• The H R antagonist cimetidine Tagamet

  2022-02-09

  

  The H2R antagonist cimetidine (Tagamet™) became the first billion-dollar drug in the 1980s for the treatment of peptic ulcer disease. Other H2R antagonists include ranitidine, famotidine, nizatidine, and zolantidine, the latter showing good BBB penetration with a steady-state brain/blood ratio of 1.

• Arena Pharmaceutical introduced a biaryl sulfone derivative

  2022-02-09

  

  Arena Pharmaceutical introduced a biaryl sulfone derivative with antagonistic activity at H3Rs known as APD-916, ((R)-1-(2-(4'-(3-methoxypropylsulfonyl)biphenyl-4-yl)ethyl)-2-methylpyrrolidine), which was rationally designed from corresponding sulfonamides in order to yield compounds with short dura

• br Acknowledgements This work was supported by

  2022-02-09

  

  Acknowledgements This work was supported by grants from the Agencia Nacional de Promoción Científica y Tecnológica (PICT2013-0495, PICT2016-1821), and from CONICET (PIP 2013-562), as well as from Fundación René Barón and Fundación Williams. Introduction Histamine poisoning, also known as scom

• br Conflicts of interest br Significance p is required

  2022-02-09

  

  Conflicts of interest Significance p53 is required for the induction of cell senescence to limit the proliferation of polyploid cells. We found that Hippo signal deficiency or Yap activation in mouse livers result in polyploid formation and polyploid cell growth. The combined loss of Hippo sig

• Cux is a cell cycle dependent

  2022-02-09

  

  Cux1 is a BAY 41-8543 receptor dependent transcription repressor that is aberrantly expressed in the Pkd1 null, Pkd1CD, and cpk mouse models of PKD, as well as in human ADPKD cells (Vanden Heuvel et al., 1996; Sharma et al., 2005; Paul et al., 2011; Alcalay et al., 2008). In Pkd1 null mice and in hu

• We are pursuing a hit to lead medicinal chemistry campaign

  2022-02-09

  

  We are pursuing a hit-to-lead medicinal chemistry campaign to optimize inhibitors of the HBV RNaseH. Here, we report the activity of seven new HIDs and nine new HPDs, with significant improvements in in vitro potency and cytotoxicity profiles for the HPD compounds. Materials and methods Result

• br Conclusion The following is the supplementary

  2022-02-09

  

  Conclusion The following is the supplementary data related to this article. Conflict of interest Funding Acknowledgements Peroxiredoxin VI (Prdx6) is a dual-functioning antioxidant enzyme that acts to protect biological membranes against damage caused by lipid peroxidation , . The enz

• br Conclusion Until recently astrocytes were recognized sole

  2022-02-08

  

  Conclusion Until recently, astrocytes were recognized solely for their maintenance role in the regulation of Ticarcillin sodium homeostasis. Nowadays, this idea has changed, it is clear that these cells play a crucial role in the regulation of neuronal activity and signal transmission. In particu

• Copanlisib receptor Deregulation of HH signaling pathway

  2022-02-08

  

  Deregulation of HH signaling pathway in epidermal keratinocytes is a primary event leading to the formation of BCC (see above). Overexpression of SHH in HaCaT keratinocytes grown in organotypic cultures induces a basal cell phenotype and increases invasiveness. This behavior is linked to increased E

• br Biologically active non peptide galanin receptor

  2022-02-08

  

  Biologically active non-peptide galanin receptor ligands The first successful attempt in overcoming these weaknesses was undertaken by Saar et al. (2002). Screening of galanin sequence established that Trp-2, Asn-5, Tyr-9 were pharmacophores, responsible for biochemical action of the peptide. Bas

• br Introduction Thrombosis is one of the leading causes of

  2022-02-08

  

  Introduction Thrombosis is one of the leading causes of deaths in the cardiovascular diseases such as myocardial infarction (MI), unstable PIK-III and acute coronary syndrome (ACS) in developed countries [1], [2]. It is estimated that venous thromboembolism (VTE) afflicts about 1 million (1–2 per

• The NuB complex interacts with Asf p which plays

  2022-02-08

  

  The NuB4 complex interacts with Asf1p, which plays a central role in controlling the flux of histones to the various chromatin assembly pathways. This interaction is also evolutionarily conserved having been detected in yeast, chicken and human Etoricoxib sale [27], [61], [104], [105]. Asf1p appear

• The Hippo pathway is a growth

  2022-02-08

  

  The Hippo pathway is a growth control signaling cascade that has been demonstrated to play an important role in regulating cell proliferation and differentiation [5,6]. The core signaling pathway consists of a group of kinases which negatively regulate the expression of transcriptional co-activators

• Freinkel first reported in the late s that maternal hypertri

  2022-02-08

  

  Freinkel first reported in the late 1960s that maternal hypertriglyceridemia benefits the fetus during starvation by increasing maternal consumption of triglyceride for ketone body synthesis giving the basis for “accelerated starvation” theory [4,5]. This maternal metabolic reprogramming during peri

• br Direct effect of HDACs on contractile function by deacety

  2022-02-08

  

  Direct effect of HDACs on contractile function by deacetylating cytoskeletal and contractile proteins Role of HDACs in electropathology by transcriptional reprogramming Next to deacetylation of α-tubulin by HDAC6 in experimental and human AF, there is also evidence for transcriptional reprogra

7399 records 474/494 page Previous Next First page 上5页 471472473474475 下5页 Last page