• AP was originally described as

  2024-12-16

  

  AP-1 was originally described as a heterodimer of the bZIP proteins c-Jun and c-Fos. The experiments described here showed that stimulation of TRPV1 channels induced the expression of both of these classical constituents of AP-1. The essential role of both proteins was analyzed in a series of experi

• Although the gene that encodes DHFR has

  2024-12-16

  

  Although the gene that encodes DHFR has been strongly conserved during evolution, subtle differences in the active sites of bacterial, human and parasite Tariquidar have been exploited to develop DHFR inhibitors specific to particular pathogens 1, 3. For example, pyrimethamine and cycloguanil bind s

• br Experimental section br Acknowledgements This work

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  Experimental section Acknowledgements This work was funded by the Italian Association for Cancer Research (AIRC IG18590 to A.A.), by “Fondi di Ateneo-University of Pisa” years 2009 and 2010 (E. N., S. N., E. O., and A. R.) and partially by the Unipi project P.R.A.2016_27 (E. N., E.O. and A. R.

• In mice the Tfm mutation increased

  2024-12-16

  

  In mice, the Tfm mutation increased the anxiety-state assessed in the novel object and in light/dark box tests, whereas no changes were detected in the open field or elevated plus maze tasks (Zuloaga et al., 2008). As for Tfm rats, this seemed to be related to an increased HPA response to stress. Th

• Whereas allostery in the cell is relatively understudied sig

  2024-12-16

  

  Whereas allostery in the β cell is relatively understudied, significant progress has been made in understanding the physiology and mechanistic biology of how AMPK and its upstream kinases govern β cell function. LKB1 phosphorylates AMPKα at Thr172 [21], and loss of LKB1 in β cells abolishes phosphor

• Since the cloning of ARs in the beginning

  2024-12-16

  

  Since the cloning of ARs in the beginning of the 1990s, the efforts to characterize them have led to the accumulation of a substantial amount of experimental data. Decades of site-directed mutagenesis (SDM; Box 1) studies, in combination with pharmacological data and computational modeling, have pav

• The assay performance was estimated using Z factors

  2024-12-16

  

  The assay performance was estimated using Z′-factors (plotted in Fig. 2A) according to Zhang et al. calculated for each plate comparing positive (in the absence of an inhibitor) and negative controls (in the presence of an AdK inhibitor). The mean Z′-factor±SD was determined to be 0.7±0.1, indicativ

• In conclusion two novel series of furo pyrimidin

  2024-12-13

  

  In conclusion, two novel series of furo[2,3-]pyrimidin4-amines and 7-pyrrolo[2,3-]pyrimidin-4-amines which exhibit potent in vitro inhibitor activity against ACK1 have been identified and evaluated. 1,3-Dithiolane-substituted pyrrolopyrimidine displays excellent ACK1 cellular inhibition, good kinas

• This study was funded and supported by Tehran University

  2024-12-13

  

  This study was funded and supported by Tehran University of Medical Sciences and Health Services; and Iran National Science Foundation. Introduction The enzyme acetylcholinesterase (AChE) plays a central role in the signal transduction in the nervous system, hydrolyzing the neurotransmitter acet

• In this study in an effort

  2024-12-13

  

  In this study, in an effort to explore the possible role of 5-HT6 receptors in mediating the memory-enhancing effects of YL-0919, we first assessed the memory-enhancing effects of YL-0919 in the Morris water maze, object recognition test and step-down passive avoidance task. In addition, we then inv

• The reductase activity in patients with OHD as

  2024-12-13

  

  The 5α-reductase activity in patients with 21-OHD, as assessed by the 5α-THF to 5β-THF (ratio 3) and by the 5α-17HP to 17HP (ratio 4) ratios, showed a similar pattern of activities (Fig. 2A–C) and significant correlations (ratio 1 vs. ratio 3; rs=0.67; pprolyl hydroxylase to the 5α-reducase activit

• We demonstrate a role for

  2024-12-13

  

  We demonstrate a role for low oxygen to regulate ATX mRNA in hepatocyte-derived HuH7 Physostigmine hemisulfate and human liver slices, consistent with reports of increased ATX expression in a variety of tumours that are frequently hypoxic. Importantly, we show a positive association between elevated

• br Conflict of interest br Introduction

  2024-12-13

  

  Conflict of interest Introduction Ovarian cancer is the most lethal gynecological malignancy, and ranks as the fifth leading cause of cancer death among women. The American Cancer Society estimates that about 22,280 new ovarian cancer cases and 14,240 deaths will occur in the United States in

• Ryoichi et al modified potent clinical

  2024-12-13

  

  Ryoichi et al. modified potent clinical candidate VX-680 (6) with 3-cyano-6-(5-methyl-3-pyrazolamino)pyridine as Aurora kinase inhibitor. Substituted cyano pyridine derivative (7) inhibited proliferation of HCT-116 cells with an IC50 value of 115 nM. It showed tumor inhibition in mice model at a dos

• br Materials and methods br Results br Discussion Numerous

  2024-12-13

  

  Materials and methods Results Discussion Numerous studies showed that Na+-K+-ATPase activity and membrane multidrug resistance transporter were decreased in cardiac tissue subjected to IR (Belliard et al., 2013; Lee et al., 2013). In return, treatment that alleviated the progress of IR-rel

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