• Compounds were screened for their activity against

  2020-07-01

  

  Compounds were screened for their activity against the hERG channel, with the 2,3-Cl compounds more active here than the 2,4-F compounds. The homopiperazine examples (, , , ) showed increased hERG activity relative to the corresponding piperazines. The cell data for the 6,7-dimethoxyquinoline compo

• We have previously disclosed the discovery of a azaindole ac

  2020-07-01

  

  We have previously disclosed the discovery of a 7-azaindole-3-acetic SCH 23390 hydrochloride receptor CRTh2 antagonist chemotype 1 from HTS and its subsequent optimization to give 2 as a potent and orally bioavailable inhibitor of eosinophil shape change (SC) in human whole blood. Subsequent to dis

• Collectively these data suggest the potential clinical utili

  2020-07-01

  

  Collectively, these data suggest the potential clinical utility of COMT inhibitors for the treatment of addiction disorders. Similar to current pharmacotherapies such as naltrexone, tolcapone\'s effects were not ethanol specific, therefore tolcapone may be effective in reducing other drug reinforced

• apomorphine receptor br Acknowledgements br Introduction Pro

  2020-07-01

  

  Acknowledgements Introduction Protein–tyrosine phosphorylation, catalyzed by protein–tyrosine kinases and protein–tyrosine phosphatases, has a pivotal role in the regulation of a wide variety of cellular processes. Similar numbers of tyrosine kinases and tyrosine phosphatases are encoded by th

• The Fontan circulation When first

  2020-07-01

  

  The Fontan circulation When first described in 1971, the Fontan operation ushered in a new paradigm in the care of children born with the varied forms of complex congenital AEBSF mg disease (CHD) characterized by a single effective pumping chamber.1., 2. This procedure, which creates a total cavopu

• Cetylpyridinium Chloride br Non cyclic nucleotide EPAC regul

  2020-07-01

  

  Non-cyclic nucleotide EPAC regulators Despite the success of 007 as a tool molecule, few studies to date have led to the identification of further EPAC-selective agonists. The most studied and controversial group of small-molecule EPAC regulators are the sulfonylurea (SU) family. SUs (Table 1) su

• atrial natriuretic peptide receptor br Activatable optical i

  2020-07-01

  

  Activatable optical imaging probes Optical fluorescence imaging, which directly detects photons emitted from fluorescent probes, has become as a powerful analytical method to study biological processes both in vitro and in vivo. It is characterized by high sensitivity, is free of radioactive irra

• First of all it should

  2020-07-01

  

  First of all, it should be emphasized that, although cPLA2α manifests a marked selectivity for phospholipids that contain AA at the sn-2 position, this does not mean in any way that, in cells, the enzyme cannot hydrolyze other fatty acyl residues to a significant extent even if this occurs at a lowe

• Our study provides proof of principle

  2020-07-01

  

  Our study provides proof of principle for dimerizing two different E3 ligases as a novel approach to inducing one ligase to degrade the other one. The outcome of ‘ligase versus ligase’ PROTAC-mediated activity might be unpredictable a priori, but could reveal a new mechanism for proximity-mediated h

• pd0332991 All DGKs have at least

  2020-07-01

  

  All DGKs have at least two cysteine-rich regions homologous to the C1A and C1B motifs of PKCs [26]. In theory, these domains may bind DAG, perhaps localizing DGKs to where DAG accumulates. However, no DGK C1 domain has so far been conclusively shown to bind DAG. In fact, structural predictions sugge

• In this context we initiated a program to

  2020-07-01

  

  In this context, we initiated a program to develop new antiviral chemotypes towards a host factor implicated in Pam2CSK4 replication: the host (human) dihydrofolate reductase (DHFR) [21]. We recently identified this enzyme as the molecular target of 1-aryl-4,6-diamino-1,2-dihydrotriazines, structur

• 1-NM-PP1 Another breakthrough towards the understanding

  2020-06-30

  

  Another breakthrough towards the understanding of the mechanisms responsible for stress-induced relapse to drug seeking behaviour is the evidence published by the group of Wise [34] in which they show that the activation of VTA CRF2 and not CRF1 receptors is responsible for stress-mediated relapse t

• Recently Zhao et al have

  2020-06-30

  

  Recently, Zhao et al. have been carried out a study to investigate the relationship between eNOS-4b/a polymorphism and the risk of LCPD in a Chinese population. Their results demonstrated that eNOS polymorphisms may be involved in the etiology of LCPD. However, the number of studies conducted to exa

• DUBs are involved in cell cycle regulation and

  2020-06-30

  

  DUBs are involved in Valinomycin australia regulation and DNA damage pathways and since, in cancer and different stress conditions all the proteins which regulate cell cycle and DNA damage/repair are either up/down regulated (Singh et al., 2013, Singh et al., 2011, Kumar and de Massy, 2010, Gupta e

• br Materials and methods br Acknowledgments This

  2020-06-30

  

  Materials and methods Acknowledgments This research was supported by funding from University of California Irvine to H.U.B. Introduction Oral squamous cell carcinoma (OSCC) is the fourth major cause of mortality among men in Taiwan and its incidence rates continue to rise annually. OSCC is

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