• DMOG receptor Our previous high throughput screening HTS cam

  2020-06-15

  

  Our previous high-throughput screening (HTS) campaign using automated, robust, and sensitive fluorescence based DMOG receptor assay [10], [11] led to the identification of several EPAC specific inhibitors (ESIs), and was subsequently followed by extensive hit-to-lead optimizations [20], [21], [22],

• Our observation that nuclear but not cytoplasmic EP

  2020-06-15

  

  Our observation that nuclear, but not cytoplasmic EP4 expression is associated with different outcomes is interesting. In breast cancer, using the same methods, we did not detect EP4 in the nucleus of malignant WIKI4 whereas cytoplasmic EP4 was commonly observed [13]. While G protein-coupled recept

• br Materials and methods br Results br Discussion Enolase ph

  2020-06-15

  

  Materials and methods Results Discussion Enolase (2-phospho-D-glycerate hydrolase) is a glycolytic enzyme that is also involved with various important roles in the intracellular and extracellular space (Copley, 2003; S. Zhang et al., 2015) such as transcriptional regulation, apoptosis, grow

• The potential off target activity of against other ATP

  2020-06-15

  

  The potential off-target activity of against other ATP-dependent enzymes, such as kinases, was also investigated. Encouragingly, there was no significant inhibition of ATP binding to 97 human kinases, when was evaluated at 10μM within a DiscoveRx scanEDGE® kinome screen (, ). All together, these dat

• br Materials and Methods br Acknowledgements

  2020-06-15

  

  Materials and Methods Acknowledgements We thank the staff of beamlines ID29 and ID30A-1 of the European Synchrotron Radiation Facility. This work was supported by, the Marie Curie Career Integration Grant (PCIG13-GA-2013-630755), the Israel Science Foundation (Grant 1383/17) and the Israeli Ca

• br Results br Discussion Many assays

  2020-06-15

  

  Results Discussion Many assays in the literature for DBH require the use of catalase to protect the active site from hydrogen peroxide, which is a by-product in the initial step of the reaction. For the non-immobilized enzyme there was a visible increase in the rate with increasing amounts of

• Two parameters were extracted from these

  2020-06-15

  

  Two parameters were extracted from these experiments to compare the interactions of the three compounds with ct-DNA. The association constant K for the binding of the naphthalimide derivatives to ct-DNA was calculated by fitting the evolution of the fluorescence spectra with a 1:1 binding model usin

• br UVC induced DNA damage a model to study

  2020-06-15

  

  UVC-induced DNA damage: a model to study DNA damage tolerance The UV components of sunlight that reaches the Earth surface are one of the most carcinogenic agents humans are exposed to, and the leading cause of skin cancer [4,12]. UV light causes different types of DNA damage through indirect and

• This project was funded by the Deutsche Forschungsgemeinscha

  2020-06-15

  

  This project was funded by the Deutsche Forschungsgemeinschaft within FOR 2251 (project grants EB 285/2-1 and WI 3272/3-1) and in part by additional contributions from the Bundesministerium für Bildung und Forschung (D.I.S award Nos. BIOSCAT [05K12YE1]) and the Horizon 2020 programme of the European

• Multi subunit RING type E ligases

  2020-06-13

  

  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

• br Results br Discussion Taking advantage of

  2020-06-13

  

  Results Discussion Taking advantage of the highly specific protein–protein interactions among cognate SB408124 that mediate SUMO conjugation to substrates, we have developed a novel strategy for achieving inhibition of SUMO conjugation in vivo based on disruption of SUMO E1–E2 interactions. We

• Another question concerns the mechanism of PC reduction duri

  2020-06-13

  

  Another question concerns the mechanism of PC reduction during the phosphate starvation response. There are at least three main mechanisms of PC depletion: suppression of PC synthesis due to substrate exhaustion, downregulation of PC synthase expression by suppression of gene transcription or intens

• Though the physiological roles of microglia derived

  2020-06-12

  

  Though the physiological roles of microglia-derived elastases in the CNS are not well understood, their involvement in the metabolism of cholecystokinin [41] and in the processing of plasminogen to produce a low molecular weight plasminogen that enhances neurite outgrowth has been reported [38]. Exp

• br Collagens as new drivers of zebrafish

  2020-06-12

  

  Collagens as new drivers of zebrafish tissue regeneration Contrary to mammals, zebrafish possess very high regeneration capacities and thereby represent a versatile model to study tissue and organ regeneration. Adult fish can fully reconstruct their brain, spinal cord, retina, kidney, liver, panc

• The Fontan circulation When first described in

  2020-06-12

  

  The Fontan circulation When first described in 1971, the Fontan operation ushered in a new paradigm in the care of children born with the varied forms of complex congenital TL32711 disease (CHD) characterized by a single effective pumping chamber.1., 2. This procedure, which creates a total cavopul

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