• Epac proteins consist of a carboxyl terminal catalytic regio

  2020-01-10

  

  Epac proteins consist of a carboxyl-terminal catalytic region and an amino-terminal regulatory region, which harbors one cAMP-binding domain in Epac1 and two in Epac2 [22], [32], [51]. In the absence of cAMP, the regulatory region covers the CDC25-homology domain and autoinhibits Epac\'s enzymatic a

• More than thirty enzymes with PLA

  2020-01-10

  

  More than thirty enzymes with PLA2 activity have been described and, based on sequence similarities, they are currently classified in 16 groups, each containing several sub-groups [16]. However, based on biochemical features these enzymes are frequently grouped into six major families: secreted phos

• This paper proposes an acceptance process and evaluation

  2020-01-09

  

  This paper proposes an acceptance process and evaluation criteria, specialized for the dedication of indirect COTS SW as well as direct ones. (Step 1) It first recognizes an indirect COTS SW as a target of dedication, unlike EPRI NP-5652/TR-106439. (Step 2) It then determines the safety category of

• Given the fact that most criticism on genetic association

  2020-01-09

  

  Given the fact that most criticism on genetic association studies is the lack of replicability (Hirschhorn, Lohmueller, Byrne, & Hirschhorn, 2002), the aim of the present study is to investigate the influence of the DBH polymorphism rs1611115 (C-970T) on RD in two independent samples of healthy part

• We recently employed a functional drug screening approach to

  2020-01-09

  

  We recently employed a functional drug screening approach to identify mithramycin as an inhibitor of EWS–FLI1. In our study, we employed a stepwise approach involving a luciferase primary screen and a novel multiplex PCR screen to evaluate over 50,000 compounds to identify mithramycin as an inhibito

• br Significance Ubl post translational modifications are pot

  2020-01-09

  

  Significance Ubl post-translational modifications are potential targets for developing novel therapeutics for life-threatening diseases, such as c-Myc- and KRas-driven cancers that lack targeted therapy. However, only a few drugs are available to target these modifications. This lack of drugs hig

• We therefore propose a scenario based on

  2020-01-09

  

  We therefore propose a scenario based on our experimental models and depicted schematically in Figure 7. In fully respiring cells, CI, CII, and DHODH transfer electrons to CoQ, which are then forwarded to CIII. This latter complex transfers electrons to CIV, which then produces water at the expense

• AACOCF3 br Methods br Results and discussion br Acknowledgem

  2020-01-09

  

  Methods Results and discussion Acknowledgements Introduction Diacylglycerol O-acyltransferase (DGAT) is a key enzyme that catalyzes the final committed step in triglyceride synthesis and is highly expressed in the small intestine, adipose tissue, liver and mammary gland.1, 2, 3, 4 Its im

• Proteases as multifunctional enzymes play key roles in contr

  2020-01-09

  

  Proteases, as multifunctional enzymes, play key roles in controlling a wide variety of cellular and extracellular processes in plants and animals, including protein degradation and processing, germination, complement activation, inflammation, responses to environmental stimuli, senescence and so on.

• Although it is believed that CYP induction is regulated

  2020-01-09

  

  Although it is believed that CYP induction is regulated in humans in principle in the same fashion as in animals, some species differences in CYP3A enzymes induction were observed. Rifampicin is known to be a potent inducer of CYP3A4 in human hepatocytes, whereas pregnenolone-16α-carbonitrile (PCN)

• Gallein br Conclusions Taken together a distinct contrast is

  2020-01-09

  

  Conclusions Taken together, a distinct contrast is observed between ERK1/2 phosphorylation in hypothalamic and extra-hypothalamic Gallein regions. The hypothalamus is the only brain region where ERK1/2 phosphorylation was increased 15minutes after the OF stressor. In SD rats CRFR1 expression was

• In light of the overall loss of activity and selectivity

  2020-01-09

  

  In light of the overall loss of activity and selectivity observed with this series of arylchromenone-4-ones bearing small -alkoxy substituents, we were pleased to identify a potent and relatively selective inhibitor , exhibiting IC values of 0.008μM and 0.07μM for DNA-PK and PI3Kα, respectively. The

• ABH expression is elevated in

  2020-01-09

  

  ABH3 expression is elevated in prostate carcinomas and has been referred to as prostate cancer antigen-1 or PCA-1. ABH3/PCA-1 was proposed as a diagnostic marker for prostate cancers, and suggested as a possible therapeutic target [82]. However, the recent studies of ABH2 and ABH3-null mice indicate

• The current study provides evidence for a previously unknown

  2020-01-09

  

  The current study provides evidence for a previously unknown role for DHODH as a growth/survival factor in KRAS mutant tumors. While many aspects of the link between DHODH inhibition and survival of KRAS mutant cells remain to be established, de novo pyrimidine biosynthesis appears to be a crucial p

• Introduction Neuropathic pain occurs in approximately

  2020-01-09

  

  Introduction Neuropathic pain occurs in approximately one-third of patients with diabetes and is refractory to currently available analgesic drugs (Abbott et al., 2011). This painful diabetic neuropathy (PDN) is associated with elevated levels of methylglyoxal (MG; a reactive glucose metabolite) an

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