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The in vitro cytotoxicity of the prodrugs was assessed in
2021-03-09
The in vitro cytotoxicity of the prodrugs was assessed in the LS174T human colon cell line (). The results were found to reflect the stability of the prodrugs, with the unstable urea compounds ( and ) giving relatively poor cytotoxicity differentials between prodrugs and parents (i.e., approximately
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Many authors have described the existence of correlation
2021-03-09
Many authors have described the existence of correlation between viability and moisture content and therefore, water availability. Sabuquillo et al. (2010) demonstrated that only Penicillium oxalicum conidial formulations whose initial moisture contents ranged between 5 and 14% retained their viabil
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Based on the above we hypothesized that a PROTAC
2021-03-09
Based on the above, we hypothesized that a PROTAC strategy would be effective to induce CK2 protein degradation. Herein reported is an approach for the preparation of novel PROTACs via “click reaction” for degradation of CK2 protein (Fig. 2). Importantly, “click reaction” is a very facile, selective
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Phosphatase Inhibitor Cocktail 1 (100X in DMSO) We hypothesi
2021-03-09
We hypothesize that both IGF-1-dependent kinase activation and locally synthesized neuroestrogens interactively regulate estrogen receptor activity in neuronal Phosphatase Inhibitor Cocktail 1 (100X in DMSO) in the absence of exogenously applied estradiol. The Neuro-2A cell line was chosen as the m
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Introduction Proteins play an important role
2021-03-09
Introduction Proteins play an important role in cellular functions; however, being and remaining properly folded is necessary for their function. Understanding the stability of the protein is necessary to investigate the folding of proteins, as well as their conformation, functions and interactions
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br Prospect of DDR antagonist DDR a receptor of tyrosine
2021-03-08
Prospect of DDR2 antagonist DDR2, a receptor of tyrosine kinase has been found now to be reported to play a significant role in onset of osteoarthritis at the early stage of diseases progression. The DDR2 are the receptor for extracellular collagen and activated upon the binding of collagen resul
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br Acknowledgements This work was supported by grants
2021-03-08
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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Introduction Tumor necrosis factor TNF is a pro
2021-03-08
Introduction Tumor necrosis factor (TNF) is a pro-inflammatory mediator with the capacity to induce apoptosis (Benderska et al., 2012). Recent reports have shown that TNF might trigger cell death, at least in part, by directly affecting the reorganization of the 1,4-DPCA mg cytoskeleton (Campos et
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Finally unilateral microinjection of CP Astressin B CP CRF
2021-03-08
Finally, unilateral microinjection of CP-376395, Astressin 2B, CP-376395 + CRF or ASTR 2B + CRF into the BLA (Fig. 3A) or CeA (Fig. 3B) did not significantly alter spontaneous motor activity in the open field test (F4,24 = 0.148, P > 0.05; F4,29 = 0.290, P > 0.05 in the BLA and CeA, respectively, AN
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br Materials and methods br Results br Discussion
2021-03-08
Materials and methods Results Discussion Intra-BNST injections of NOC-9 (at all doses) were able to produce freezing and anxiogenic-like effects. Freezing was observed immediately after the NO donor injection and lasted about 2–3min (data not shown). When exposed to the EPM 5min after intra
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Data from immunohistochemical detection of CIC revealed that
2021-03-08
Data from immunohistochemical detection of CIC-3 revealed that the immunostaining of CIC-3 can be present both in hepatocarcinoma and its matched normal controls though; CIC-3 was, on the whole, significantly elevated in hepatocarcinoma relative to its paired normal control. In consideration of the
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The presence of a vicious cycle established between tumor
2021-03-08
The presence of a “vicious cycle” established between tumor proliferation and paratumor osteolysis plays a crucial role in the development of primary bone tumors [53]. Cancer cells produce soluble factors that activate directly or indirectly via osteoblasts, osteoclast differentiation and maturation
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br Materials and methods br Results br Discussion The
2021-03-08
Materials and methods Results Discussion The oestrogen agonist properties and androgen antagonist activities of parabens have been well documented by a variety of in vitro and in vivo assay systems over the past decade (Chen et al., 2007, Darbre and Harvey, 2008, Golden et al., 2005). To th
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The Eph ephrin signaling system has the ability to elicit
2021-03-08
The Eph–ephrin signaling system has the ability to elicit bidirectional signaling, classical forward signaling by both Eph receptor via its intrinsic tyrosine kinase activity and reverse signaling by the transmembrane ephrin ligand via its cytoplasmic domain [38], [39]. Thus when EphB4 binds with ep
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As a co factor CIITA lacks the ability to recognize
2021-03-08
As a co-factor, CIITA lacks the ability to recognize and directly bind to specific DNA elements to regulate transcription; instead, it relies on interaction with sequence-specific transcription factors (TFs) to be recruited to the chromatin. Therefore, the observation that CIITA binds to a specific
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