• Molecular docking study of compound was performed using the

  2020-06-05

  

  Molecular docking study of 15-deoxy-Δ-12,14-Prostaglandin J2 was performed using the Schrödinger Small-Molecule Drug Discovery Suite taking advantage of known X-ray crystal structures of activated EPAC2 protein. The model shows that compound occupies the CBD of EPAC2 and forms hydrogen bonds with

• Emphysema is an important component of COPD

  2020-06-05

  

  Emphysema is an important component of COPD, which is responsible for airflow limitation. In the present study, a significant airspace enlargement was observed 21 days after elastase administration. Interestingly, daily administration of olaparib provided greater protection against emphysema as comp

• In this study we were able derive

  2020-06-05

  

  In this study, we were able derive new insights into the biology of DDR2 including the demonstration that cellular tyrosine phosphorylated proteins co-localise with DDR2 and exogenously added collagen I (Fig. 1G). This finding suggests that similar to the focal adhesion complexes associated with int

• Due to the high attractiveness of E and E ligases

  2020-06-05

  

  Due to the high attractiveness of E2 and E3 ligases as drug targets, a number of drug discovery assays have been published, based on detection by fluorescence (Dudgeon et al., 2010, Krist et al., 2016, Zhang et al., 2004), Malotilate synthesis (Davydov et al., 2004, Huang et al., 2005, Kenten et al

• br Restenosis after angioplasty remains a remarkable challen

  2020-06-05

  

  Restenosis after angioplasty remains a remarkable challenge, although drug-eluting stents have reduced the incidence of restenosis considerably . Vascular smooth muscle BX-912 (VSMCs) play a pivotal role in the development of intimal thickening and restenosis. VSMCs proliferate and migrate from t

• Egr together with catecholamine biosynthetic enzymes such as

  2020-06-05

  

  Egr1, together with catecholamine biosynthetic enzymes, such as tyrosine hydroxylase (TH), dopamine β-hydroxylase (DBH), and phenylethanolamine N-methyltransferase (PNMT), is induced in adrenal medulla by different types of stress (Liu et al., 2005, Morita et al., 1996, Nankova et al., 1993, Papanik

• Proof of concept studies with disulfiram suggest

  2020-06-05

  

  Proof-of-concept studies with disulfiram suggest the potential utility of DβH inhibitors for treatment of cocaine use disorder. In a study of 74 subjects stabilized on methadone and randomized into disulfiram and placebo groups for 10weeks, disulfiram treatment reduced cocaine-positive urines, and d

• phosphodiesterase inhibitors Total synthesis requires the tw

  2020-06-05

  

  Total synthesis requires the two key intermediates 3 and 7, which were synthesized using the route described in below. Phenylethylamine 3 was readily synthesized from vanillin or isovanillin; the overall yield was 50–52%. To prepare the intermediates 7, bromination of 2-(4-hydroxyphenyl) acetate wi

• Furthermore Survivin is a member of the inhibitor of

  2020-06-05

  

  Furthermore, Survivin is a member of the inhibitor of apoptosis family. IR induces a rapid nuclear accumulation of survivin and subsequent phosphorylation of the protein in the nucleus. Co-immunoprecipitation and immunofluorescence co-localization analyses revealed an interaction among survivin, Ku7

• br Materials and methods br

  2020-06-05

  

  Materials and methods Results Discussion We found that mRNA expression of PCNA significantly was down-regulated in BCP-ALL purinergic receptors following co-treatment with doxorubicin and NU7441 (Fig. 6e). Our result is congruent with Gehen et al. study reporting that down-regulation of PC

• DNA damage represents a persistent threat

  2020-06-05

  

  DNA damage represents a persistent threat to genomic stability. A critical link exists between DNA mutation, chromosomal rearrangement and cancer development. In myeloid malignancies, various chromosomal translocations and/or mutations increased cellular reactive oxygen species (ROS), followed by DS

• ion channels br STAR Methods br Acknowledgments We are grate

  2020-06-05

  

  STAR★Methods Acknowledgments We are grateful to Matthias Mayer at ZMBH in Heidelberg for access to his CD-spectrometer and his help in data interpretation. Technical support by Wolfgang Weinig is gratefully acknowledged. This project was financially supported by the European Union as part of t

• However there are still some issues

  2020-06-05

  

  However, there are still some issues that remain poorly understood. For instance, how TGF-β modulates DDR2 expression and whether Smads participate in the regulation. How does DDR2 regulate the expression of PTHrP via Runx2? Is there any other kinase downstream of DDR2 participating in PTHrP regulat

• 2665 Collectively the results presented here provide new

  2020-06-05

  

  Collectively, the results presented here provide new insights into ligand binding, clustering, spatial distribution, and phosphorylation of DDR1b and DDR2 in response to soluble collagen I. As depicted in the cartoon of Scheme 1, we postulate a model in which the spatial distribution and assembly of

• In vitro work by us and others revealed that high

  2020-06-05

  

  In vitro work by us and others revealed that high affinity interaction with collagen requires dimerization and/or pre-oligomerization of DDR1 (Agarwal et al., 2007, Abdulhussein et al., 2008, Leitinger, 2003). It has also been reported that a significant percentage of the DDR1 population forms ligan

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