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In our former work our
2020-03-09
In our former work, our interest was in discovery of novel VEGFR-2 inhibitors as anti-angiogenesis agents. Along this line, with natural alkaloid taspine as the lead compound, rounds of structure optimization were performed to develop novel VEGFR-2 inhibitors [[13], [14], [15]]. Among them, BPS-7, b
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Films treated with Diaz ES VWFIIINle but
2020-03-07
Films treated with Diaz-ES-VWFIIINle but not exposed to UV light supported only slight platelet deposition, suggesting that passively-bound peptides were removed under shear. However, treatment with Diaz-ES-VWFIIINle and UV restored platelet surface coverage to about 50% of the level on native colla
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In the course of our program which was aimed
2020-03-07
In the course of our program, which was aimed at developing CRTH2 antagonists for the treatment of allergic diseases, we have been pursuing a new class of potent and selective CRTH2 antagonist lead based on the structures of CRTH2 antagonists known to date (, , ). Using a fused 6–6-membered ring sys
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Two isoforms of intracellular ER ER and ER after binding
2020-03-07
Two isoforms of intracellular ER, ERα, and ERβ, after binding to estrogens and translocate to the nucleus, activate some transcription factors and signaling pathways. The deregulation of estrogenic pathways can elevate transcriptional activity contributed to the development of cancer. Expression of
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protein phosphatase inhibitor The third challenge is to unde
2020-03-07
The third challenge is to understand the mechanisms of drug resistance. There are several different mechanisms of ES tumor to develop drug resistance. First, cancer stem cells are capable of proliferate and generate tumor cells with new sets of mutations which may harbor different protein targets [1
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EphB appears to be a low affinity receptor for
2020-03-07
EphB4 appears to be a low-affinity receptor for rhEpo based on the biochemical data. The concentration of rhEpo used for the biological experiments (50 IU/ml) corresponds to 10–15 nM, which is 1% to 2% of the KD value (KD = 881 nM) for the binding of rhEpo to EphB4, as measured in the MST assay. The
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It is believed that emphysema
2020-03-07
It is believed that emphysema in smokers is mediated by proteases released from inflammatory TBCA mg that cause destruction of the extracellular matrix in alveolar septa [1]. Metalloprotease-12 is mainly released by macrophages and is considered the enzyme responsible for emphysematous lesions in e
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br Material and methods br Results br Discussion
2020-03-07
Material and methods Results Discussion A. fumigatus utilizes several virulence factors that facilitate its establishment in human hosts. Among these factors, the best known are hydrolytic enzymes such as proteases and phospholipases, toxins, melanine and catalases that neutralize the react
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br Acknowledgments br Multicellular organisms respond rapidl
2020-03-07
Acknowledgments Multicellular organisms respond rapidly, and adapt to cellular stress to maximize cell survival. The cellular stress response, also called (ISR), is universally conserved and independent of the stressor. ISR induces rapid, transient reprogramming of cellular protein translation
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A growing number of other post translational modifications
2020-03-07
A growing number of other post-translational modifications are implicated in regulation of the ubiquitin system, including substrate modification by hydroxylation, glycosylation, acetylation, methylation, modification by poly(ADP-ribose) (PAR), and attachment of ubiquitin-like modifiers. The HIF1-α
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Given the important regulatory roles Ub signaling
2020-03-07
Given the important regulatory roles Ub signaling pathways play in eukaryotes, bacterial pathogens and viruses have evolved elaborate mechanisms to hijack host Ub signaling pathways and evade the immune response. This is highlighted by the numerous E3 Ub ligases and spectrum of DUBs encoded by bacte
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br DNA PK After sensing and binding to the
2020-03-07
DNA-PK After sensing and binding to the DSB, Ku quickly recruits DNA-PKcs to the site of the DNA break. Similar to Ku70/80, recruitment of DNA-PKcs to DSBs occurs within seconds of their creation [12]. The interaction between Ku70/80 and DNA-PKcs requires the presence of dsDNA and the complex for
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In studies directed toward the development of sequence speci
2020-03-07
In studies directed toward the development of sequence-specific major-groove binding small gli1 [11], we desired a non-intercalating molecular scaffold that could direct attached moieties into the major groove. As an initial step toward this goal, we wished to study the DNA binding mode and affinit
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Nowadays colorimetric assay has been applied
2020-03-07
Nowadays, colorimetric assay has been applied in detecting DNA MTase activity. Li et al. used DNA modified gold nanoparticles (AuNPs) coupled with enzyme-linkage reactions to detect the activity of methylases [20]. In a previous study, our group presented a label-free colorimetric method, using unmo
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br Introduction In mammals there are ten known
2020-03-07
Introduction In mammals there are ten known isoforms of the enzyme diacylglycerol kinase (DGK), as well as gene splice variants. Enzymes of this family all have a homologous active site but differ widely in their molecular mass, mechanisms of activation and biological function (Shulga et al., 201
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