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br Acknowledgements This work was supported
2020-06-23
Acknowledgements This work was supported by the European Committee Fifth Framework Project QLK5-1999-01360. We are grateful to Dr. T.T. Hoang for the provision of plasmids pEX18Tc, pPS858 and pFLP2, Prof. B.L. Wanner for providing us with the plasmid pKD4 and related strains, and Prof. P. Soucail
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Furthermore in silico physicochemical characters and pharmac
2020-06-22
Furthermore, in silico physicochemical characters and pharmacokinetic parameters for the synthesized compounds were predicted using dedicated computer software [34], [35], [36] to ensure successful in vivo therapeutic activity. Practical logP testing was performed and compared to the theoretical val
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LPA is known to regulate the peroxisome proliferator activat
2020-06-22
LPA is known to regulate the peroxisome proliferator-activated receptor γ and the reorganization of actin cytoskeleton [58]. However, the physiological functions of LPA in cells are still poorly understood. The simultaneous production of PA with/without 1-LPA or 2-LPA may be important to maximize a
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br Materials and methods br Results br
2020-06-22
Materials and methods Results Discussion Natural compounds and their derivatives have been investigated as candidates for the treatment of bone diseases and can also be the sources of nutraceutical agents and therapeutic agents [28]. Using peptides as therapeutic effects on bone-related dis
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The quaternary structure of many of the family B members
2020-06-22
The quaternary structure of many of the family B members (i.e., secretin, glucagon, glucagon-like peptide and CX-6258 receptor receptors) have been actively studied and it has been demonstrated that they can form homodimers/oligomers (Gao et al., 2009; Ng & Chow, 2015; Ng, Lee, & Chow, 2013). Harik
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br Steroid biosynthesis br Steroid hormone metabolism in bre
2020-06-22
Steroid biosynthesis Steroid hormone metabolism in breast cancer Conclusion Steroid hormones elicit their biological actions primarily by binding to steroid receptors such as the ER, AR, PR and GR. Although classical breast cancer diagnostic panels assess the expression of the ER and PR, as
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BV6 DDR is one of two
2020-06-22
DDR1 is one of two, non-integrin tyrosine kinase receptors activated by collagen. Although DDR1 has five isoforms (1a, 1b, 1c, 1d, 1e) generated by alternative splicing, only DDR1a and 1b have active kinase domains, whereas DDR2, encoded by a distinct gene, has one isoform (Vogel et al., 2006). Coll
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Nimodipine is an L type calcium channel antagonist that
2020-06-22
Nimodipine is an L-type calcium channel antagonist that reduces excessive calcium influx during pathological conditions, contributing to its neuroprotective properties (Zornow and Prough, 1996; Kobayashi and Mori, 1998). Autophagy can be induced by increased [Ca2+] (Rami et al., 2008). Nimodipine si
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br Conclusions and future directions In recent years we
2020-06-22
Conclusions and future directions In recent years we saw major advances in our knowledge of H2A-DUB biology, with discovery of novel mammalian H2A-DUBs, better understanding of their biochemical properties, and development of several animal models to address their in vivo functions. However at pr
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The death associated protein kinase DAPK is
2020-06-20
The death-associated protein kinase (DAPK) is an actin-associated, calcium/calmodulin-dependent enzyme with serine/threonine kinase activity [11], [12]. DAPK is a pro-apoptotic gene and participates in various apoptotic systems, such as TNF-α- and Fas-triggered apoptosis [10], IFN-γ-induced cell dea
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Phylogenetically three related CXC chemokines are classified
2020-06-20
Phylogenetically three related CXC chemokines are classified as the possible ligands for the teleost CXCR1 and CXCR2. They are referred to as CXCL8_L1 (CXCL8/IL-8/CXCa), CXCL8_L2 (CXCc) and CXCL8_L3 (Alejo and Tafalla, 2011, Chen et al., 2013, Laing et al., 2002, Laing and Secombes, 2004, Nomiyama e
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The contribution of local ETA and ETB receptors towards heat
2020-06-20
The contribution of local ETA and ETB receptors towards heat hyperalgesia induced by inoculation of XC tumor Fumagillin in the paw of mice has been demonstrated by Baamonde and colleagues (Baamonde et al., 2004). Furthermore, using neuropathic and inflammatory nociception models, several studies hav
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Since the initial identification of DNA ligase
2020-06-20
Since the initial identification of DNA ligase inhibitors by a structure-based approach [[18], [26]], there have been several reports describing LigI inhibitors using computer modelling and derivatives of the original DNA ligase inhibitors [[49], [50], [51]]. While these studies have shown that the
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The possibility that a carboxyl group
2020-06-20
The possibility that a carboxyl group attached to the or position of an -arylaminomethylenemalonate ester would lead to increased selectivity for DHODH has been tested and found not to be the case. Indeed, reduced selectivity compared with the corresponding ester is observed and is attributed to a
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This hydrophobic biphenyl tail gave good binding affinity fo
2020-06-20
This hydrophobic biphenyl tail gave good binding affinity for human DHODH enzyme (IC Wortmannin was found to be the main metabolite in human microsomes and it was 100-fold less active against hDHODH than the ester. In an attempt to identify the specific non-covalent binding interactions which were
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