• In addition to the ESIs identified

  2019-09-26

  

  In addition to the ESIs identified that target both EPAC1 and EPAC2, ESI-05 and ESI-07 were identified as compounds that selectively antagonise EPAC2, displaying almost no inhibition of EPAC1 at concentrations up to 100μM [99]. Both compounds were effective inhibitors EPAC2 GEF activity towards Rap1

• br Results br Discussion The ubiquitin system has in recent

  2019-09-26

  

  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

• Downregulation of tumor suppressors is a

  2019-09-26

  

  Downregulation of tumor suppressors is a major factor that leads to tumorigenesis. Phosphatase and tensin homolog deleted on chromosome 10 (PTEN), a common tumor suppressor, the Akt Inhibitor IV kinase of which is often downregulated or even absent in the majority of human cancers, functions as a ph

• In conclusion we demonstrated phenoconversion of CYP A

  2019-09-26

  

  In conclusion, we demonstrated phenoconversion of CYP3A in stable kidney transplant recipients, and that higher plasma indoxyl sulfate concentrations in these subjects may be involved in the phenomenon. The present findings suggest that dose adjustment of drugs metabolized by CYP3A may be needed in

• Several mechanisms are implicated in lipid induced insulin r

  2019-09-26

  

  Several mechanisms are implicated in lipid-induced insulin resistance in muscle, including oxidative stress (Koves et al., 2008, Zhang et al., 2011, Muoio and Neufer, 2012). Mitochondrion is a major source of ROS production. The oxidation of pyruvate and fatty PCI-32765 yielding acetyl-CoA occurs in

• Does hydroxylation of proline have a

  2019-09-26

  

  Does hydroxylation of proline have a specific role in the structure and function of the conotoxins? Several studies in the literature provide insights into the role of proline hydroxylation in the Conus peptides. The consequences of proline hydroxylation on oxidative folding and biological activity

• Initially studies of GPCRs predominantly assessed the

  2019-09-26

  

  Initially, studies of GPCRs predominantly assessed the signalling pathways downstream of receptors on the cell surface. There is now an understanding that GPCRs can localize to and signal from various intracellular compartments, such as the nucleus (reviewed in [40]). These intracellular pools of re

• More than thirty enzymes with PLA activity have

  2019-09-26

  

  More than thirty enzymes with PLA2 activity have been described and, based on sequence similarities, they are currently classified in 16 groups, each containing several sub-groups [16]. However, based on biochemical features these enzymes are frequently grouped into six major families: secreted phos

• br Conclusion br Acknowledgment The authors would

  2019-09-26

  

  Conclusion Acknowledgment The authors would like to thank “Science and Engineering Research Board (SERB) of Department of Science and Technology (DST) Govt. of India” (Grant No.YSS/2015/002017) for funding the project. Introduction Mutations occurring within EGFR exons 18 to 21 are present

• Prenylation may turn a flavonoid from an agonist to

  2019-09-25

  

  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

• The relatively low overall response rates suggest the need

  2019-09-25

  

  The relatively low overall response rates suggest the need for better predictive markers for response. The patient demographics in the SARC trial did not reflect typical Ewing sarcoma demographics as the patients tended to be older and had primarily soft tissue tumors. In addition, although accrual

• br Funding This work was partly supported by the grant

  2019-09-25

  

  Funding This work was partly supported by the grant ‘Maria Grazia Cuccoli’ from Fondazione Cassa di Risparmio di Bologna. Declarations of interest Acknowledgements Introduction The main strategy of oncolytic viral therapy is based on the fact that naturally occurring or engineered virus

• br Experimental Procedure br Acknowledgment

  2019-09-25

  

  Experimental Procedure Acknowledgment This work was supported by Ministry of Education, Singapore (MoE Tier-2) grant (R-154-000-625-112) and R154-000-A72-114 (AcRF Tier 1 grant) respectively. We acknowledge the Advanced Photon Source Beamline 24-ID-C, Argonne National Laboratory, USA. D.N. is

• The important role of miRNAs in cellular

  2019-09-25

  

  The important role of miRNAs in cellular differentiation has been proposed recently. Previous studies had suggested roles for different miRNAs during osteogenesis [20]. Certain miRNAs could promote osteoblast differentiation, such as miR-194 [20], whereas others could inhibit the cell differentiatio

• In the past few years neuroprotection via GLP

  2019-09-25

  

  In the past few years, neuroprotection via GLP-1R activation has been shown in several animal models of stroke, Alzheimer\'s, Parkinson\'s, Huntington\'s, ALS and traumatic CTPB pathway injury. This research field is rapidly growing and several reviews have been recently published (Darsalia et al.,

16022 records 958/1069 page Previous Next First page 上5页 956957958959960 下5页 Last page