• Our data indicate that the ability

  2020-11-16

  

  Our data indicate that the ability of these promiscuous kinases to bind chemically diverse inhibitors is defined by the hydrophobic pocket formed by the activation loop, which is only accessible in the DFG-Asp-out conformation. Inhibitors do not artificially induce the DFG-Asp-out conformation as wa

• For radiochemotherapy it is well known that mitotic

  2020-11-16

  

  For radiochemotherapy, it is well known that mitotic cell death and apoptosis present the major cell death modes. More recently, autophagy-dependent cell death has been described to occur upon radiochemotherapy (Daido et al., 2005, Song et al., 2017). This form of regulated cell death depends on com

• In the present study we

  2020-11-16

  

  In the present study, we used a new luminescent method to measure CYP activity with Luciferin-ME as a substrate which is used for wide ranges of mammalian CYPs, including CYP1A2, CYP2C8, CYP2C9, CYP2J2, CYP4A11, and CYP4F3B. As a result, no significant modulations of CYP activities in B[a]P exposure

• Some studies have demonstrated that BMSCs can

  2020-11-16

  

  Some studies have demonstrated that BMSCs can provide several trophic and growth factors that play important roles in cell survival, angiogenesis, and BMSC differentiation, but not cell replacement (Peled et al., 1999, Shen et al., 2007, Ji et al., 2004). This paracrine effect of BMSCs is a potentia

• br Results br Discussion GPCRs recognize a broad

  2020-11-16

  

  Results Discussion GPCRs recognize a broad range of molecules with a vast chemical Adefovir Dipivoxil through different mechanisms. Our understanding of the recognition of lipid mediators by GPCRs primarily comes from the structural studies of receptors for lysophospholipids and endocannabino

• By live imaging of GUL GFP we observed

  2020-11-16

  

  By live imaging of GUL-1-GFP, we observed the kinetics of aggregate movement within the cell. One of the marked characteristics of GUL-1-GFP cytosolic (but not nuclear-associated) aggregate motion was a “comet-like” movement that was found to be dependent on the presence of properly polymerized micr

• Cell swelling stimulates the release of certain

  2020-11-16

  

  Cell swelling stimulates the release of certain amino acids, in particular the non-protein amino Bioactive Compound Library taurine, via a pathway which has the characteristics of a channel rather than a carrier [54], [69]. Indeed, on the basis of pharmacological inhibition, it was suggested that v

• Determination of relative potency EC

  2020-11-14

  

  Determination of relative potency (EC50) by dose response assays in vitro is subject to the same sources of variability as determination of affinity, since the EC50 and Hill slope of the dose response curve are highly dependent on the binding of ligand to a competing receptor that may be present, an

• Estrogen treatment in postmenopausal women

  2020-11-14

  

  Estrogen treatment in postmenopausal women requires combination with a progestogen in order to prevent endometrial stimulation. This is not necessary, however, with tibolone as progestogenic activity is associated with its Δ4-metabolite that is formed in the liver, as well as locally in the endometr

• calcium sensing receptor The ERR gene lacks the typical TATA

  2020-11-14

  

  The ERRα gene lacks the typical TATA and CAAT boxes, but has multiple consensus Sp1 binding elements in the GC-rich promoter (Shi et al., 1997). Previously, our laboratory has shown that ERRα expression is upregulated in the mouse uterus by estrogen (Shigeta et al., 1997) and recently we identified

• Nocodazole The ADME profile of AAT was very

  2020-11-14

  

  The ADME profile of AAT-008 () was very promising, with high stability in HLM. The pre-clinical pharmacokinetic properties of AAT-008 were also assessed in rats (Sprague-Dawley, male), dogs (beagle, male), and monkeys (cynomolgus, male). The experimentally determined parameters are summarized in . A

• Enzyme activity loss during the hydrolysis process has tradi

  2020-11-14

  

  Enzyme activity loss during the hydrolysis process has traditionally been associated with thermal, mechanical, and/or chemical mechanisms (Okino et al., 2013, Ye et al., 2012, Zhang et al., 2010). Due to the recent discovery of enzyme activity loss due to interaction with substrate, it is important

• br Orthotopic liver transplantation OLT is the only

  2020-11-13

  

  Orthotopic liver transplantation (OLT) is the only curative therapy available for patients with end-stage liver disease. The surgical procedure of liver transplantation inherently involves cold ischemia during graft preservation , followed by reperfusion of the transplanted graft which results in

• Valproic acid VPA is a first line treatment for epilepsy

  2020-11-13

  

  Valproic N1-Methylguanosine-5'-Triphosphate (VPA) is a first-line treatment for epilepsy and bipolar disorder, although its therapeutic mechanism of action is not fully understood. Considerable evidence suggests that VPA can act through the GABAergic system, NMDA receptors, and/or sodium channels (

• br Materials and methods br Results br Discussion ParI

  2020-11-13

  

  Materials and methods Results Discussion ParI, the first C5-DNA-MTase from a psychrophilic bacterium to be characterized, displays DNA methylation activity in vivo and in vitro. Its biophysical characteristics are consistent with large regions of disorder including thermal unfolding transit

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