• Covalent inhibitors are well suited for targeting the E

  2020-05-12

  

  Covalent inhibitors are well suited for targeting the E1 HET0016 of Ubl modifications. Because the E1 enzymes in Ubl modifications, such as the SUMO E1 and Atg7, have a slow turnover rate (Boggio et al., 2004), prolonged inhibition can be achieved without requiring compounds to be stable in circula

• Analysis of Table shows that

  2020-05-12

  

  Analysis of Table 1 shows that compound 7b, in which the biphenyl scaffold does not bear any substituent, displays its inhibitory potency in the micromolar range (IC50 = 11 μM). If the amide bridge is moved from position 1 to 3 of the biphenyl system, product 7c is yielded, whose potency is about 4

• Acanthopanax senticosus Rupr Maxim Harms a nontoxic

  2020-05-12

  

  Acanthopanax senticosus (Rupr. & Maxim.) Harms, a nontoxic herb belongs to the family of Araliaceae, which found in Northeast Asia. A. senticosus traditionally used as a tonic to treat rheumatism, diabetes, and hepatitis [7]. Previous phytochemical and biological investigations found its roots and s

• Cysteine protease activities have been suggested to be impor

  2020-05-12

  

  Cysteine protease activities have been suggested to be important for Giardia’s pathogenesis [[11], [12], [13],16,18,19,21,28,29,35]. Recently several giardial CPs were shown to be released during host cell interactions [9,10]. The three major released CPs have recently been shown to be involved in t

• Here we found that these leukotriene antagonists also

  2020-05-12

  

  Here we found that these leukotriene antagonists also inhibit the effects of nucleotides acting at P2Y receptors in dU937 cells, which are known to express a number of nucleotide receptors, such as P2Y2 or P2Y4[30]. In an effort to characterize the P2 receptor subtypes subject to negative modulation

• Recently cross talk between DDR and

  2020-05-11

  

  Recently, cross-talk between DDR2 and the insulin receptor and between Notch1 and DDR1 was proposed. Stimulation of cells with collagen I and insulin promotes Tyr740 as well as total tyrosine phosphorylation of DDR2 receptor to a greater extent than the phosphorylation stimulated by collagen I alone

• Advances in the total chemical synthesis

  2020-05-11

  

  Advances in the total chemical synthesis of ubiquitin have enabled the efficient synthesis of new and improved ubiquitin-based reagents. Using an optimized linear synthesis, ubiquitin can now be easily obtained in high yield and purity [35]. Using this synthetic methodology, ubiquitin can be functio

• how to dilute a solution Introduction Protein ubiquitination

  2020-05-11

  

  Introduction Protein ubiquitination is a posttranslational modification that plays a major role in almost all cellular processes in eukaryotes (Hochstrasser, 2009; Komander & Rape, 2012). It involves the covalent attachment of ubiquitin (Ub) via its C-terminal glycine carboxylate to a primary amine

• br Conclusions br Conflict of interest statement br Acknowle

  2020-05-11

  

  Conclusions Conflict of interest statement Acknowledgments This research was funded by São Paulo Research Foundation (FAPESP) (ProcessN. 2012/08621-1). Thanks to F.J.H. Blázquez and the staff of the Laboratório de Anatomia Microscópica e Imuno Histoquímica (LAMIH − FMVZ − USP) for the permi

• A number of studies have been carried out

  2020-05-11

  

  A number of studies have been carried out to understand lipid production pathways and to increase TAGs level in higher plants. Overexpression of key nrf2 inhibitor of the Kennedy pathway until now is by far the most successful strategy to increase TAG lipid content in Brassica napus, Arabidopsis th

• her2 inhibitor br Conclusions This study showed that in EOC

  2020-05-11

  

  Conclusions This study showed that in EOC cells, tyrosine kinase receptor DDR1 was expressed mainly in EOC her2 inhibitor with an Epithelial phenotype. The repressed expression of DDR1 in EOC cells with Mesenchymal phenotype could be due to the higher CpG methylation levels observed at the promo

• br Cysteine proteases as molecular targets for trypanosomati

  2020-05-11

  

  Cysteine proteases as molecular targets for trypanosomatid diseases Approaches relying on a molecular target, such as SBDD and target-based screening, have supported outstanding scientific developments in current pharmaceutical R&D. By integrating experimental and computational methods, these str

• Previous studies revealed the expression of the CCR

  2020-05-11

  

  Previous studies revealed the expression of the CCR3 receptor in neurons and its neuroprotective function using mice lacking CCR3 expression (Wainwright et al., 2009). The regulation of CCR3 receptor expression in the microglia and astrocytes was shown in neurological disorders and has been demonstr

• Recently several Pt IV complexes as prodrugs

  2020-05-11

  

  Recently, several Pt(IV) complexes as prodrugs have been designed and studied to enhance anti-tumor efficacy of traditional Pt(II) drugs, improving their cellular uptake and blood-circulation time [26], [27], [28], [29]. Compared with their Pt(II) counterparts, six-coordinated Pt(IV) complexes with

• br Acknowledgements br Introduction Protein tyrosine phospho

  2020-05-11

  

  Acknowledgements Introduction Protein–tyrosine phosphorylation, catalyzed by protein–tyrosine kinases and protein–tyrosine phosphatases, has a pivotal role in the regulation of a wide variety of cellular processes. Similar numbers of tyrosine kinases and tyrosine phosphatases are encoded by th

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