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br Halogenases Enzymatic C H activation
2020-12-18
Halogenases Enzymatic C–H activation leading to halogenation is another emerging area in biocatalysis [55,56]. Incorporation of halogen atoms during medicinal chemistry eff ;orts is a well-established practice, presenting an effective means to control the molecule’s bioactivity and physicochemical
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br Clinical potential of ET receptor biased
2020-12-18
Clinical potential of ET receptor biased ligands Is there a clinical need for ET receptor biased ligands? Evidence is strongest from research in epithelial ovarian cancer demonstrating that ET-1 stimulated ETA-mediated β-arrestin signalling leads to activation of the oncogenic mediator NF-κB [21]
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There are conflicting studies on ET axis and its
2020-12-18
There are conflicting studies on ET axis and its relationship with clinicopathologic parameters in various cancers. Endothelin axis expression in the tissue and in blood has been associated with advanced cancer characteristics in colorectal, breast, and prostate cancer, while showing no linkage to c
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Among the high value compounds derived from
2020-12-18
Among the high value compounds derived from agricultural residues there are enzymes with industrial application. The extraction processes have been focused on the development of new strategies that guarantee high recovery rates with maximum activity (Nadar et al., 2017). The residues of these two fr
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The discoidin domain receptors DDR and DDR
2020-12-18
The discoidin domain receptors, DDR1 and DDR2, are receptor tyrosine kinases that are activated by different types of collagen (Shrivastava et al., 1997, Vogel et al., 1997). Both receptors interact with a number of fibrillar collagens, and DDR1, but not DDR2, is also activated by the network-formin
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In accordance with its original discovery EBI may play
2020-12-18
In accordance with its original discovery, EBI2 may play its major role in response to viral infections or in a pathological context such as in autoimmunity. Although we found a significant delay of onset in the Th17 transfer EAE model, active EAE was unchanged in absence of EBI2. At the moment, we
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To analyze EBI expression and its function in T cells
2020-12-18
To analyze EBI2 expression and its function in T cells in vivo, we created an EGFP reporter/knockout mouse strain, termed EBI2EGFP. This mouse strain in heterozygous configuration allows for a systematic analysis of the expression of EBI2 in distinct cell types in steady-state and under inflammatory
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br Conclusion br Introduction br CRL E ligases in
2020-12-18
Conclusion Introduction CRL4 E3 ligases in tumorigenesis Small molecule-based PROTACs PROTAC: Major biological impacts Acknowledgements The authors sincerely apologize to all those colleagues whose important work was not cited in this paper owing to space limitations. They thank th
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Subgroup analysis showed that patients
2020-12-18
Subgroup analysis showed that patients with relatively lower CrCl levels (>50–80 mL/min) were more likely to initiate treatment on a lower dose (17% for all DPP-4 inhibitors; 22% excluding linagliptin). Nevertheless, even in patients with higher CrCl value (>80–120 mL/min and >120 mL/min), at least
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br Conclusion The present work describes the synthesis of na
2020-12-18
Conclusion The present work describes the synthesis of 18 naphthoquinonolyl-1,2,3-triazole compounds based on natural product modification with antiplasmodial activity. Lapachol derivatives disclosed higher activity than the natural product. Six of these final modified lapachol 1,2,3-triazole com
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QSAR based on the D structures of
2020-12-18
QSAR based on the 3D structures of ligands plays an important role in the ligand-based drug discovery and design [12]. Comparative molecular field analysis, CoMFA [11], and comparative molecular similarity index analysis, CoMSIA [12] are among the most popular QSAR models. They focus on changes in 3
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Rosiglitazone HCl br Acknowledgements This work was supporte
2020-12-18
Acknowledgements This work was supported by grants from Agence Nationale de la Recherche (ANR CAPHE) and from Ligue contre le Cancer. We acknowledge the continuous support of CNRS and the University of Strasbourg. We thank the technical assistance of the “Plateforme de Chimie Intégrative de Stras
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A phenylacetic acid derivative discovered in a
2020-12-17
A phenylacetic cdk9 inhibitor mg derivative (), discovered in a high throughput screen for CRTH2, inhibited the binding of H-PGD to CRTH2 receptors on 293 cells with an IC of 0.010μM, and inhibited the binding of H-PGD to DP receptors with an IC of only 8.3μM (). Compound also inhibited CRTH2 med
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It is important to note that CRF may be
2020-12-17
It is important to note that CRF1 may be activated during acute stress and early phases of anxiety disorders (Coric et al., 2010, Ising et al., 2007), as well the administration of Astressin 2B into the lateral septum did not have an effect on anxiety-like behavior in low-stress conditions but had a
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br Atypical collagen glycosylation The disaccharide Glc Gal
2020-12-17
Atypical collagen glycosylation The disaccharide Glc(α1-2)Gal(β1-O) decorating collagens is strongly conserved across the animal kingdom, yet for every rule, nature provides exceptions. The deep-sea worm Riftia pachyptila of the phylum Annelida represents an intriguing exception. R. pachyptila is
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