• Prenylation may turn a flavonoid from an agonist

  2020-03-03

  

  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 conformat

• Cyclosporine NEORAL Oral Solution Novartis is an immunosuppr

  2020-03-03

  

  Cyclosporine (NEORAL® Oral Solution, Novartis) is an immunosuppressant widely used in organ transplantation and many other clinical conditions [12]. It undergoes extensive hepatic and intestinal biotransformation mainly via the metabolizing enzyme, CYP3A4 [[12], [13], [14], [15]]. Considering the na

• br Introduction As a strong

  2020-03-02

  

  Introduction As a strong analgesic, morphine is often used to treat acute and chronic pain. However, morphine is a substance with low lipid solubility that slowly enters the nerve tissue through the blood–brain barrier and produces neurotoxicity. Morphine-induced neurotoxicity can be produced aft

• br Materials and methods br

  2020-03-02

  

  Materials and methods Results Discussion Drug of abuse induces widespread CBL0137 hydrochloride changes in the molecular and cellular functions in circuits between VTA and its neighbored regions such as NAC, and amygdala. It is belived that these changes result behavioral phenotype that ch

• Historically covalent drugs have had great

  2020-03-02

  

  Historically, covalent drugs have had great success (e.g., aspirin and penicillin), and covalent drugs have become a focus in anticancer and antiviral drug discovery (Kalgutkar and Dalvie, 2012, Singh et al., 2011). These compounds contain low reactivity warheads that allow covalent adducts to form

• Furthermore collagen could be further utilized to surface mo

  2020-03-02

  

  Furthermore, collagen could be further utilized to surface modification of biologically inert materials, such as polymer materials and metal materials, which are always hydrophobic, lacking functional groups and poor cell adhesion. Therefore, various strategies have been tested to improve the proper

• In conclusion we demonstrated phenoconversion

  2020-03-02

  

  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

• In this study we characterized the metabolic function

  2020-03-02

  

  In this study, we characterized the metabolic function of tra2 in the Drosophila fat body. Similar to the 9G8 phenotype, decreasing tra2 levels in the Drosophila fat body using RNAi resulted in increased starvation resistance and a large increase in triglycerides. This increased storage of triglycer

• Renal injury by cisplatin has been associated

  2020-03-02

  

  Renal injury by cisplatin has been associated with oxidative stress, inflammation, and apoptosis (Francescato et al., 2007, Iseri et al., 2007, Kiymaz et al., 2008, Ueki et al., 2012). Specifically, apoptosis is an important mode of cell death in cisplatin nephrotoxicity, and many studies including

• br Significance Our understanding of the

  2020-03-02

  

  Significance Our understanding of the ubiquitin biology has been rapidly expanding. The role of the ubiquitin system in the pathogenesis of numerous disease states has increased the interest in finding new strategies to pharmacologically interfere with the enzymes responsible of the ubiquitinatio

• ATRX belongs to the switch sucrose

  2020-03-02

  

  ATRX belongs to the switch/sucrose non-fermenting (SWI/SNF) chromatin remodeling family, mutations in which cause syndromal mental retardation and downregulation of α-globin expression (Gibbons et al., 1995). Most of these mutations are located in two highly conserved regions of the ATRX protein: a

• br Methods To study electrostatic substrate channeling we em

  2020-03-02

  

  Methods To study electrostatic substrate channeling, we employed two methodologies, Brownian dynamics and a continuum model based on the Smoluchowski theory. Whereas Brownian dynamics simulations are useful for tracking the motion of individual particles, the continuum model is convenient for cal

• br Acknowledgments br Introduction Understanding the charact

  2020-03-02

  

  Acknowledgments Introduction Understanding the characteristics of the Amazonian Dark soils “Terras Pretas de Índio” (TPIs) is of ecological importance, because the TPI soils represent a residue-based model for tropical sustainable agriculture (Sombroek et al., 2003, Neves et al., 2003, Cohen-O

• It is interesting that of the

  2020-03-02

  

  It is interesting that of the control groups, female TG controls only had significantly higher MB-COMT protein than non-TG male controls (Supplemental Table 9, P = 0.005), while these two groups have almost equal expression of S-COMT protein (8.54- vs. 8.34-fold) and their COMT enzyme activity is al

• Antioxidants such as SFN have been

  2020-03-02

  

  Antioxidants such as SFN have been proposed to be chemopreventive agents to inhibit, delay or reverse the development of cancer (Bayat Mokhtari et al., 2018). SFN was shown in breast epithelial cell culture to suppress oxidative metabolism of E2/E1 and thus protect against estrogen-mediated DNA dama

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