• The first rationally designed dual mPGES LO inhibitor was

  2024-05-21

  

  The first rationally designed dual mPGES-1/5-LO inhibitor was reported in 2008 and represents a structural derivative of pirinixic KT 5720 - a synthetic agonist of PPARα with lipid-lowering properties (Koeberle et al., 2008b). Further α-alkyl- and α-aryl-substituted derivatives have been synthesized

• Our co IP data show that

  2024-05-21

  

  Our co-IP data show that 5HT1A or 5HT2A receptors do not heterodimerize with mGluR1α receptors. Given that both 5-HT and mGlu receptors are GPCRs and produce anxiolytic effects, a degree of cooperativity via a functional cross-talk may still exist between these receptors [11]. In addition to the fun

• Compounds are representatives of an array

  2024-05-21

  

  Compounds – are representatives of an array of MBG targets (, ) related to imidazole standard that were synthesized and initially tested in a rat CYP17 lyase screening assay (). The inhibitors were synthesized as racemates by coupling of 6,7-dimethoxy-naphthalene-2-isopropyl ketone with the requisi

• PF also a dual Aurora A and Aurora B

  2024-05-21

  

  PF-03814735, also a dual Aurora-A and Aurora-B inhibitor, was administered in a phase I dose escalation study in a 3-weekly pimaricin for 5 or 10 consecutive days [69], [70]. To date 25 patients have been included in 7 dose levels (5–100mg/day for 5 days). Using the 5-day schedule the MTD was defin

• Anisomycin Two parallel branches of the

  2024-05-21

  

  Two parallel branches of the DNA damage-dependent S-phase checkpoint are thought to co-operate by inhibiting distinct steps of DNA replication. One branch includes the phosphorylation of structural maintenance of chromosomes 1 (SMC1), a cohesin that is activated by ATM or ATR after IR treatment or r

• Our results clearly demonstrate that inhibition of

  2024-05-21

  

  Our results clearly demonstrate that inhibition of ATM pathway activation results in resistance to Vγ2Vδ2 T cell-mediated cell death. Therefore, enhancing ATM activation along with Vγ2Vδ2 T cell treatment would promote the cytotoxicity of resistant ovarian cancer cells. To our knowledge, this is the

• Then Autodock was employed for site directed docking

  2024-05-21

  

  Then, Autodock4.2 was employed for site directed docking on AD with the ligands of the cluster(s) having high binding affinities in VS II experiment (Morris et al., 2009). Docking protocols were followed as per our earlier report with 200 GA (genetic algorithm) run (Kalani et al., 2015). Likewise, l

• Mitochondrial dysfunction resulting from mtDNA abnormalities

  2024-05-21

  

  Mitochondrial dysfunction resulting from mtDNA abnormalities may trigger retrograde signaling pathways from the mitochondrion to the nucleus, which regulate the expression of genes involved in diverse cellular processes, including metabolism, stress responses, tumor progression, nutrient sensing, li

• It is noticed that MDL only

  2024-05-21

  

  It is noticed that MDL-28170 only partly reversed isoflurane-induced AIF release and nuclear translocation. In addition to calpain mechanism, activation of the DNA repair enzyme poly (ADP-ribose) polymerase-1 (PARP-1) is also essential for AIF release (Culmsee et al., 2005; Moubarak et al., 2007), a

• br Physiology of the apelin pathway br

  2024-05-21

  

  Physiology of the apelin pathway Role of apelin in heart disease Both apelin and apelin receptor null mice manifested moderate reduction in cardiac contractile function under basal conditions and their exercise capacity was markedly reduced (Table 1) [56]. Apelin has direct effects on the prop

• In order to further explore whether

  2024-05-21

  

  In order to further explore whether the cytoprotective effect of isogarcinol against oxidative stress in H2O2-induced HepG2 PP 3 is a consequence of the breakdown of the endogenous antioxidant defence mechanism, we measured the LDH release, MDA levels, GSH levels and SOD activity. A large body of e

• There are increasing repeated reports of amphotericin

  2024-05-21

  

  There are increasing repeated reports of amphotericin B-resistance in pathogenic fungi including Candida spp. [35], [36]. Nolte et al. characterized some fluconazole and amphotericin B-resistant Candida albicans isolates from leukemia patients [37]. Fan-Havard et al. (1991) have shown multi-antifung

• Another hypothesis is angiogenesis inhibition Angiogenesis i

  2024-05-21

  

  Another hypothesis is angiogenesis inhibition. Angiogenesis is a process that involves the growth, migration and differentiation of endothelial Tamoxifen to form new blood vessels. Angiogenesis favorably influences tumor growth and also influences tumor invasion of vessels, resulting in tumor metas

• Our research group has been involved

  2024-05-21

  

  Our research group has been involved by many years in the synthesis of new 2,3-benzodiazepin-4-ones (e.g. 1, Fig. 1) and in the characterization of their mechanism of action.15, 16, 17 Within the development of these compounds, we demonstrated that an improvement of AMPAR antagonism by 2,3-benzodiaz

• HsALDH enzyme has been purified

  2024-05-21

  

  HsALDH enzyme has been purified for the first time in our laboratory from human saliva and has been kinetically characterized using different aromatic substrates [35]. Also, the effect of some common substances frequently encountered by the enzyme in the oral cavity (such as ethanol, hydrogen perox

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