• A highly attenuated B pertussis strain named BPZE has

  2023-11-04

  

  A highly attenuated B. pertussis strain, named BPZE1, has recently been described [10]. It produces enzymatically inactive pertussis toxin (PT), no dermonecrotic toxin and only trace amounts of tracheal cytotoxin. Markedly reduced lung pathology was observed in mice intranasally (i.n.) infected with

• In conclusion we have demonstrated that diaryl pyrazolo pyri

  2023-11-04

  

  In conclusion, we have demonstrated that ,-diaryl-1-pyrazolo[3,4-]pyrimidine-3,6-diamines represent a novel class of ACK1 inhibitors. The presence of a polar substituent at C-4 of the N-6 aryl ring was shown to be unnecessary for maintaining high levels of inhibitory activity. Furthermore, selectivi

• The most potent compounds within the current series of compo

  2023-11-03

  

  The most potent compounds within the current series of compounds were therefore , , , , and , with PKI 14-22 amide, myristoylated possessing the best selectivity towards the lyase reaction in comparison to the hydroxylase reaction, indeed, this compound was found to possess an IC value of 1210nM

• ML355 Moreover showed reduction in fibroblast growth factor

  2023-11-03

  

  Moreover, showed 73% reduction in fibroblast growth factor–induced neovascularization in a mouse corneal micropocket assay at a dose of 100mg/kg and 50% reduction at 50mg/kg. Both results were highly statistically significant (PML355 have recently shown only moderate efficacy (40% inhibition) in

• Ticlopidine HCl Having established the structural requiremen

  2023-11-03

  

  Having established the structural requirements for potency in both the biochemical and biomarker (CRA) assays, we evaluated key compounds in the metabolic stability assay. Disappointingly, we found that all compounds had high intrinsic clearances in mouse microsomes. To ascertain whether the in vitr

• Having taken a step back from affinity

  2023-11-03

  

  Having taken a step back from affinity to gain better exposure and solubility, we started work to replace the unstable oxazolinone, and address the selectivity over the hERG channel. Keeping in mind the binding mode of the series from crystal structures, triazole was identified as another mildly aci

• In our H K ATPase assay Fig and Supplementary

  2023-11-03

  

  In our H+, K+-ATPase assay (Fig. 1 and Supplementary Fig. 1), myricetin (IC50 = 0.58μM) was more potent than acid-activated omeprazole (IC50 = 1.50μM). In contrast, in oral administration in mice (Fig. 3), omeprazole (20mg/kg) more effectively inhibited gastric regulator of g protein signaling secr

• Protein phosphorylation is an important posttranslational me

  2023-11-03

  

  Protein phosphorylation is an important posttranslational mechanism for the regulation of distribution, trafficking, and function of modified proteins (Wang et al., 2014). GluA1 phosphorylation at S845 also has functional consequences (Lu and Roche, 2012). For instance, S845 phosphorylation drove tr

• Wound healing without blastema formation causes

  2023-11-03

  

  Wound healing without blastema formation causes partial restoration of lost tissue, and gives rise to fibrotic scars. Healing by fibrotic scarring rather than by regeneration leads to tissue dysfunction, and can place a huge burden for the health of the animal [4]. Therefore, understanding the molec

• br Materials and methods br Results

  2023-11-03

  

  Materials and methods Results Discussion In this study, we administrated BDE-153 to newborn rat pups at PND 10 and cultured primary neurons, measured neuronal apoptosis and LDH activity in vivo and in vitro, then explored the possible predominant pathway underlying the neuronal apoptosis by

• Acarbose The contractility index showed positive inotropic e

  2023-11-03

  

  The contractility index showed positive inotropic effects of apelin in both doses at min 5 (Fig. 3, Fig. 5). Although the mean arterial pressure did not recover to the baseline, the contractility index increased, the relaxation index (tau) and ±dp/dt max returned back to their baseline, and left ven

• To further address the mechanism of Didox s suppressive effe

  2023-11-03

  

  To further address the mechanism of Didox’s suppressive effects on mast cell activation, FceRI receptor Brefeldin A and downstream transcription factor induction were assessed. We found that Didox had no effect on FceRI surface expression, and thus concluded that Didox effects must be occurring dow

• In Pham et al employed the microsphere based

  2023-11-03

  

  In 2014, Pham et al. [22] employed the microsphere-based technology to create a Luminex probe-based assay for the rapid identification of single nucleotide polymorphisms that are known to confer resistance to one or more echinocandins in C. glabrata. The targets for the FKS probes were generated usi

• According to the phytochemical screening Lophira procera is

  2023-11-03

  

  According to the phytochemical screening, Lophira procera is rich in phenolic compounds including total polyphenols, total flavonoids, tannins and proantocianidins. It has been reported that there is a correlation between total polyphenol content and antioxidant activity [29]. The present invention

• Some of the earliest LOX inhibitors

  2023-11-03

  

  Some of the earliest 12-LOX inhibitors were redox inhibitors, including nordihydroguaiaretic CCG 203971 (NDGA), BW 755C, and baicalein 48, 49, 50. Redox inhibitors block the oxidation of the nonheme iron at the cataylytic site, preventing its conversion from the inactive (Fe2+) to the active (Fe3+)

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