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Present malarial chemotherapies mainly rely on a very few ch
2019-07-24
Present malarial chemotherapies mainly rely on a very few chemotypes or their allied structures such as quinolines, anti-folates and some cyclic endo-peroxides (Nayyar et al., 2012). Over the last few decades, the extensive and repetitive deployment of these drugs has stimulated resistance in the pa
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br Fragment based drug discovery FBDD is a powerful
2019-07-24
Fragment-based drug discovery (FBDD) is a powerful method to discover drug leads and has been widely adopted in both academia and industry. FBDD can be used to explore chemical hdac inhibitors space with libraries which are smaller in size, producing drug leads with high ligand-binding efficiency
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Two major mechanisms including apoptosis and
2019-07-24
Two major mechanisms including apoptosis and oxidative stress have been suggested for MTX-induced cytotoxicity (Hafez et al., 2015; Neuman et al., 1999; El-Sheikh et al., 2015). It has been reported that MTX promotes cell death via apoptosis in both cancerous and non-transformed cells (Mazur et al.,
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It is well known that the tumor suppressor p plays
2019-07-24
It is well known that the tumor suppressor p53 plays an important role in regulating the Swainsonine and cellular senescence [43,46,48]. For example, FOXO4 could interact with P53, which selectively induced apoptosis in senescent cells [48]. In addition, loss of MECP2 was found to lead to the induct
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During recent years two primary types
2019-07-24
During recent years, two primary types of models have been applied for calculating various thermodynamic properties of amino Nanaomycin A solutions, i.e. excess Gibbs energy (gE) models used numerously to describe the solubility of amino acid solutions, and equations of state (EOS) models appropria
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Leukotrienes themselves are implicated in the development of
2019-07-24
Leukotrienes themselves are implicated in the development of gastrointestinal ulcers, asthmas, and different inflammatory processes [18], [19]. It is noteworthy that COX isozymes and LOX share the same substrate arachidonic acid; therefore, inhibition of prostaglandins production by cyclooxygenase p
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In order to validate the ATP competitive
2019-07-24
In order to validate the ATP competitive mode of inhibition, compound 12 was selected as a representative inhibitor of this series, and the IC50 values were determined at eight different concentrations of compound 12 ranging from 0.001 to 100 μM, and repeated four times using different ATP concentra
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The histologic finding that EBV infected B cells
2019-07-24
The histologic finding that EBV-infected JNJ 5207852 dihydrochloride in infectious mononucleosis tend to avoid the GCs and instead accumulate under the epithelium of certain mucosal tissues34, 129 could be explained by the above-mentioned expression patterns of chemokine receptors on EBV-infected B
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Enzyme mimics belong to a type
2019-07-23
Enzyme mimics belong to a type of rising catalysts which show the similar function with their corresponding natural enzymes [20], [21], [22], [23], [24], [25], [26], [27], although their structures are different from natural enzymes. In the area of prodrug activation, the widely-used enzyme mimics a
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Emphysema is an important component
2019-07-23
Emphysema is an important component of COPD, which is responsible for airflow limitation. In the present study, a significant airspace enlargement was observed 21 days after elastase administration. Interestingly, daily administration of olaparib provided greater protection against emphysema as comp
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Here we describe preparation of three stable
2019-07-23
Here, we describe preparation of three stable conjugates that are linked by either oxyester, disulfide, or isopeptide bonds (Fig. 10.1). Each of these conjugates depends upon the prior purification of E2 and ubiquitin proteins that have been engineered to favor specific linkages. For the oxyester- a
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lactacystin The Lysine mutant is located in the tail
2019-07-23
The Lysine429 mutant is located in the tail region of 5-HT2A, which is predicted to be unstructured. This region has been shown to interact, in vitro, with PSD95 and leads to differences in signaling (Xia et al., 2003). The ASK motif, a component of the tail region, is also important for regulation
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Findings from the present study indicate that CRF receptors
2019-07-23
Findings from the present study indicate that CRF1 receptors are especially important in fear acquisition. CP154,526 given before acquisition training, at least partly, reinstated the fear-potentiated startle response and blocked the development of contextual conditioned fear in SERT−/− rats. CP154,
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br Theory br Method To test
2019-07-23
Theory Method To test our hypotheses as shown in Fig. 1, we conducted a survey at an international media company (hereafter referred to as ‘MediaCo’) headquartered in the UK. Its 5500 employees are dispersed throughout the world, partly due to massive acquisitions within the past decade. In ex
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C646 chemical Furthermore positioning the naphthalene nucleu
2019-07-23
Furthermore, positioning the naphthalene nucleus in 3d within the main active site and forming one hydrogen bond with Tyr385 in addition to many hydrophobic interactions with Val349, Leu352, Gly526, Ala527 and Leu531 residues, correlates well with the position and hydrophobic interactions of the tri
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