as inhibitory) are expressed on pyramidal orexin antagonist as well as GABAergic interneurons that exert inhibitory control over pyramidal cells (Leiser et

• Later the same group designed and prepared several steroidal

  2023-12-19

  

  Later, the same group designed and prepared several Δ16-steroidal C17 benzoazoles and pyrazines and evaluated their CYP17 and 5α-reductase inhibitory activities, binding to and transactivation of the AR, as well as their antiproliferative effects against two human PC cell lines (LNCaP and LAPC4) [18

• 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

• 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

• 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,

• 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

• 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

• 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

• 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

• 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

• 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

• 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

• 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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