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As mentioned above variation of the
2023-09-05
As mentioned above, variation of the A-ring was undertaken in order to improve microsomal stability and kinase selectivity relative to mma f (). 1-Imidazole-2-carboxamides with substitution at the 4-position (–) were mostly tolerated with 4-cyano-imidazole-2-carboxamide () having comparable inhibito
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Aurora A overexpression is also
2023-09-05
Aurora-A overexpression is also related to the activation of NF-κB, a potent anti-apoptotic effector that may play a role in preventing apoptosis in cancer Erastin synthesis [18]. These data show that we are still at the beginning of unraveling the complex mechanism by which these gene products an
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exemplifies three of the compounds investigated in the selec
2023-09-05
exemplifies three of the compounds investigated in the selection for a candidate drug (CD). Our first criteria was an IC monensin as such did not show any genotoxicity in the SOS/umu assay, but this does not say anything about any possible genotoxicity of its metabolites or degradation products. A
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The tumor suppressor function of LOX
2023-09-05
The tumor-suppressor function of 15-LOX-2 in normal prostate epithelial cells may be explained by the induction of replicative senescence [14,15]. Thus, 15-LOX-2 is overexpressed in age-dependent prostatic hyperplasia, but cell senescence may hinder progression to malignant transformation. Notwithst
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br Conflicts of interest br Financial support This work was
2023-09-05
Conflicts of interest Financial support This work was supported by grants from the Fondazione Cariplo [Grant number 2011-0463] (Carini); and by Funds for Original Research of the Università del Piemonte Orientale (2016, Project: Carini-Boldorini). The sponsors had no involvement in study desig
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br Declaration of interest br Funding br Introduction The
2023-09-05
Declaration of interest Funding Introduction The endocrine disruptor bisphenol A (BPA) is a high-production chemical used in several consumer products, including polycarbonate bottles, epoxy resins, dental sealants, and thermal paper receipts (Geens et al., 2012). Importantly, BPA monomers
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Apoptosis a major process of programmed cell
2023-09-05
Apoptosis, a major process of programmed cell death, and in response to many chemopreventive agents (Jeyamohan et al., 2016). In general, two major signaling pathways control apoptosis, namely, a pathway mediated by cell death receptor and a pathway mediated by mitochondrion, and possible drug targe
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br Drugs with documented pro apoptotic effects on platelets
2023-09-05
Drugs with documented pro-apoptotic effects on platelets More than 200 drugs are reported to cause thrombocytopenia [5,42]. The concept of platelet apoptosis is relatively new and was only recently evaluated in the context of drug-induced thrombocytopenia [43]. Table 2 lists the drugs presently k
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Applications for protein switches are numerous In
2023-09-05
Applications for protein switches are numerous. In diagnostics, protein switches can detect analytes as components of inexpensive homogeneous assays that do not require specialized equipment or time-consuming incubation and washing steps characteristic of immunoassays [8]. Protein switches have also
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There are increasing repeated reports of
2023-09-05
There are increasing repeated reports of amphotericin B-resistance in pathogenic fungi including Candida spp. [35], [36]. Nolte et al. characterized some fluconazole and amphotericin B-resistant Candida albicans isolates from leukemia patients [37]. Fan-Havard et al. (1991) have shown multi-antifung
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Among all the polysaccharide derivatives cationic carbohydra
2023-09-05
Among all the polysaccharide derivatives, cationic carbohydrate polymers such as quaternary ammonium salts and quaternary phosphonium salts have been the most popular and most efficient target cell adhesion molecules in medical applications [24] and water treatment [25]. Recently, quaternary phosph
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br HIF Signaling in AA Therapy Resistance
2023-09-05
HIF-α Signaling in AA Therapy Resistance An important result emerging from Phase 3 clinical trials testing AA therapies is improvement of progression-free survival (PFS) that is not accompanied by enhanced overall survival (OS) [26]. This dichotomy has been attributed to mechanisms of acquired re
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In order to postulate its binding
2023-09-05
In order to postulate its binding mode in APN, hcv virus 13v was docked into the active site of APN (PDB code: 2DQM) using Sybyl_X 1.3. As illustrated in Fig. 5A, the catalytic zinc ion of APN was chelated by the hydroxamate moiety of 13v, and the S1, S1′ and S2′ pockets of APN were occupied by the
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br Material and methods br Results br Discussion
2023-09-05
Material and methods Results Discussion RSV is a major cause of lower respiratory tract infections in infancy and early childhood. Several observations suggest that immunological mechanisms may be the key to understand the severity of RSV bronchiolitis in infancy. Several laboratories have
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br Conclusion br Conflict of
2023-09-05
Conclusion Conflict of interest Acknowledgments We thank Nancy Kerkvliet for helpful advice. The research in the lab of CE and THS is supported by the Deutsche Forschungsgemeinschaft (grants ES103/7-1 and 9-1, HA7346/2-1). We apologize to all authors whose work could not be cited due to lim
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