• A set of small molecule LigI inhibitors were identified thro

  2019-09-16

  

  A set of small molecule LigI inhibitors were identified through an in silico structure-based screen, using the atomic resolution structure of LigI complexed with nicked DNA [[18], [26]]. This screen yielded inhibitors that were selective for LigI (L82), inhibited both LigI and LigIII (L67) and inhib

• br Phenotypic responses alkylation induced cell death and mu

  2019-09-16

  

  Phenotypic responses: alkylation-induced cell death and mutagenesis E. coli alkB mutants were isolated in a screen for strains specifically sensitive to the cytotoxicity of MMS but not UV-irradiation. This was the first indication that the AlkB protein is a primary cellular defence against alkyla

• br Results br Discussion The importance

  2019-09-16

  

  Results Discussion The importance of mitochondria for the initiation and progression of tumorigenesis is now emerging. It is evident that, despite the well-known Warburg effect, tumors have active mitochondrial bioenergetic metabolism (Marin-Valencia et al., 2012, Hensley et al., 2016). Disrup

• How does an increase in E affinity for the RING

  2019-09-12

  

  How does an increase in E2 affinity for the RING domain favor higher activity and polyubiquitination by the E2? Binding of the RING domain to the E2 positions the donor Ub in the E2~Ub conjugate in a closed complex [16], [17], [18] that increases the reactivity of the thioester [60]. A higher affini

• The crystal structure of full length CHK is still

  2019-09-12

  

  The crystal structure of full-length CHK is still unsolved. However, the close homology between CHK and Csk suggests that these kinases share a similar structure. Therefore, the engagement of the CHK SH2–kinase linker with the αC-helix could control the activity of the CHK kinase domain. Sequence al

• trans-AUCB br Materials and methods br Results and discussio

  2019-09-12

  

  Materials and methods Results and discussion Conclusions Acknowledgments This work was supported by the National Research Foundation of Korea (NRF) grant funded by the Korean government (MEST) (No. 2011-0030635) and the MarineBio Research Program (NRF-C1ABA001-2011-0018561). The Fonta

• In vitro study indicated the

  2019-09-12

  

  In vitro study indicated the cell death of hippocampal neurons was mediated by DAPK1 following ceramide-3 treatment (Pelled et al., 2002). the same study showed that DAPK1-deficient mice treated by acyl ceramide exhibit a less sensitivity to apoptosis, this proposed that DAPK1 plays a central role i

• Cyclo p and p which are downstream of

  2019-09-12

  

  p21 and p16, which are downstream of pAkt and pERK1/2, are tumor suppressors which induce cell senescence and Cyclo arrest [[56], [57], [58]]. Inhibitors of pAkt or pERK1/2 can activate p21 and p16 and promote cell senescence and cell cycle arrest [11,12,[59], [60], [61]]. It is well known that p21

• Beside the previously reported Topo I inhibition time and co

  2019-09-11

  

  Beside the previously reported Topo I inhibition, time and concentration dependent CRM1 inhibitory properties of klavuzon derivatives have been shown as a second mechanism of action in this work. Especially, compounds 3 and 20 are the most effective derivatives and they completely inhibit CRM1 activ

• The use of recombinant ER

  2019-09-11

  

  The use of recombinant ERα and ERβ binding assays offers a relatively inexpensive, rapid technique for screening compounds for potential direct Mevastatin receptor modulatory activity and understanding the mechanisms of existing herbal medicines. For background on the protein production system used

• br Discussion We are reporting a cryptic insertion of chromo

  2019-09-11

  

  Discussion We are reporting a cryptic insertion of chromosome 22 material (EWS) to the long arm of chromosome 11 (11q24, FLI-1) recognizable by FISH in glycoprotein iib iiia inhibitors exhibiting trisomy 8 as the sole cytogenetic anomaly. In ES and PNET tumors, trisomy 8 is the most common secon

• One possible pitfall of using EPAC activators in

  2019-09-11

  

  One possible pitfall of using EPAC2 activators in the treatment of T2DM is their potential to increase glucagon levels. As discussed previously, although the ability of EPAC2 to increase glucagon expression and production is controversial, several studies show that this protein increases Gcg mRNA le

• br Conclusion The present work describes the

  2019-09-11

  

  Conclusion The present work describes the synthesis of 18 naphthoquinonolyl-1,2,3-triazole compounds based on natural product modification with antiplasmodial activity. Lapachol derivatives disclosed higher activity than the natural product. Six of these final modified lapachol 1,2,3-triazole com

• br Acknowledgements br Introduction Serum triglyceride

  2019-09-11

  

  Acknowledgements Introduction Serum triglyceride concentrations increase following ingestion of a fat containing meal resulting in postprandial hyperlipidemia. Peak serum triglyceride levels are observed within 2 to 4h of fat consumption and then gradually return to baseline levels within appr

• In conclusion we demonstrated phenoconversion

  2019-09-11

  

  In conclusion, we demonstrated phenoconversion of CYP3A in stable kidney transplant recipients, and that higher plasma indoxyl sulfate concentrations in these subjects may be involved in the phenomenon. The present findings suggest that dose adjustment of drugs metabolized by CYP3A may be needed in

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