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The X ray crystal structure of palbociclib bound to
2020-11-25
The X-ray crystal structure of palbociclib bound to CDK6 without a TMPyP4 tosylate (PDB ID: 5L2I) is very similar to that of the CDK6-cyclin V structure (Fig. 7B). However, the drug binds to the αCout conformation of monomeric CDK6 while it binds to the αCin conformation of the CDK6-cyclin V comple
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br Materials and methods br Results br
2020-11-24
Materials and methods Results Discussion This study is the first to our knowledge that describes upstream cis-elements and transcription factors that are important for Crm1 expression and that drive its high expression in cancer and transformed cells. Using deletion and mutation analysis we
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br Acknowledgment br Introduction Pesticides are largely use
2020-11-24
Acknowledgment Introduction Pesticides are largely used in agriculture to enhance food production and, to a lesser extent, to control unwanted pests and disease vectors in public health. However, these compounds are often associated with toxicity in non-target species including humans. Occupat
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Several reasons may explain that other
2020-11-24
Several reasons may explain that other studies using PDE-5-Is yielded negative or contradictory results [30], [31], [32]. Lee [30] applied 50mg sildenafil to seven patients with liver cirrhosis. NO and cGMP in the hepatic Hoechst 34580 significantly increased, hepatic and pulmonary resistance decr
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Evidence for interactions between the endothelin and the ang
2020-11-24
Evidence for interactions between the endothelin and the angiotensin system has also become plentiful. It has become clear that the two systems, in addition to acting independently, can act synergistically (Emori et al., 1989, Imai et al., 1992) as well as promote the peptide mRNA expression in endo
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In rodent models the loss of estrogens
2020-11-24
In rodent models, the loss of estrogens through ovariectomy has been shown to promote the development of intracranial aneurysms. Conversely, the administration of an 17 alpha hydroxylase receptor beta agonist restores its protective effect, but is abolished with the introduction of a nitric oxide sy
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Early VL diagnosis makes it possible
2020-11-24
Early VL diagnosis makes it possible to formulate a quicker and more effective treatment against the disease, which could increase the possibility of a cure for the patients, as well as reduce the toxicity of the drugs (Coelho et al., 2009); however, conventional and molecular parasitological method
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For most enolases fluoride acts as an inhibitor while Mg
2020-11-24
For most enolases, fluoride acts as an inhibitor, while Mg2+ is the most important metal activator. In yeast systems, metal cations and fluoride bind to enolase at the active center of the enzyme, forming a complex. The complex blocks the binding of substrates to the enzyme in yeast systems, thereby
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Since the number of peptides hydrolized by
2020-11-24
Since the number of peptides hydrolized by PEP is quite large, it is not easy to relate the increase of enzymatic activity with the altered changes of a concrete peptide. However, it is noticeable that imbalances of several natural substrates of PEP [6], such as angiotensins, bradykinin, vasopressin
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Previously we showed that MS a
2020-11-24
Previously, we showed that MS-10, a combined extract of Cirsium japonicum var. Maackii (Maxim.) Matsum. (Korean milk thistle) and Thymus vulgaris L., increases the efficiency of estrogen in the estrogen-deficient state by activating the estrogen receptor (ER). MS-10 increased bone mineral density (B
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EBI and its ligand s
2020-11-24
EBI2 and its ligand(s) EBI2 was found in a screen of upregulated genes in human B cells upon infection with EBV [1]. EBI2 is a G-protein (Gαi type) coupled receptor [2] but as long as 18 years after its discovery the nature of its ligand remained undisclosed. With the help of transfected cell lines
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In another study Nutlin a mediated p activation induced
2020-11-24
In another study, Nutlin-3a-mediated p53 activation induced strong negative impact on NF-κB signaling in LPS-stimulated neutrophils and macrophages [34]. Nutlin-3a limited cellular immune response to LPS, partly by attenuating DNA binding activity of NF-κB and impairing transcription of its target c
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Immunofluorescence assays were performed to localize
2020-11-23
Immunofluorescence assays were performed to localize the enzyme during growth and differentiation to further characterize Giardia E1. As stated before, the assays showed that the SirReal2 generated recognized specific E1 forms (E1-114, E1-90 and E1-67 with anti-gNTE1; and E1-47 with anti-gE1CT); th
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br Ubiquitination and deubiquitination pathways
2020-11-23
Ubiquitination and deubiquitination pathways Ubiquitination is a part of the post-translational modification (PTM) process. Ubiquitination affects proteins in various ways, but its main functions are to signal protein degradation via the 26S proteasome, modify cellular location of proteins, affec
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Advances in the total chemical
2020-11-23
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
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