• br Results and discussion br Conclusion We have constructed

  2021-03-24

  

  Results and discussion Conclusion We have constructed a series of potent and greatly selective DPP-4 inhibitors with pyrazolo[1,5-a]pyrimidin-7(4H)-one core surrogates. The modification of the core led us to b2 which has IC50 of 80 nM and > 1000 fold selectivity over DPP-8 and DPP-9. We utiliz

• Impaired dopaminergic systems associated with MA have been

  2021-03-24

  

  Impaired dopaminergic systems associated with MA have been well-documented (Walsh and Wagner, 1992, Kim et al., 1999, Nakajima et al., 2004, Shin et al., 2012, Shin et al., 2017b, Dang et al., 2016, Dang et al., 2017b). Previous reports have suggested that early MA use may be linked to higher risk f

• Some mechanistic experiments performed in the early s

  2021-03-24

  

  Some mechanistic experiments performed in the early 2000s by Ongusaha et al. [78], suggest that DDR1 induction protects apelin receptor from apoptosis in a p53-dependent manner, and that impairment of DDR1 expression or function leads to a pronounced increase of DNA damage-induced apoptosis. This e

• br Materials and methods br

  2021-03-24

  

  Materials and methods Acknowledgements SD was supported by a pre-doctoral research fellowship from the Flanders Agency for Innovation and Entrepreneurship (VLAIO-Flanders, Belgium). YB is supported by a postdoctoral fellowship from Research Foundation Flanders (FWO, Belgium). We thank Isabelle

• In our preliminary evaluation of this series

  2021-03-24

  

  In our preliminary evaluation of this series, we were surprised to discover that SB 431542 was found to bind CSF-1R in a classical DFG-in binding mode (a). Dramatic conformational differences in the juxtamembrane domain and activation loops are apparent when this DFG-in structure is compared with

• br Materials and methods br

  2021-03-24

  

  Materials and methods Results The i.v. administration of urocortin 2 reduced the mean arterial blood pressure in a dose-dependent manner (Fig. 1). The ED50 for the urocortin 2 cumulative dose–response effect on mean arterial blood pressure was 0.014±0.004 mg kg−1. Urocortin 2 administration ha

• Within the BLA both CRF and the CRF receptor have

  2021-03-24

  

  Within the BLA, both CRF and the CRF1 receptor have been shown to functionally regulate synaptic activity. In vivo, CRF release into the BLA originates from projections from the CeA (Roozendaal, Brunson, Holloway, McGaugh, & Baram, 2002). Central administration of both CRF and CRF1 agonists has been

• The CPA parameters of SO were

  2021-03-24

  

  The CPA parameters of SO2 were calculated based on Eq. (11) using the vapor pressure and saturated liquid density data of SO2 over the reduced temperature range of 0.55 to 0.9. All of the data used were taken from the NIST database [53]. The resulting CPA parameters of SO2 are presented in Table S1

• As shown in Figs a and b with

  2021-03-24

  

  As shown in Figs. 3(a) and (b), with the SO effect, the absolute values of the VDEs change by at most 0.19eV. Table 1 also shows that the observed peak splitting energies in the Sm-Ho complexes were reproduced even without the SO effect. Considering its significant importance in the electronic struc

• The two SNPs rs rs presented

  2021-03-23

  

  The two SNPs rs4818-rs4680 presented above are part of the haploblock (rs6269, rs4633, rs4818, rs4680) presenting the 3 major haplotypes which influence the enzymatic activity of COMT. This activity is inversely related to the sensitivity of pain in a chronic pain syndrome; so the haplotype (GCGG)

• br Study design br Results

  2021-03-23

  

  Study design Results We enrolled 50 subjects awaiting SOT (15 kidney, 14 liver, 1 liver + small bowel, 11 lung, 9 heart) and 50 controls (Table 1) who were similar with respect to median age (subjects 49.1 yrs., controls 48.6 yrs.) gender (64% male subjects and controls), and CMV-seropositivit

• Of all ES cases approximately are metastatic

  2021-03-23

  

  Of all ES cases, approximately 26–28% are metastatic diseases at diagnosis with the remainder being localized disease [14]. Instituting a systemic chemotherapy regimen in combination with surgery and/or radiotherapy has significantly increased the survival of patients with localized disease. The 5-y

• PI K is a lipid

  2021-03-23

  

  PI3K is a lipid kinase and generates phosphatidylinositol-(3,4,5)-trisphosphate, which is a second messenger critical for the translocation of Akt to the cytoplasmic membrane. The phosphorylation of Ser473 Akt is important in the cell survival by regulating the eNOS among other targets (Dimmeler et

• Inappropriate heme metabolism has been linked

  2021-03-23

  

  Inappropriate heme metabolism has been linked to several neuropsychiatric disorders. In the hippocampi of Alzheimer's disease (AD) patients, for example, heme was found to binds intracellular amyloid β (Aβ), resulting in reduced heme bioavailability and its functional deficiency (Atamna and Frey, 20

• In another study Nutlin a mediated p

  2021-03-23

  

  In another study, Nutlin-3a-mediated p53 activation induced strong negative impact on NF-κB signaling in LPS-stimulated neutrophils and macrophages [34]. Nutlin-3a limited cellular immune response to LPS, partly by attenuating DNA binding activity of NF-κB and impairing transcription of its target c

15466 records 668/1032 page Previous Next First page 上5页 666667668669670 下5页 Last page