• This structure guided the variation

  2019-08-08

  

  This structure guided the variation of the compounds aiming either at enhanced interaction with CK1 or to exclude interaction with CK1 (R=Me, 15). We chose the 5-cloro substituted oxoindole as backbone as it is supposed to show enhanced metabolic stability, which is commonly used in medicinal chemis

• Endothelin appears to have direct effects on neoplastic cell

  2019-08-08

  

  Endothelin 1 appears to have direct effects on neoplastic Digoxigenin-11-dUTP by inducing cellular proliferation, angiogenesis, migration, invasion, and inhibition of apoptosis [10]. Endothelin 1 mediates mitogenic effects in some epithelial tumors such as colorectal, ovarian, and prostate cancers

• br STAR Methods br Acknowledgments We would like to

  2019-08-08

  

  STAR★Methods Acknowledgments We would like to thank Dr. Tsung-Ping and Dr. Shang-Yi Tsai, National Institute on Drug Abuse, NIH for sharing protocols on pulse chase experiments and analysis. We would like to thank Dr. William G. Telford for his valuable input on Amnis flow cytometry experiment

• To study the effect of DDR inhibition by

  2019-08-08

  

  To study the effect of DDR inhibition by imatinib, nilotinib and dasatinib in a cellular environment we generated DDR1 and DDR2 expressing HEK293 cell lines by stable transfection. Of the five DDR1 splice variants we focused on the 1b variant whose over-expression has been associated with pulmonary

• To assess whether the described cooperation between the EGFR

  2019-08-08

  

  To assess whether the described cooperation between the EGFR and FGFR receptors was relevant at the clinical level, we determined the effect on progression-free survival of FGFR1 expression in patients with adenocarcinoma who were receiving erlotinib or gefitinib. As we had observed EGFR-FGFR1 coope

• Within the availability of large number of experimental data

  2019-08-07

  

  Within the availability of large number of experimental data, it is easy to develop the relation between the mechanical strength and corrosive resistance of the RHA added cement concrete. The developed correlation is given in the following Eq. (4.8). This equation can be used to predict any of the p

• In this study the ASTM

  2019-08-07

  

  In this study, the ASTM C1260 and ASTM C1567 test methods were followed to conduct the ASR tests. Three mortar bars were prepared using three types of RHA (600-RHA, 150-RHA, and 44-RHA) and CFA. To prepare the mortar bars, the OPC was replaced by each type of RHA for 10% and 20%, respectively by wei

• There is a considerable molecular genetic heterogeneity with

  2019-08-07

  

  There is a considerable molecular genetic heterogeneity within ES/PNET. As mentioned above, either or can rearrange with in these gene fusions. Furthermore, for either gene fusion, additional heterogeneity stems from the location of the genomic breakpoints of the translocation, resulting in differen

• A possible explanation for these

  2019-08-07

  

  A possible explanation for these observations has been provided by a recent study showing that EWS-FLI-1 increases the Skp2-mediated 26S proteasome degradation, decreasing p27 protein stability and preventing cell senescence [42]. Mechanism of action of EWS-FLI-1 Molecular analysis has revealed

• ABT-869 br Target enzyme attributes and substrate peptide se

  2019-08-07

  

  Target enzyme attributes and substrate peptide selection Protein kinases catalyze the phosphorylation of serine, threonine, and tyrosine residues in both proteins and peptides using ATP as the phosphoryl donor. The human kinome is comprised of 518 protein kinases and 40 lipid kinases. The vast ma

• br Particle swarm optimization for NLBP

  2019-08-07

  

  Particle swarm optimization for NLBP Computational tests Conclusions Acknowledgements This work was supported by the State Key Development Program for Basic Research of China (No. 2009CB421104) and the National Natural Science Foundation of China (Nos. 50809004 & 41071323). Main Text

• Introduction The Discoidin Domain Receptors

  2019-08-07

  

  Introduction The Discoidin Domain Receptors (DDRs), comprising DDR1 and DDR2, are collagen-binding receptor tyrosine kinases (RTKs) that function as microenvironmental sensors at the interface of the extracellular matrix and the intracellular signal transduction machinery [1]. In response to ligand

• Proteolysis by CPs is crucially important

  2019-08-07

  

  Proteolysis by CPs is crucially important for cereal seed development and germination. However, these enzymes must be tightly controlled. Pre-harvest sprouting is a phenomenon in which the control of CPs is disrupted. This disruption manifests in the premature synthesis and activation of CPs, leadin

• br Results and discussion br Conclusions An optimization stu

  2019-08-07

  

  Results and discussion Conclusions An optimization study of the dipeptidyl enoates was performed by chemical structure modifications (Fig. 5). Compound FGA50 displaying R configuration at C-3 was more active than its epimer FGA40. Two modifications of the chemical structure of FGA50 were done:

• During the course of our research on mGlu

  2019-08-07

  

  During the course of our research on mGlu PAMs,, the hydroxyacetophenone scaffold was found to possess dual mGlu PAM and CysLT1 antagonism activity, presumably as orthosteric antagonist (). There is currently an increasing interest in drug discovery to explore multitarget drugs or polypharmacology

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