• MAPKs are a family of phosphorylating enzymes

  2020-02-28

  

  MAPKs are a family of phosphorylating enzymes that orchestrate various cellular response in proliferation, apoptosis, inflammation, stress response, and energy metabolism [11]. There are at least four major members including extracellular signal-regulated kinase 1 and 2 (ERK1/2), p38 mitogen-activat

• The role of Epac in the regulation of intracellular

  2020-02-28

  

  The role of Epac in the regulation of intracellular Ca homeostasis and contractility is still matter of debate. In rat adult cardiomyocytes, acute Epac stimulation decreased the amplitude of Ca transients [6], [9], [10] with either no changes [6] or increments [9] in cell shortening, suggesting an e

• In conclusion we designed novel E inhibitors based

  2020-02-28

  

  In conclusion, we designed novel E1 inhibitors based on the three-dimensional structure of E1 in complex with ubiquitin. Following an enzymatic assay evaluating synthetic compounds , , and , we identified compound as a novel E1 inhibitor. Comparing the inhibitory activity of compound with and ,

• Future advances in the in vivo molecular

  2020-02-28

  

  Future advances in the in vivo molecular imaging of enzyme activity will greatly benefit from the progress towards the quantitative detection of enzymes. Quantitative imaging requires knowledge of both the location and concentration of a specific enzyme, which is dependent on the simultaneous measu

• The synthesis of the required substrates is shown in

  2020-02-28

  

  The synthesis of the required substrates is shown in (see for experimental details). Treatment of heterocycle with MK 886 under basic conditions afforded a mixture of the mono-substituted product (22%) and the di-substituted compound (38%) which were separated by column chromatography. Compou

• br Oxidoreductase like MEM for

  2020-02-28

  

  Oxidoreductase-like MEM for prodrug activation Future outlook Although MEM-mediated prodrug activation has been performed by different MEMs and prodrugs, and their effectiveness have been proved in vivo, only a few types of MEMs or prodrugs have been explored in prodrug activation until now [2

• DSBs can be repaired by two major pathways

  2020-02-28

  

  DSBs can be repaired by two major pathways: canonical non-homologous end-joining (c-NHEJ) and homologous recombination (HR) (Chapman et al., 2012). c-NHEJ comprises two sub-pathways, a resection-independent process and a resection-dependent process, and can rejoin break ends with little or no sequen

• In this review we present compelling evidence in support of

  2020-02-28

  

  In this review, we present compelling evidence in support of DHODH as an essential enzyme for the survival of cancer cells. DHODH, and its relationship to de novo pyrimidine metabolism, will be discussed along with factors that influence its regulation and expression. We will show evidence of DHODH\

• Electron transport via DHODH activity

  2020-02-28

  

  Electron transport via DHODH activity will allow the generation of mitochondrial ROS without the consumption of α-ketoglutarate or NADH. Glutamine-dependent flux through the TCA cycle and oxidative phosphorylation can also enable generation of mitochondrial ROS (Weinberg et al., 2010). The latter pr

• br Conclusions and future perspectives It is

  2020-02-28

  

  Conclusions and future perspectives It is now evident that selective ETA or nonselective endothelin receptor antagonism provides therapeutic potentials against a variety of cardiovascular diseases such as hypertension, PAH, and diabetic microvascular dysfunction (Fig. 1). However, PAH is currentl

• br Conclusion br Declaration of interest br Introduction Gly

  2020-02-28

  

  Conclusion Declaration of interest Introduction Glyphosate [N-(phosphonomethyl)glycine] is the main active ingredient in one of the most widely used herbicides in the world. The commercially used concentrations of glyphosate range from 1% for domestic use to 41% for conventional agricultura

• br Author contributions br Funding M E B was

  2020-02-28

  

  Author contributions Funding M.E.B. was supported by Research Fund #3096. Competing interests Introduction Lung cancer has become one of the most common death causes in both male and female malignant tumors (Jemal et al., 2011). Air pollution, smoking and estrogen level are known risk f

• The in vitro enantioselective metabolism of pesticides has b

  2020-02-28

  

  The in vitro enantioselective metabolism of pesticides has been investigated by employing human liver microsomes, which are a reliable resource to perform MCL enantioselective risk assessment in humans (Carrão et al., 2019; de Albuquerque et al., 2018, 2016; Yao et al., 2016). The enantioselective m

• br Results br Discussion It has been thought that

  2020-02-28

  

  Results Discussion It has been thought that commitment to the plasma cell fate begins while Canagliflozin synthesis are still in the GC (Suan et al., 2017, Victora and Nussenzweig, 2012), but the main obstacle to test this model and, if correct, to clarify how the plasma cell-prone GC cells d

• br Methods br Results br Discussion Preclinical

  2020-02-27

  

  Methods Results Discussion Preclinical data indicate that nepicastat modulates sympathetic drive to the WIN 64338 hydrochloride with a mild pressor effect in various animal models of hypertension (Stanney et al., 1998). However in this clinical study, the doses of nepicastat employed did n

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