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Of the acidic hydroxyazoles involved hydroxypyrazole had
2020-07-25
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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The work described by Dong Groves and
2020-07-24
The work described by Dong, Groves, and co-workers (11) tested the hypothesis that neural stem cell development is sensitive to the clustering and mechanical state of the EphB4:ephrin-B2 receptor-ligand complex. They show that the quality of ephrin-B2-ligand signaling depends on its biophysical stat
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br Conclusions br Acknowledgements Implantable
2020-07-24
Conclusions Acknowledgements Implantable Microsystems for Personalised Anti-Cancer Therapy is a EPSRC (Engineering and Physical Sciences Research Council, UK) funded grant (Ref. EP/K034510/1) Introduction Flemingia philippinensis, belonging to the legume family, is a polyphenol rich plant
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Imatinib STI is a first line tyrosine kinase inhibitor TKI
2020-07-24
Imatinib (STI-571) is a first-line tyrosine kinase inhibitor (TKI) targeted at breakpoint cluster region-Abelson kinase (ABL) for the treatment of chronic myeloid leukemia (CML) [26]. As a type II inhibitor, imatinib achieves significant selectivity by binding to an inactive DFG-out conformation (DF
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br Cytokine profile in MPN Results from experimental investi
2020-07-24
Cytokine profile in MPN: Results from experimental investigation Cytokines are small molecules constituted by proteins or glycoproteins, which regulate the immune cell function and the immune system. They are secreted mainly by immune Talabostat mesylate but also by other cells such as epithelia
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Our module is designed to allow
2020-07-24
Our module is designed to allow in-process measurement of [C]-tracer molar activity (MA, GBq/μmol at EOB) using a d luciferin detector with a UV detector at the outlet of the HPLC-portion of the system. In the HPLC chromatogram, peak analysis of the chromatographic data utilized PeakSimple software
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Introduction Double strand break DSB is the
2020-07-23
Introduction Double strand break (DSB) is the most deleterious damage that threats DNA integrity. This frequent damage arises from environmental stress like UV, chemical agents or ionizing radiations (IRs). Although environmental stress does not lead directly to DSB, it produces ganciclovir damage
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Cell migration and invasion are central processes
2020-07-23
Cell migration and invasion are central processes in the development and metastasis of cancer. The regulation of cell migration by DDR1 has been reported in many types of cancer cell lines; however, conflicting results have been reported regarding the inhibitory as well as promotive effects of DDR1
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br Results and discussion br Conclusion In this
2020-07-23
Results and discussion Conclusion In this investigation, pharmacophore models of CK1 inhibitors were developed using a pharmacophore modeling protocol proposed by us. The optimal pharmacophore hypothesis, Hypo2, was adopted to retrieve potential CK1 inhibitors from the commercial chemical data
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In normal chow fed mice EP deficiency also decreased
2020-07-23
In normal chow fed mice, EP4 deficiency also decreased the expression of CYP8B1, the downstream target of CYP7A1. Similarly, knockdown of EP4 with small interfering RNA reduced the expression of CYP8B1 in HepG2 cells. Therefore, it was anticipated that there would be an increased expression of CYP8B
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br Materials and methods br Results br Discussion Anti
2020-07-23
Materials and methods Results Discussion Anti-EGFR therapy for epithelial carcinomas has important clinical significance, but widespread intrinsic or acquired resistance seriously affects efficacy. Mutation and heterodimerization of EGFR are the two main causes of resistance to anti-EGFR th
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br ET Antagonist for the
2020-07-22
ET Antagonist for the Future: Macitentan and Atresentan Macitentan is an insurmountable antagonist, resulting from structure-activity studies to improve the efficacy and tolerability of bosentan, and gained approval in the United States in 2013 for the treatment of PAH. Actelion describes the com
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Although enantioselective accumulation of metalaxyl
2020-07-22
Although enantioselective accumulation of metalaxyl in organisms is an integrated outcome of bio-process including absorption, transportation, and transformation, it is observed in our study that catalysis of CYP450 may lead to the enantioselective accumulation of metalaxyl. However, the mechanisms
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The two most important biological
2020-07-22
The two most important biological machineries controlling proteostasis, PQC, and degradation are autophagy and the ubiquitin-proteasome system (UPS) (). Autophagy is a lysosome-dependent, tightly regulated catabolic process that degrades unwanted cell organelles and cytoplasmic constituents in lysos
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The relatively less well studied encodes the E type
2020-07-22
The relatively less well-studied encodes the E2 type SUMO-conjugating enzyme. In plants, the SCE family members play roles in abiotic stress responses. An E2 enzyme, SaSce9, from plays roles in salinity and drought stress responses (). Furthermore, SCE can respond to heat stress in rice (). Howeve
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