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To determine the time course of ZD
2021-06-16
To determine the time course of ZD2767P+CPG2 DNA–DNA interstrand cross-link formation, HT29 and LS174T colorectal tumour Mesoridazine Besylate were exposed to the drug for 10, 30 or 60 min. The levels of DNA interstrand cross-links in HT29 or LS174T cells did not increase with exposure time, sugges
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apiii australia br Results and discussion br Conclusion This
2021-06-16
Results and discussion Conclusion This study describes the development of a highly sensitive on-sorbent derivatisation technique, using the novel high-surface area CMV devices, to sample methamphetamine vapour. Previous methods for air sampling for methamphetamine such as sampling cassettes ha
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br Acknowledgements Professor Olli A J
2021-06-15
Acknowledgements Professor Olli A. Jänne is warmly thanked for support and for providing excellent research facilities. Professor Patrik Finne is acknowledged for his help with statistical analyses. Drs Ronald Evans, Vincent Giguère, Jorma Palvimo, Malcolm Parker, and Anastasia Kralli are acknowl
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Introduction Glucose is the major
2021-06-15
Introduction Glucose is the major carbon source in most organisms. Cancer Clindamycin HCl receptor in particular require a steady source of energy to maintain growth and proliferation, and preferentially use glycolysis for their energy supply even under aerobic conditions. Glucose uptake in mammal
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br Clinical potential of ET receptor biased ligands Is
2021-06-15
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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SIRT is a representative member of Sirtuins
2021-06-15
SIRT1 is a representative member of Sirtuins, which is a family of highly conserved NAD+-dependent class III histone deacetylases. SIRT1 deacetylates plentiful nonhistone protein substrates [Atgs, Foxo1, Foxo3, PGC-1α, NF-kB, E2F1 and p53] (Conrad et al., 2016; Gu et al., 2016; Tu et al., 2018) to p
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Further indirect evidence supporting an important role of DP
2021-06-15
Further indirect evidence supporting an important role of DPP-4 in the modulating the actions of both incretins comes from the observations that analogues of GLP-1 and GIP, modified to be resistant to DPP-4 cleavage, were subsequently shown to have greater metabolic stability in vivo which was assoc
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In light of the overall loss of activity and selectivity
2021-06-15
In light of the overall loss of activity and selectivity observed with this series of arylchromenone-4-ones bearing small -alkoxy substituents, we were pleased to identify a potent and relatively selective inhibitor , exhibiting IC values of 0.008μM and 0.07μM for DNA-PK and PI3Kα, respectively. The
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Long stretches of ssDNA have also been
2021-06-15
Long stretches of ssDNA have also been observed in rad53-1 mutant Cathepsin K Activity Fluorometric Assay Kit under replication stress using EM images (Sogo et al., 2002). Deletion of EXO1, a 5′-to-3′ exonuclease, can suppress the generation of ssDNA detected in rad53-1 mutant cells (Cotta-Ramusin
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Collagen compaction and alignment are generated by
2021-06-15
Collagen compaction and alignment are generated by cell-mediated contractile forces (Stopak and Harris, 1982). The transmission of actomyosin forces to collagen has been mainly attributed to integrins and the activation of the Rho-ROCK pathway (Clark et al., 2007, Kural and Billiar, 2013, Provenzano
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We have reported previously that aminoacrylate
2021-06-15
We have reported previously that β-aminoacrylate derivatives of the general structure () are inhibitors of DHODH. In particular, tricyclic derivatives and displayed sub-micromolar IC values against DHODH, and in the case of there was a 1000-fold greater potency compared to the human enzyme (DHOD
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Acknowledgment This work was supported by
2021-06-15
Acknowledgment This work was supported by the Swedish Research Council, the Knut and Alice Wallenberg Foundation, the Göran Gustafsson Foundation, the Swedish Pain Relief Foundation, the Torsten Söderbergs Stiftelse, the Swedish Children's Cancer Foundation, and the Swedish Cancer Society. The h
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In the present study we used a new
2021-06-15
In the present study, we used a new luminescent method to measure CYP activity with Luciferin-ME as a substrate which is used for wide ranges of mammalian CYPs, including CYP1A2, CYP2C8, CYP2C9, CYP2J2, CYP4A11, and CYP4F3B. As a result, no significant modulations of CYP activities in B[a]P exposure
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anderson kpt The binding pattern of was analysed by flexible
2021-06-11
The binding pattern of 1 was analysed by flexible molecular docking. The anderson kpt inserted into the narrow ATP binding site of CK2 (Fig. 2). As shown the aliphatic chain of 1 was located at the edge of the pocket and established van der Waals interactions with the side chains residues of Ile95,
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br Introduction Estrogens play an important
2021-06-11
Introduction Estrogens play an important role in the NKH 477 (Arevalo et al., 2015). During several decades, estrogen withdrawal in women has been associated with cognitive impairment, increased Alzheimer's disease (AD) risk (Pike, 2017) and with psychiatric disorders such as schizophrenia (Kulk
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