• br Conclusion In vivo pharmacokinetic studies showed that da

  2021-01-14

  

  Conclusion In vivo pharmacokinetic studies showed that dasatinib monohydrate pretreatment significantly decreased the blood level of CsA in rats, which was most probably due to the induction of CYP3A2 isoenzymes. The nilotinib pre-treatment had no significant effects on cyclosporine pharmacokinet

• Acknowledgments br Introduction Various researches have been

  2021-01-14

  

  Acknowledgments Introduction Various researches have been made in the field of the treatment of cancer and inflammatory diseases. Different mechanisms are involved in the progression of cellular damage that gives an idea about new drug targets. There are always some efforts to improve efficacy,

• br Material and methods br

  2021-01-14

  

  Material and methods Results Discussion In vitro evidence indicates that LAS191859 is a potent CRTh2 antagonist as demonstrated in GTPγS binding studies with potency in the low nanomolar range and in addition it demonstrates a long receptor residence time. This potency is also maintained in

• br Conclusion br Introduction Interleukin IL is a

  2021-01-14

  

  Conclusion Introduction Interleukin (IL)-18 [1] is a member of the IL-1 cytokine family activating corner stones of inflammatory signaling, among others nuclear factor (NF)-κB and p38 mitogen-activated protein kinase. Striking similarities exist between IL-1β and IL-18 including processing by

• Accordingly we prepared three compounds and

  2021-01-14

  

  Accordingly, we prepared three compounds (, , and ) as shown in . Condensation of commercially available Schizandrin A with glycine methyl ester gave amide . A Friedel–Crafts reaction between compound and 4-methyl valeryl chloride in the presence of aluminum chloride mainly produced undesired co

• The overall shape of p iSH is dramatically different from

  2021-01-13

  

  The overall shape of p110α/iSH2 is dramatically different from DGKB or SK1, instead of forming a homodimer, p110α/iSH2 heterodimer has a triangular shape with iSH2 laying on the top and ABD, RBD, helical and kinase domain of p110α sitting in the bottom (Fig. 2B) (Gabelli et al., 2010; Huang et al.,

• Ingested folate needs to be chemically modified in order

  2021-01-13

  

  Ingested folate needs to be chemically modified in order to become a one carbon donor for cell metabolism. Firstly, folate turns to dihydrofolic ARCA Cy3 EGFP (DHF), it is then converted into tetrahydrofolate (THF) by the dihydrofolate reductase enzyme (DHFR) and finally converted into N5, N10-methy

• RNA sequencing RNA seq is a

  2021-01-13

  

  RNA-sequencing (RNA-seq) is a particularly effective technology for gene discovery in a given process, especially in non-model species for which reference genome sequences are not available. Although the major application of RNA-seq analyses is the identification of differentially expressed genes (D

• Materials and methods Cell culture and receptor gene transfe

  2021-01-13

  

  Materials and methods Cell culture and receptor gene transfection. PC12 p53 tumor suppressor were purchased from the Institute of Cell Biology, Chinese Academy of Sciences, Shanghai, China. The cDNA for mouse CysLT1 or CysLT2 receptor (mCysLT1 and mCysLT2, subcloned into pcDNA3.0) was kindly gifte

• During the course of our research on mGlu

  2021-01-13

  

  During the course of our research on mGlu PAMs,, the hydroxyacetophenone scaffold was found to possess dual mGlu PAM and CysLT1 antagonism activity, presumably as orthosteric antagonist (). There is currently an increasing interest in drug discovery to explore multitarget drugs or polypharmacology

• In this study for the first time we demonstrated

  2021-01-13

  

  In this Micafungin receptor study, for the first time, we demonstrated that herb-derived LFS-01 induces concomitant mitophagy and apoptosis in lymphoma cells. Through various biochemical studies, we showed that LFS-01 directly targets the sulfhydryl (-SH) group of a conserved cysteine in the nuclea

• br Advantages of modified proteins over unmodified ones In

  2021-01-13

  

  Advantages of modified proteins over unmodified ones In contrast to small-molecule drugs, proteins are readily amenable to site-specific alterations through genetic engineering. In principle, therefore, it is possible to build in features that allow them to remain active for longer in the body an

• PHA-848125 br Acknowledgements This work was supported

  2021-01-13

  

  Acknowledgements This work was supported by a grant from the Deutsche Forschungsgemeinschaft to Uwe Knippschild and Martin Wabitsch (SFB 1149/B4). P. Fischer-Posovszky is funded by a Margarete von Wrangell scholarship financed by the Ministerium für Wissenschaft, Forschung und Kunst Baden-Württem

• Although enantioselective accumulation of metalaxyl in organ

  2021-01-12

  

  Although enantioselective accumulation of metalaxyl in organisms is an integrated outcome of bio-process including absorption, transportation, and transformation, it is observed in our study that catalysis of CYP450 may lead to the enantioselective accumulation of metalaxyl. However, the mechanisms

• Pol is responsible for the bulk of leading strand

  2021-01-12

  

  Pol ε is responsible for the bulk of leading-strand synthesis in vivo (Daigaku et al., 2015, Nick McElhinny et al., 2008, Pursell et al., 2007) and physically associates with CMG (Langston et al., 2014, Sengupta et al., 2013, Sun et al., 2015, Zhou et al., 2017). Furthermore, leading-strand synthesi

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