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The previously described endogenous patterns
2021-06-04

The previously described endogenous patterns of IGF-1-induced kinase signaling, and resulting interaction between MAPK and PI3K, differ across neuronal sub-types. In R28 retinal neuron-like cells, IGF-1 treatment elicits prolonged activation (at least 80 min) of both PI3K and MAPK (Kong et al., 2016
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Prenylation may turn a flavonoid from an agonist to an
2021-06-04

Prenylation may turn a flavonoid from an agonist to an antagonist and improve the selectivity to both ERs depending on the position of the substitution. C-8 prenylation appears to promote antagonism to a larger extent than C-6 in ERα due to steric hindrance against generation of agonistic conformati
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br Introduction Concrete is one of
2021-06-04

Introduction Concrete is one of the most commonly used materials in the construction industry and its raw material is available throughout the world. Concrete is derived from ordinary Portland cement and is used for the construction and development of infrastructures. Research shows that demand f
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Our previous high throughput screening HTS
2021-06-04

Our previous high-throughput screening (HTS) campaign using automated, robust, and sensitive fluorescence based dna-pk pathway assay [10], [11] led to the identification of several EPAC specific inhibitors (ESIs), and was subsequently followed by extensive hit-to-lead optimizations [20], [21], [22]
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br The synthesis of these antagonists relied heavily on
2021-06-04

The synthesis of these antagonists relied heavily on Stille and Suzuki coupling reactions. The preparation of the required building blocks is presented in . Reduction of ethyl 6-bromo-2-pyridinecarboxylate with diisobutylaluminum hydride in tetrahydrofuran followed by treatment with triisopropylsi
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Several effective strategies have been developed
2021-06-04

Several effective strategies have been developed to design activatable MR probes according to the Solomon, Bloembergen and Morgan (SBM) theory, including modulation of the number of inner-sphere water molecules (q), the rotational tumbling time (τ) and the residence lifetime of inner-sphere water mo
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br Competing interests br Acknowledgments This work was supp
2021-06-04

Competing interests Acknowledgments This work was supported by grants from Fujian Fujian Provincial Natural Science Foundation (2016J01612). Introduction Cancer is still one of the most serious diseases in the world. According to the World Health Organization (WHO), cancer is the second mo
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br Materials and Methods br Acknowledgements br Introduction
2021-06-04

Materials and Methods Acknowledgements Introduction Collagen fibrillogenesis, the assembly of collagen fibers, is a critical process in the development, maturation, and repair of mammalian tissue. Alterations in the structure and amount of deposited collagen fibers can greatly alter the int
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br Materials and methods br Results br Discussion The studie
2021-06-04

Materials and methods Results Discussion The studies reported here provide a more direct link between conformations of the glycine-rich region of DAPK and enzyme activity. As schematically illustrated in Fig. 3, the various conformations of DAPK with bound substrate or product can be consid
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An important strength of our study is the use
2021-06-04

An important strength of our study is the use of an elastic net regression model to select the variable and construct the model, which performed ideally in terms of both predictive accuracy and sparsity for the high-dimensional datasets [16]. As a result, the apparent predictive effect of multiple c
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Recently several Pt IV complexes as prodrugs
2021-06-03

Recently, several Pt(IV) complexes as prodrugs have been designed and studied to enhance anti-tumor efficacy of traditional Pt(II) drugs, improving their cellular uptake and blood-circulation time [26], [27], [28], [29]. Compared with their Pt(II) counterparts, six-coordinated Pt(IV) complexes with
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The use of recombinant ER and ER binding
2021-06-03

The use of recombinant ERα and ERβ binding assays offers a relatively inexpensive, rapid technique for screening compounds for potential direct Epidermal Growth Factor (EGF), human recombinant receptor receptor modulatory activity and understanding the mechanisms of existing herbal medicines. For b
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Tibolone is also efficacious on
2021-06-03

Tibolone is also efficacious on bone in elderly women and induces a clear reduction in bone turnover markers [50], [51]. Rymer et al. showed that, after 10 years of treatment with tibolone, the difference in bone mineral density compared with a placebo group was more than 12% for both lumbar spine a
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Telotristat PGE EP activation has been
2021-06-03

PGE2-EP4 activation has been found to attenuate the activation of microglia and to prevent lipid peroxidation and pro-inflammatory gene expression in a murine model of lipopolysaccharide (LPS)-induced Telotristat inflammation [15]. Moreover, PGE2/EP4 signaling has elicited a protective function in
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br Acknowledgments This work was supported by
2021-06-03

Acknowledgments This work was supported by Région Auvergne “Nouveau chercheur”. This study has been performed with the assistance of Christelle Damon-Soubeyrand for histology technical assistance using “Anipath” Platform (GReD) and Sandrine Plantade, Keredine Ouchen and Philippe Mazuel for animal
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