• Prenylation may turn a flavonoid from an agonist to an

  2019-09-10

  

  Prenylation may turn a flavonoid from an agonist to an antagonist and improve the selectivity to both ERs depending on the position of the substitution. C-8 prenylation appears to promote antagonism to a larger extent than C-6 in ERα due to steric hindrance against generation of agonistic conformati

• br Discussion The present results demonstrate that high

  2019-09-10

  

  Discussion The present results demonstrate that high dose estrogen–progestogen OC treatment produced impaired glucose tolerance and glucose tolerance was preserved during low dose estrogen–progestogen, high or low dose progestogen-only OC use. The study also shows that impaired glucose tolerance

• br Transparency document br Acknowledgements We thank

  2019-09-10

  

  Transparency document Acknowledgements We thank Prof. Barbara Brodsky for valuable comments and discussion. We thank the support of the Tufts start-up fund and the Knez Family Faculty Investment Fund for Y.-S. L, and the Tufts Summer Scholar program for E.C. Introduction Discoidin domain r

• Ademetionine and br Results br Discussion The ubiquitin syst

  2019-09-10

  

  Results Discussion The ubiquitin system has in recent years become an exciting area for drug discovery (Cohen and Tcherpakov, 2010), as multiple enzymatic steps within the ubiquitylation process are druggable. The potential of targeting the ubiquitin-proteasome pathway was first demonstrated i

• br Discussion and conclusion Ubiquitination and deubiquitina

  2019-09-10

  

  Discussion and conclusion Ubiquitination and deubiquitination have emerged as important mechanisms involved in p53 management. This review revealed that various DUBs can regulate p53 or p53-Mdm2-MdmX networks. Herein, we reviewed the current progress made toward elucidating the complexities in th

• As illustrated in Table monocyclic acid analogs were synthes

  2019-09-09

  

  As illustrated in Table 3, monocyclic DPP4 Activity Fluorometric Assay Kit analogs were synthesized and evaluated. 2-Oxido-3H-1,2,3,5-oxathiadiazol analog 8 showed 15-fold less potent EP1 receptor affinity relative to 2b, while it showed 2.2-fold more potent antagonist activity. Oxadiazole-5-one ana

• In contrast to AChE BuChE Table

  2019-09-09

  

  In contrast to AChE, BuChE (Table 2) exhibited a measurable time-dependent inactivation only with Ro 31-8220 pathway 2 among the four acetophenones in this study. Values of Ki obtained from steady-state inhibition of BuChE by all four acetophenones were, as noted in the Results, 10- to 200-fold gre

• Data from immunohistochemical detection of CIC revealed that

  2019-09-09

  

  Data from immunohistochemical detection of CIC-3 revealed that the immunostaining of CIC-3 can be present both in hepatocarcinoma and its matched normal controls though; CIC-3 was, on the whole, significantly elevated in hepatocarcinoma relative to its paired normal control. In consideration of the

• Chk and Chk are functionally redundant protein kinases that

  2019-09-09

  

  Chk1 and Chk2 are functionally redundant protein kinases that respond to checkpoint signals emanating from the phosphatidylinositol 3-kinase family members ATM (ataxia-telangiectasia mutated) and ATR (Ataxia-telangiectasia and Rad-3 related). A concerted research effort has revealed many mechanistic

• br Materials and methods br Results

  2019-09-09

  

  Materials and methods Results Discussion For many years, oral PDE5-Is have been prescribed as an on-demand regimen for treating ED. Several studies have reported on the efficacy and safety of such a regimen, with an overall efficacy rate of 60–70% [21]. However, many patients complain of a

• phospholipase a2 inhibitor Methods br Results br Discussion

  2019-09-09

  

  Methods Results Discussion In this study we make the novel observation that villin-1 and gelsolin are down-regulated in response to diverse cellular stressors, including bacteria associated with the pathogenesis of CD. The high plasticity and dynamics of the phospholipase a2 inhibitor cytosk

• Torin 2 Similar to EGFR another receptor tyrosine

  2019-09-09

  

  Similar to EGFR, another receptor tyrosine kinase (RTK), fibroblast growth factor receptor 4 (FGFR4), is gaining attention in the lung cancer setting. The protein expression of this receptor has been recently associated with a negative impact on lung cancer prognosis, supporting the idea that FGFR4

• While oxysterols were most extensively studied for its

  2019-09-09

  

  While oxysterols were most extensively studied for its potent ability to mediate feedback regulation of cholesterol biosynthesis, some early investigations showed that the enzymes involved in its syntheses were highly upregulated in macrophages and dendritic cells—an indication of possible roles in

• Multi subunit RING type E ligases

  2019-09-09

  

  Multi-subunit RING-type E3 ligases are exemplified by the CULLIN-RING-ligase (CRL) and the anaphase-promoting complex/cyclosome (APC/C) [19]. CRLs constitute the biggest family of other multi-component E3 ligases. These consist of a cullin scaffold protein (CULLIN 1, 2, 3, 4A, 4B, 5, 7), a substrate

• In general cellular senescence is considered a programmed

  2019-09-09

  

  In general, cellular senescence is considered a programmed response to stress that can be activated by oxidative stress, irradiation or action of substances or drugs. These stressors cause DNA damage and, through the action of specific proteins (p53 and p21), lead to cell senescence (di Fagagna, 200

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