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Accordingly we prepared three compounds and as shown in
2019-10-16
Accordingly, we prepared three compounds (, , and ) as shown in . Condensation of commercially available PLX 4032 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 compound ra
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br Results and discussion br Conclusion A new series of
2019-10-16
Results and discussion Conclusion A new series of 2-mercapto-quinazolin-4-one analogues is designed and synthesized to possess electron withdrawing or donating functional groups (Cl or CH3O) at position 6- or 7-, 4-methoxyphenyl function at position 3. The 2-mercapto function is used to connec
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Traditionally serum triglycerides have been measured in
2019-10-16
Traditionally, serum triglycerides have been measured in the clinic in the fasted state in order to reduce variability and also to facilitate the calculation of LDL-cholesterol via the Friedewald equation, which was derived using fasted samples (Warnick and Nakajima, 2008). We have previously report
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Some mechanistic experiments performed in the
2019-10-16
Some mechanistic experiments performed in the early 2000s by Ongusaha et al. [78], suggest that DDR1 induction protects 78 2 from apoptosis in a p53-dependent manner, and that impairment of DDR1 expression or function leads to a pronounced increase of DNA damage-induced apoptosis. This evidence sug
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Currently approved anti obesity drugs for long term use
2019-10-16
Currently approved anti-obesity drugs for long term use such as orlistat, lorcaserin and liraglutide are efficient in reduction of weight gain but are limited in usage due to their adverse effect profile and higher cost (Krentz et al., 2016; Mopuri and Islam, 2017). In chemical d to this, plant der
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Within the cluster of North African populations the
2019-10-16
Within the cluster of North African populations the Sousse population sample is somewhat different from the other six populations. One has to analyze more in depth the reasons of this isolation that has been shown by other genetic studies (Fadhlaoui-Zid et al., 2015). It seems that the particular ge
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bgb324 pathway Synthetic peptides have proven highly valuabl
2019-10-16
Synthetic peptides have proven highly valuable in replicating the characteristics of collagen and in defining the sites on collagen essential for binding and studying protein–collagen interactions. There are, however, disadvantages to synthetic collagen-like peptides. First, the thermal stability of
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An increased CK activity was found in septal
2019-10-16
An increased CK2 activity was found in septal neuronal roscovitine dissected from rat embryos after hypoglycemia [36]. These data indicated that CK2 activity is not only regulated by insulin but also by the glucose concentration. One essential step in insulin action is the binding of the hormone t
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Phosphorylation of small GTPases has been also observed to
2019-10-16
Phosphorylation of small GTPases has been also observed to affect binding affinity for the GDP/GTP cycle regulators notably GDP dissociation inhibitor (GDI) [10]. Indeed the EGF or cAMP-dependent phosphorylation of Cdc42 is associated with enhanced Cdc42–GDI interaction [8], [11]. RhoA inhibition by
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Recent studies have shown that
2019-10-16
Recent studies have shown that the extracellular regulated protein kinase 1 and 2 (ERK1 and ERK2), commonly referred to collectively as ERK 1/2, are members of the mitogen-activated protein kinase (MAPK) family. This family of kinases transport signals from the surface of the cell to the nucleus, th
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Imatinib STI is a first line tyrosine kinase inhibitor TKI
2019-10-15
Imatinib (STI-571) is a first-line tyrosine kinase inhibitor (TKI) targeted at breakpoint cluster region-Abelson kinase (ABL) for the treatment of chronic myeloid leukemia (CML) [26]. As a type II inhibitor, imatinib achieves significant selectivity by binding to an inactive DFG-out conformation (DF
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Gefitinib br Inhibiting APC C during Interphase and prior to
2019-10-15
Inhibiting APC/C during Interphase and prior to Anaphase Because ubiquitylation by APC/C triggers cell division, it is essential that APC/C is restrained until cells are prepared for its substrates to be degraded. In addition to regulation by phosphorylation, an additional layer of control comes
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Structural characterization of A S Given the low specific ac
2019-10-15
Structural characterization of A1S_0222. Given the low specific activity of our protein preparations and the considerable problems to concentrate the protein to levels above 2.5 mg/mL, we employed SAXS to structurally characterize and generate a low-resolution model of A1S_0222 in solution. Fig. 5 a
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proteasome inhibitor Electron transport via DHODH activity w
2019-10-15
Electron transport via DHODH activity will allow the generation of mitochondrial ROS without the consumption of α-ketoglutarate or NADH. Glutamine-dependent flux through the TCA cycle and oxidative phosphorylation can also enable generation of mitochondrial ROS (Weinberg et al., 2010). The latter pr
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The IV chains of mature
2019-10-15
The α3/α4/α5(IV)-chains of mature GBM are built exclusively by podocytes (not by endothelial cells) (Abrahamson et al., 2009), placing the podocytes into the focus of GBM-diseases such as Alport syndrome. Alport syndrome (AS) is caused by mutations in the COL4A3, 4 or 5 genes coding for the α3/α4/α5
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