• br Results and discussion br Conclusion Novel

  2021-03-15

  

  Results and discussion Conclusion Novel and selective aziridine-based inhibitors for the Leishmania mexicana protease LmCBP2.8 were discovered. Compounds 7d (Ki = 0.8 μM), 9d (Ki = 1.36 μM), 12d (Ki = 0.77 μM), 14d (Ki = 0.9 μM) and 18 (Ki = 0.441 μM) showed the highest potency and selectivity

• br Conclusion The results of the present study demonstrate t

  2021-03-15

  

  Conclusion The results of the present study demonstrate that cysteinyl leukotrienes LTC4, LTD4 and LTE4 cause moderate to marked whereas the dihydroxy leukotriene LTB4 causes small muscle contraction in the stomach in vitro. The LTD4-induced contraction is mediated by CysLT1 in fundus but by CysL

• Recently a sandwich cultured hepatocyte model

  2021-03-15

  

  Recently, a sandwich-cultured hepatocyte model has been proved to be a valuable in vitro system that maintains specific hepatic cytomorphology and function relevant to drug metabolism, disposition and toxicity, and thus, closely resembles the in vivo setting. This hepatocyte model was recognized as

• CRF and urocortin produce marked

  2021-03-15

  

  CRF and urocortin 1 produce marked effects on the SU6656 when administered both i.v. or directly into the CNS (Parkes et al., 2001). Systemic i.v administration of CRF and urocortin 1 cause a marked and long-lasting reduction in mean arterial blood pressure in rats Briscoe et al., 2000, Lawrence et

• Finally unilateral microinjection of CP Astressin

  2021-03-15

  

  Finally, unilateral microinjection of CP-376395, Astressin 2B, CP-376395 + CRF or ASTR 2B + CRF into the BLA (Fig. 3A) or CeA (Fig. 3B) did not significantly alter spontaneous motor activity in the open field test (F4,24 = 0.148, P > 0.05; F4,29 = 0.290, P > 0.05 in the BLA and CeA, respectively, A

• br Acknowledgments This research was

  2021-03-15

  

  Acknowledgments This research was supported by grants from the Ministerio de Ciencia e Innovación (Grants SAF/FEDER 2010-17907; 2013-49076-P), Spain, Red de trastornos adictivos (RETICS RD12/0028//0003, Instituto de Salud Carlos III, Spain) and Fundación Séneca (15405/PI/10, Región de Murcia, Spa

• The mechanisms in the central nervous system CNS controlling

  2021-03-15

  

  The mechanisms in the central nervous system (CNS) controlling the sympathetic tone of the GLPG0634 are associated to behavioral strategies, such as those involved in response to stress. In this regard, morphine withdrawal induces profound and severe stress reactions evidenced by enhancement of NA

• The pure component paramet http www apexbt com

  2021-03-13

  

  The pure component parameters were taken from literatures. The 4C association scheme was considered for all the H2O, MDEA and H2S. Furthermore, CO2 supposed to be a non-associating component which can construct a cross-association with H2O through acceptations of an DC_AC50 pair. Some of the possibl

• We hypothesize that both IGF dependent kinase activation and

  2021-03-13

  

  We hypothesize that both IGF-1-dependent kinase activation and locally synthesized neuroestrogens interactively regulate estrogen receptor activity in neuronal ARM1 in the absence of exogenously applied estradiol. The Neuro-2A cell line was chosen as the model system for these studies because IGF-1

• br Acknowledgements br Introduction L Rhamnosidases EC are

  2021-03-13

  

  Acknowledgements Introduction α-L-Rhamnosidases (EC 3.2.1.40) are glycosyl hydrolases (GHs) that cleave terminal α-l-rhamnose from a large number of natural products [1]. The action of α-L-rhamnosidases (α-RHAs) has been reported, among others, on different complex substrates such as heteropol

• Targeting the MAPK pathway has

  2021-03-13

  

  Targeting the MAPK pathway has attracted significant interest in cancer therapy. Efforts directly targeting RAS protein are believed to be very challenging in spite of the promise shown by a few RAS inhibitors in the early development stage. Clinical benefits achieved by BRAF and MEK inhibitors have

• The action of pt PGE

  2021-03-13

  

  The action of 17-pt-PGE2 as an EP1 receptor agonist [34] was demonstrated in several experimental settings, including cancer, neurons, vascular system, kidney and was confirmed by application of EP1 receptor selective antagonists [35], [36], [37], [38], [39], [40], [41]. Receptor binding studies in

• Multiple technologies exist for analyzing the

  2021-03-13

  

  Multiple technologies exist for analyzing the contents of single cells, including single-cell DNA sequencing, RNA expression analysis, and protein level and activity measurements (Hu et al., 2018; Narrandes & Xu, 2018; Ortega et al., 2017; Wang & Navin, 2015). Single-cell DNA sequencing is generally

• In agreement with the evidence on the Plg binding

  2021-03-13

  

  In agreement with the evidence on the Plg-binding function of tapeworm enolases, eukaryotic enolases have been shown to be multifunctional proteins, with other activities besides their role as glycolytic enzymes (Pancholi, 2001). In this respect, several flatworms have been proved to express enolase

• The development of novel approaches to study GPCR

  2021-03-13

  

  The development of novel approaches to study GPCR-mediated transactivation in live transferase is important, and this study describes a unique BRET-based quantification of Grb2 recruitment to the EGFR as a direct readout of GPCR-mediated transactivation. We have previously used the recruitment of G

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