• Our initial approach to identify hits

  2024-05-20

  

  Our initial approach to identify hits was two-pronged and included a high-throughput screening (HTS) campaign of the OSI lobeline library as well as a virtual screening (VS) campaign, utilizing a publically available crystal structure of ACK1 (PDB code: ). A tolerance for protein flexibility was in

• AP24534 br Regulation and pharmacology of mPGES mPGES kDa am

  2024-05-20

  

  Regulation and pharmacology of mPGES-1 mPGES-1 (16 kDa, 152 amino acids) is a trimeric integral membrane protein of the endoplasmic reticulum with each monomer containing four transmembrane domains (Samuelsson et al., 2007; Sjogren et al., 2013). The three active site cavities are located at the

• akt inhibitor The altered frequency of CD T cells in LO

  2024-05-20

  

  The altered frequency of CD4+ T akt inhibitor in 5-LO−/− mice led us to hypothesize that these leukocytes could be exerting a primary control of the inflammatory response. In fact, the lack of 5-LO resulted in the accumulation of CD4+CD25+ cells expressing Treg markers. It is plausible to speculate

• The subdivision of HT receptors started in the s by

  2024-05-20

  

  The subdivision of 5-HT receptors started in the 1950s by Gaddum and colleagues, when they realised that in the guinea pig ileum, the effects of 5-HT could be blocked in part by morphine (M), and in part by dibenzyline (D). Gaddum and Picarelli proposed two receptor classes, 5-HT M and 5-HT D (1957)

• Later the same group designed and

  2024-05-20

  

  Later, the same group designed and prepared several Δ16-steroidal C17 benzoazoles and pyrazines and evaluated their CYP17 and 5α-reductase inhibitory activities, binding to and transactivation of the AR, as well as their antiproliferative effects against two human PC cell lines (LNCaP and LAPC4) [18

• c-Myc tag Regarding brain tumors AXL has been

  2024-05-20

  

  Regarding c-Myc tag tumors, AXL has been implicated in gliomagenesis and chemoresistance [39]. Previous investigations found that AXL is constitutively phosphorylated in many glioma cell lines, murine xenograft tumors and primary patient tumor samples [40]. Immunohistochemical analysis of AXL and Ga

• To test the compounds metabolic stability we measured

  2024-05-20

  

  To test the compounds metabolic stability, we measured the half-life of compounds and in mouse hepatic microsomes (1mg/mL) and found them to have modest stability, with half-lives of 7.5 and 2.9min respectively, indicating these compounds may be unsuitable for studies. In order to gain structura

• br Experimental protocols br Results and discussion

  2024-05-20

  

  Experimental protocols Results and discussion Conclusion 15-LOX-1 is an important mammalian lipoxygenase which plays an important role in the biosynthesis of leukotrienes, lipoxins and other signalling molecules. These signalling molecules play a regulatory role in several respiratory disea

• Recent work has detailed the impact of genetic deletion

  2024-05-20

  

  Recent work has detailed the impact of genetic EPI-001 of AMPK in the liver, revealing only minor phenotypes upon removal in mice (Boudaba et al., 2018). However, these studies very elegantly showed the potential for small molecule-mediated activation of AMPK to elicit large changes in lipid metabol

• Women are usually at risk of

  2024-05-20

  

  Women are usually at risk of sleep deprivation or restriction during pregnancy, especially in the third trimester of gestation, due to the pregnancy-associated anatomic, physiological and hormonal changes (Pien and Schwab, 2004). However, several major cy5 dye developmental events, such as the neur

• In past Zebra fish Danio rerio has

  2024-05-20

  

  In past, Zebra fish (Danio rerio) has emerged as a suitable model for early vertebrate development, and a number of targeted mutations in the zebrafish genome led to phenotypic alterations that resemble human diseases [34]. A 12-LOX in Zebra fish has been cloned and knock down of this zf12-LOX enzym

• As one of emerging high throughout methods

  2024-05-18

  

  As one of emerging high-throughout methods, metabolomics detects metabolites which are ultimate response of biological systems to environmental changes [14]. Metabolomics uncovers metabolic alteration at the systems level. Comparison of global metabolic profiling reflects some unidentified biologica

• SCR 7 mg It thus appeared reasonable that AR needed to be in

  2024-05-18

  

  It thus appeared reasonable that AR needed to be inhibited and great experimental efforts began which are still on-going [6]. Indeed, hundreds of ARIs have been characterized but no significant drug development has followed. The case of Sorbinil, which did not pass clinical trials is emblematic [7]

• Pregnane X receptor PXR is a nuclear receptor that

  2024-05-18

  

  Pregnane X receptor (PXR) is a nuclear receptor that plays an important role in regulation of metabolism and disposition of structurally diverse xenobiotics as well as endogenous steroids and bile acids (Bertilsson et al., 1998, Kliewer et al., 1998, Lehmann et al., 1998). PXR regulates the metaboli

• In model plant Arabidopsis there are myosin XI isoforms XI

  2024-05-18

  

  In model plant Arabidopsis, there are 13 myosin XI isoforms (XI-1, XI-2, XI-A, XI-B, XI-C, XI-D, XI-E, XI-F, XI-G, XI-H, XI-I, XI-J, and XI-K) and 4 myosin VIII isoforms (ATM1, ATM2, VIII-A, VIII-B) [9,13]. Arabidopsis myosin XIs have the common domain composition: a motor domain that interacts with

14955 records 119/997 page Previous Next First page 上5页 116117118119120 下5页 Last page