• Testosterone is inactivated through hydroxylation and conjug

  2020-07-02

  

  Testosterone is inactivated through hydroxylation and conjugation pathways [3], [4]. 6β-Hydroxylation is the main pathway among testosterone hydroxylation processes in the liver microsome. Testosterone 6β-hydroxylation is mainly catalyzed by cytochrome P450 3A (CYP3A) [5], [6], which is expressed in

• Previously to detect CDKL activity we used a radioactive

  2020-07-02

  

  Previously, to detect CDKL5 activity, we used a radioactive phosphorylation assay with amphiphysin 1 protein as a substrate [,,]. However, it is necessary to establish a safe and rapid method for analyzing CDKL5 mutant activity. Here, we report a new method for investigating autophosphorylation acti

• Within the BLA both CRF

  2020-07-02

  

  Within the BLA, both CRF and the CRF1 receptor have been shown to functionally regulate synaptic activity. In vivo, CRF release into the BLA originates from projections from the CeA (Roozendaal, Brunson, Holloway, McGaugh, & Baram, 2002). Central administration of both CRF and CRF1 agonists has been

• Pahlavanzadeh and Fakouri Baygi employed PC SAFT

  2020-07-02

  

  Pahlavanzadeh and Fakouri-Baygi [6] employed PC-SAFT EoS to predict the brincidofovir of carbon dioxide by aqueous MEA solutions. They used the ideal form of Smith–Missen algorithm to calculate liquid phase concentrations. The results illustrate acceptable accuracies so that the AAD was achieved eq

• br Chagas disease and HAT drug

  2020-07-01

  

  Chagas disease and HAT drug R&D Drug R&D for Chagas disease and HAT has historically relied on serendipitous findings achieved using low-technology approaches. The absence of biotechnology tools associated and the very limited understanding of the biomolecular processes of the parasites are among

• br Acknowledgements This work was supported by the National

  2020-07-01

  

  Acknowledgements This work was supported by the National Institute of Neurologic Disorders and Stroke (U54 HD061222, 1K23 NS107646-01, and 1K12NS089417-01), Rocky Mountain Rett Association, International Foundation for CDKL5 Research, the Ponzio Family Chair in Neurology Research, and NHMRC Senio

• br Materials and methods br Results and discussion

  2020-07-01

  

  Materials and methods Results and discussion In the present work, we have applied two methodologies, CoMFA and CoMSIA to build 3D-QSAR models. There is no crystal structure available; therefore, an indirect method i.e., a ligand-based approach is the method of choice. The highly active molecul

• br Acknowledgments br Casein kinases CK are serine threonine

  2020-07-01

  

  Acknowledgments Casein kinases (CK) are serine/threonine-specific enzymes and can be divided two subtypes: casein kinase 1 (CK1) and casein kinase 2 (CK2). CK1 contains at least seven isoforms (α, β, γ1, γ2, γ3, δ and ε) expressed in eukaryotic organisms, CK1 is involved in various cellular pro

• br EphB as a therapeutic target in

  2020-07-01

  

  EphB4 as a therapeutic target in cancer Eph receptors and ephrins are promising new therapeutic targets in cancer. Various strategies have been employed to evaluate the interference of tumor-promoting effects or the enhancement of tumor suppressive effects. The inhibition of the Eph-ephrin system

• An Ubl modification requires several steps that are

  2020-07-01

  

  An Ubl modification requires several steps that are catalyzed by three enzymes, referred to as E1 (activating enzyme), E2 (conjugation enzyme), and E3 (ligase). The SUMO E1 is a heterodimer of SAE1 and Uba2 (also known as SAE2). In brief, an Ubl is first activated by E1 through ATP hydrolysis and fo

• E ubiquitin ligases are key

  2020-07-01

  

  E3 ubiquitin ligases are key players in the ubiquitin-proteasome pathway because they catalyse ubiquitination of substrate proteins.39, 40, 41 As important regulators of cellular ubiquitination, E3 ligases are emerging as attractive drug targets, particularly in cancer.42, 43, 44 However, E3 ligases

• This pathway appears to have

  2020-07-01

  

  This pathway appears to have importance in epilepsy. DGKε(−/−) mice had significantly fewer motor seizure and epileptic events compared with DGKε(+/+) mice [18]. This could be explained by the fact that in the knockout mice a greater fraction of the SAG would be converted to 2-AG. 2-AG itself is kno

• br Acknowledgements Thanks are due to

  2020-07-01

  

  Acknowledgements Thanks are due to Science and Technology Development Fund – Egypt for the Research Support Technology Development Grant (RSTDG) no. 12626. Our deep thanks and gratitude is also extended to National Cancer Institute (NCI), Bethesda, Maryland, USA for performing the anticancer eval

• Cysteinyl leukotrienes CysLTs are potent inflammatory mediat

  2020-07-01

  

  Cysteinyl leukotrienes (CysLTs) are potent inflammatory mediators closely associated with cerebral ischemic injury. CysLTs induce inflammatory responses mediated by at least two different CysLT receptors (CysLT1R and CysLT2R) (Bäck et al., 2011, Singh et al., 2010). It has been reported that the Cy

• ARQ197 br Acknowledgments br Introduction Cysteinyl leukotri

  2020-07-01

  

  Acknowledgments Introduction Cysteinyl leukotrienes (CysLTs), LTC4, LTD4 and LTE4, are 5-lipoxygenase pathway metabolites of arachidonic ARQ197 and deeply involved in bronchial asthma via activation of CysLT1 receptors [1], [2]. Specific CysLT1 receptor antagonists, including pranlukast [3],

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