• To develop novel EPAC inhibitors Zhou and co

  2020-02-27

  

  To develop novel EPAC inhibitors, Zhou and co-workers optimized the HTS hit as the chemical lead. After modifications of the substituents on the phenyl ring or C6-position of compound , compound () was identified to be the more potent compound in this series with an IC value of 4.0µM (EPAC2). Dock

• br Materials and methods br Results br

  2020-02-27

  

  Materials and methods Results Discussion Endothelial cells are crucial for both vascular homeostasis and protecting the vasculature against atherogenic insults [3]. OxLDL-mediated injury to endothelial cells is crucial for endothelial dysfunction in the pathogenesis of atherosclerosis and a

• On the other hand the interaction of the Kaempferia

  2020-02-27

  

  On the other hand, the interaction of the Kaempferia parviflora extract with CYP3A was uncompetitive with a low Vmax value. In the in vivo study, the Kaempferia parviflora extract did not interfere with CYP3A activity throughout the entire duration of treatment. This is fortunate as CYP3A isoforms a

• Our study showed that parental morphine

  2020-02-27

  

  Our study showed that parental morphine exposure in the adulthood is associated with an increased tendency toward morphine consumption in F1 but not F2 male offspring. Thus, it seems that trans-generational effects of parental morphine consumption disappear in the second generation. In support of ou

• Dgat mice however had less adipose tissue as reflected

  2020-02-27

  

  Dgat−/− mice, however, had less adipose tissue, as reflected by lower total fat pad weights and body triglyceride content. Because of these findings, we hypothesized that, although Dgat−/− mice could make triglycerides through non-DGAT pathway(s), their triglyceride synthesis capacity might not be e

• bcr-abl tyrosine kinase inhibitors br Fragment based drug di

  2020-02-27

  

  Fragment-based drug discovery (FBDD) is a powerful method to discover drug leads and has been widely adopted in both academia and industry. FBDD can be used to explore chemical bcr-abl tyrosine kinase inhibitors space with libraries which are smaller in size, producing drug leads with high ligand

• Introduction Cyclin dependent kinases CDKs are a

  2020-02-27

  

  Introduction Cyclin dependent kinases (CDKs) are a family of proline-directed serine/threonine kinases with roles in regulation of crucial cellular processes such as AR-42 HDAC and transcription [1]. One of the unifying features of this family is its dependence on association with cyclins/cyclin-l

• br Discussion In depression an

  2020-02-27

  

  Discussion In depression, an activation of the inflammation process and production of cytokines (including chemotactic cytokines – chemokines) and their receptors may occur due to the stimulation of the immune system. One of the earliest studied and described cytokines in depression is interleuki

• Intriguingly one E residue may serve

  2020-02-26

  

  Intriguingly, one E2 residue may serve as a molecular ‘gate’ to allow the C-terminus of ubiquitin to access the closed E2~Ub conformations favorable for ubiquitin transfer. This residue, Asp87 in UbcH5 family members, resides on one side of the opening that leads to the active site Cys (Fig. 4D). In

• br Results and Discussion br Experimental

  2020-02-26

  

  Results and Discussion Experimental Procedures Acknowledgments The ubiquitin–proteasome system (UPS) is important for biological processes such as protein degradation and protein function regulation. In general, poly-ubiquitinated proteins are degraded by proteasomes, and some proteins ac

• Upstream Stimulatory Factor USF binding to the

  2020-02-26

  

  Upstream Stimulatory Factor (USF) binding to the −65 E-box is required for the regulation of FAS promoter activity in fasting/feeding [97], [98]. DNA-PK are identified as a USF-interacting protein [99]. In response to feeding/insulin, the transient double-stranded DNA breaks occurred during the tran

• The possibility that a carboxyl group attached to the

  2020-02-26

  

  The possibility that a carboxyl group attached to the or position of an -arylaminomethylenemalonate ester would lead to increased selectivity for DHODH has been tested and found not to be the case. Indeed, reduced selectivity compared with the corresponding ester is observed and is attributed to a

• ac 723 In the present study we combined activity based

  2020-02-26

  

  In the present study, we combined activity-based protein profiling, biochemical and genetic approaches to identify the PLCPs involved in the sphingolipid pathway leading to plant PCD. By using Arabidopsis ac 723 and leaves, we demonstrate that this sub-class of plant proteases is activated in respo

• Introduction The Bromeliaceae family is

  2020-02-26

  

  Introduction The Bromeliaceae family is one of the most morphologically and ecologically diverse flowering plant families native to the tropics and subtropics of the New World (Benzing, 2000). They comprise >3000 species and are traditionally divided into three subfamilies: Pitcairnioideae, Bromeli

• In summary our findings show that LPS can

  2020-02-26

  

  In summary, our findings show that LPS can activate CysLT2R on microglial signaling to induce microglial inflammation and microglia-dependent neuronal death. Furthermore, pharmacological inhibition or knocking down of CysLT2R expression protects neurons against neurotoxicity via suppression of LPS-

15926 records 864/1062 page Previous Next First page 上5页 861862863864865 下5页 Last page