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A growing body of data indicates that
2020-04-06
A growing body of data indicates that endothelial NOS (eNOS) is a rate-limiting enzyme for the synthesis of nitric oxide (NO), its downstream nearly molecule. High pathological concentrations of NO produced from inducible NO synthase (iNOS) induce apoptosis, whereas a reduction in the concentration
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Nrf and HO are key
2020-04-06
Nrf2 and HO-1 are key factors in the regulation of oxidative stress in the body. Research has shown that KLF2 can activate Nrf2 and HO-1 [14]. To investigate the mechanisms by which KLF2 regulates eNOS uncoupling and oxidative stress, Nrf2 was inhibited or HO-1 was knocked down in KLF2 overexpressin
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Due to the high attractiveness
2020-04-06
Due to the high attractiveness of E2 and E3 ligases as drug targets, a number of drug discovery assays have been published, based on detection by fluorescence (Dudgeon et al., 2010, Krist et al., 2016, Zhang et al., 2004), imidazoline receptors (Davydov et al., 2004, Huang et al., 2005, Kenten et a
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br Conclusions br Acknowledgements br Introduction Liver can
2020-04-06
Conclusions Acknowledgements Introduction Liver cancer was the fifth most common cancer and the second leading cause of cancer-related death worldwide [1]. Most of primary liver cancers (70–90%) occurring worldwide are hepatocellular carcinoma (HCC) [2]. Persistent hepatitis B virus (HBV) i
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Finally considering the encouraging inhibitory and selectivi
2020-04-06
Finally, considering the encouraging inhibitory and selectivity properties of compound and against isolated CK1δ, we have also acquired a very preliminary cytotoxicity profile on human ovarian carcinoma cell line (2008) and on its cisplatin-resistant clone (C13). Results showed that after 48h of e
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In contrast irinotecan has shown much less myelosuppression
2020-04-06
In contrast, irinotecan has shown much less myelosuppression and may be more active in Ewing sarcoma both alone and in combination with temozolamide. One phase II study of 13 heavily pretreated Ewing sarcoma patients demonstrated a response rate of 38% including 2 complete responses (Bisogno et al.,
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The interface between the E
2020-04-06
The interface between the E3 ligase and the E2 enzyme can vary, and ZNF451 and SP-RING ligases stabilize this interaction via noncovalent binding to a scaffold SUMO (SUMOB) on the backside of the E2 (Cappadocia et al., 2015; Eisenhardt et al., 2015; Streich & Lima, 2016). By contrast, RanBP2 does no
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sc4 library Over the past decade targeting DNA repair protei
2020-04-06
Over the past decade, targeting DNA repair proteins has emerged as an effective tool to enhance chemosensitivity of malignant cells [9]. However, identification and selection of the proper target of DNA repair pathways is critical to increase cytotoxic activity of chemotherapeutic agents in cancer c
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In agreement with the evidence
2020-04-03
In agreement with the evidence on the Plg-binding function of tapeworm enolases, eukaryotic enolases have been shown to be multifunctional proteins, with other activities besides their role as glycolytic enzymes (Pancholi, 2001). In this respect, several flatworms have been proved to express enolase
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br Chemistry Scheme shows the synthesis of compounds from co
2020-04-03
Chemistry Scheme 1 shows the synthesis of compounds 15-1–15-33 from commercially available 2-(4-aminophenyl)acetonitrile (8a). Protection of the starting material 8a with di-t-butyl dicarbonate afforded 9. The reaction of 9 with methyl 1-chloroisoquinoline-4-carboxylate in the presence of sodium
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As described above we designed and synthesized a
2020-04-03
As described above, we designed and synthesized a new 1,4-di-substituted isoquinoline lead compound, and was identified as a ligand with moderate potency for the CRTH2 receptor. We initially we examined the effects of the steric factor of R group on the CRTH2 binding potency (). When the methyl grou
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Crystal structures of various CRM complexes have provided in
2020-04-03
Crystal structures of various CRM1 complexes have provided insight into molecular details of the interactions between CRM1 and its interaction partners during the transport cycle. CRM1 cooperatively binds RanGTP and cargo in the nucleus (Paraskeva et al., 1999). In this ternary complex, RanGTP is lo
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Introduction Trichloroacetic acid TCA might enhance the acti
2020-04-03
Introduction Trichloroacetic PF-670462 mg (TCA) might enhance the activation of T cells and disrupt various activities of peripheral T cells [1], which is related to human immune function and reduces human immunity. Trichloroethylene (TCE) has been widely used in many manufacturing industries [2],
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Epidermal Growth Factor (EGF), human recombinant The binding
2020-04-02
The binding pattern of 1 was analysed by flexible molecular docking. The Epidermal Growth Factor (EGF), human recombinant inserted into the narrow ATP binding site of CK2 (Fig. 2). As shown the aliphatic chain of 1 was located at the edge of the pocket and established van der Waals interactions with
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It is common for plants that are deficient in P
2020-04-02
It is common for plants that are deficient in P to invest in their roots in order to maximise P uptake from the soil. Here, plants grown in soil amended with OA had a higher root biomass:shoot letrozole cost ratio compared with plants in the INORG-P treatment. Additionally, greater allocation of C
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