• Testosterone can be converted into estrogens by aromatase ac

  2023-11-06

  

  Testosterone can be converted into estrogens by aromatase action. Aromatase is encoded by CYP19, belongs to cytochrome P450 superfamily, and synthesizes estradiol (E2) and estrone (E1) from testosterone and androstenedione respectively (Fig. 1). Aromatase is expressed in the ORS of anagen hair folli

• It has been reported that trehalose shows beneficial

  2023-11-06

  

  It has been reported that trehalose shows beneficial effects in a mouse model of several neurodegenerative diseases [21], [22], [23]. There are also reports showing that trehalose can improve the impaired cognitive and learning ability and reduced Aβ deposit in hippocampus of APP/PS1 transgenic mice

• br Discussion Mycobacterium tuberculosis infection is a main

  2023-11-06

  

  Discussion Mycobacterium tuberculosis infection is a main threat to mankind, with one third of the world population being infected. [9] Over nine million new cases of tuberculosis and two million deaths from this disease occur yearly worldwide. [10] The rising incidence of tuberculosis over the l

• nisoldipine As in humans and other mammalians spontaneous ac

  2023-11-04

  

  As in humans and other mammalians spontaneous activity of sinoatrial pacemaker nisoldipine in in the zebrafish heart crucially depends on proper HCN4 channel activity (If) and spontaneous diastolic depolarization [15,81]. Whether Na+/K+-ATPase currents regulate next to phase of myocardial repolariz

• The LOX hydroxide metabolites are converted to

  2023-11-04

  

  The 15-LOX hydroxide metabolites are converted to secondary lipid mediators such as lipoxin A4 from 15-HETE and protectin D1/resolvin D1 from 17-HDoHE [45] (Fig. S3). Importantly, all of these secondary lipid mediators have anti-inflammatory and pro-resolving properties [46], [47], [48]. Lipoxin A4

• The current study was designed to

  2023-11-04

  

  The current study was designed to investigate the effects of the 12/15-LOX inhibitor, LOXBlock-1 (LB1) in mice using a FeCl3-induced distal MCAO model, and to test its utility in conjunction with subsequent thrombolysis with tPA, which is to date the only FDA-approved drug for acute stroke treatment

• Imaging QTL studies may have

  2023-11-04

  

  Imaging QTL studies may have several potential advantages over case-control studies, including increased power . Imaging endophenotypes of disease in QTL studies can separate patients and normal subjects more accurately and therefore limit the confound of including asymptomatic subjects in the contr

• The role of circulating physiologic concentrations of FGF in

  2023-11-04

  

  The role of circulating physiologic concentrations of FGF21 in glucose metabolism, however, remains unclear. Circulating FGF21 levels in obese and diabetic rodents, and in patients with type 2 diabetes are significantly higher than those in controls without diabetes [4], [5], [6]. On the other hand,

• 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

15551 records 194/1037 page Previous Next First page 上5页 191192193194195 下5页 Last page