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RHA is an agricultural by product obtained from
2021-02-02
RHA is an agricultural by-product obtained from the burning process of rice hull [7], [8]. Rice hull is the outer layer of paddy grain. About 20% of rice hull converts into RHA when it is burnt during the GZD824 generation processes [8], [9]. If RHA produced at less than 700 °C, it chemically posse
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Introduction Neuropathic pain occurs in
2021-02-02
Introduction Neuropathic pain occurs in approximately one-third of patients with diabetes and is refractory to currently available analgesic drugs (Abbott et al., 2011). This painful diabetic neuropathy (PDN) is associated with elevated levels of methylglyoxal (MG; a reactive glucose metabolite) an
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Another enzyme class that has emerged as a potential alterna
2021-02-02
Another enzyme class that has emerged as a potential alternative to P450s are the so-called ‘unspecific peroxygenases’ (UPOs). They also contain a heme but are extracellularly expressed fungal enzymes that are often more stable than P450 monooxygenases. Importantly, UPOs use H2O2 instead of O2 as th
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br Early developments Historically the advent
2021-02-02
Early developments Historically, the advent of SMEPT can be traced to the 1980′s, where the first example of localized prodrug conversion was achieved using a judiciously placed enzyme – in order to achieve a localized feed of 5-fluorouracil (5-FU). Immobilization of E. coli-derived cytosine deam
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br Conflict of interest br Acknowledgements We wish
2021-02-02
Conflict of interest Acknowledgements We wish to thank Arantza Pérez (University of the Basque Country) for her technical contribution to this study. This work was supported by grants from the Jesús Gangoiti-Barrera Foundation, Gobierno Vasco (GIC07/84), MEC () and SAIOTEK (SA-2008/00046).
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Besides chemopreventive effects against oxidative DNA damage
2021-02-02
Besides chemopreventive effects against oxidative DNA damage we evaluated the protective effects of the three Hypericum sp. and isolated compounds against alkylating DNA damage induced by MMS in HT29 cells. Human exposure to alkylating agents, from different sources, occurs in a continuous way and i
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NSC228155 Of the acidic hydroxyazoles involved hydroxypyrazo
2021-02-02
Of the acidic hydroxyazoles involved, hydroxypyrazole had the weakest acidic profile (pKa in the range of 6–7), although highly deprotonated at physiological pH. During hit optimization, the two pyrazole ring positions available for substitution provide an opportunity for a better exploration of the
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Preparation of the regioisomeric pyridooxazepinones
2021-02-02
Preparation of the regioisomeric pyridooxazepinones 10 and 11 was accomplished utilizing the synthetic sequence depicted in Scheme 3. Amide coupling of 63 and KB SRC 4 synthesis chloride 64 afforded amide 65. Removal of the alcohol protecting group, followed by base catalyzed cyclization afforded a
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We aim to apply the same
2021-02-02
We aim to apply the same technology to target other collagen-binding proteins using motifs from collagens that are specific for other receptors or matrix components. Previously, we synthesized THP libraries, called Toolkits, composed of an active guest sequence flanked by five GPP host triplets that
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In vitro study indicated the cell death of hippocampal
2021-02-01
In vitro study indicated the cell death of hippocampal neurons was mediated by DAPK1 following ceramide-3 treatment (Pelled et al., 2002). the same study showed that DAPK1-deficient mice treated by acyl ceramide exhibit a less sensitivity to apoptosis, this proposed that DAPK1 plays a central role i
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In conclusion our work led to the characterization of
2021-02-01
In conclusion, our work led to the characterization of some signalling events of the CysLT1 receptor variants, at several levels, and showed that a punctual serine mutation could alter the response of receptors to cysLTs. Although atopy is a complex phenotype implicating different cell types, mediat
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br Conclusions CK inhibition protects
2021-02-01
Conclusions CK2 inhibition protects young and aging WM function against an ischemic episode by preserving oligodendrocytes and axonal structure by maintaining mitochondrial integrity. CK2 recruits CDK5 and AKT/GSK3ß signaling to mediate WM ischemic injury in a differential spatiotemporal manner s
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Resistance to avermectins has been associated with point mut
2021-02-01
Resistance to avermectins has been associated with point mutations of GluCls in C. elegans, D. melanogaster, T. urticae and P. xylostella (Dent et al., 2000; Dermauw et al., 2012; Kane et al., 2000; Kwon et al., 2010; Wang et al., 2016a, 2017). Our electrophysiological study found a 8.2-fold reducti
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Parathyroid Hormone (1-34), bovine In the horse oviduct the
2021-02-01
In the horse oviduct, the EP2 receptor was most strongly expressed in epithelial Parathyroid Hormone (1-34), bovine particularly in nonciliated (secretory) epithelial cells as evidenced by IHC. Furthermore, relative amount of EP2 mRNA was greater in the ampulla than in the isthmus, although this lik
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br Advent of SMEPT br SMEPT for localized synthesis
2021-02-01
Advent of SMEPT SMEPT for localized synthesis of nitric oxide Critical evaluation and outlook Examples discussed in this review present SMEPT as a methodology for localized drug synthesis – a unique opportunity for site specific therapeutic interventions using implantable biomaterials. This
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