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The estrogenic activity of steroids with a C methyl group
2021-08-17
The estrogenic activity of steroids with a C19 methyl group may provide a selective advantage in estrogen physiology that is not provided by E2. In this regard, 5α-androstanediol has been proposed to be a second physiological estrogen in fetal mouse Calpeptin based on the timing of ERβ synthesis in
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br Genomic and non genomic signaling
2021-08-17
Genomic and non-genomic signaling crosstalk As exemplified in the previous sections, it is evident that the mechanisms of action of estrogen in the various cell targets represent a combination of complex multifactorial processes. Besides the independent genomic and non-genomic pathways described
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NF B is a family of protein mediators
2021-08-17
NF-κB is a family of protein mediators that regulate various innate and adaptive immune responses [29,30]. The NF-κB family consists of the following five proteins: c-Rel (Rel); p65 (RelA); RelB; p50(NF-κB1); and p52(NF-κB2). It has been confirmed that NF-κB is activated by TNF family cytokines, suc
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The optimization of the lead compound was initiated and the
2021-08-17
The optimization of the lead compound () was initiated and the initial key SAR and the results of the structural modifications of lead compound are summarized in . Replacement of the carboxylic sars-cov moiety with other functional groups led to loss of functional activity against EP4 receptor. Alth
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br Iterative design approach overview An iterative design st
2021-08-17
Iterative design approach overview An iterative design strategy is used to identify a peptidase-resistant reporter that acts as an efficient substrate for kinases in cell lysates as well as intact cells (Fig. 1). In this process, small-scale, rationally designed libraries are used to screen pepti
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br Protein protein interactions of LEI L DNase II and
2021-08-17
Protein-protein interactions of LEI/L-DNase II and the control of cell death Evolutionary tips The serpin inhibitory mechanism is extremely well adapted to evolutionary changes because a single amino c-Myc Peptide substitution in the RSL can led to the inhibition of a totally different proteas
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Among the Ub interactions observed
2021-08-17
Among the ~Ub interactions observed in the HOIP structure is one that involves a RING2 domain (from the non-cognate HOIP) [47]. A similar binding interaction was defined between HHARI RING2 and the hydrophobic patch on Ub by NMR [54]. HHARI RING2 mutations that ablate the interaction inhibit formati
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hnRNP E functions in a number of mRNA
2021-08-17
hnRNP E1 functions in a number of mRNA regulatory processes including transcription [74], [75], splicing [7], [74], [76], [77] and translation [6], [8], [69], [78], interacting with RNAs through CU rich regions such as the differentiation control element (DICE) and the TGFβ activated translation (BA
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br Authors contribution br Disclosure statement br
2021-08-17
Authors contribution Disclosure statement Acknowledgements This study has received funding from the Italian Ministry of University and Research (PRIN 2015, grant number 2015373Z39_008) and from the Innovative Medicines Initiative 2 Joint Undertaking under grant agreement No 115797 (INNODIA)
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Several reports have exploited the application
2021-08-16
Several reports , , , , have exploited the application of HRM for detecting differentially methylated DNA. Even though DNA methylation analysis by HRM cannot determine the methylation status of individual CpGs, it does provide a robust and inexpensive method to differentiate DNA based on the overal
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br Anti inflammatory effects of
2021-08-16
Anti-inflammatory effects of MTX In addition to cytotoxic and cytostatic effects, the anti-inflammatory activity of MTX was also described by several studies. Inhibition of ATIC by MTX has been found to result in the accumulation of 5-aminoimidazole-4-carboxamide-1-β-d-ribofuranosyl 5′-monophosph
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Leupeptin These data raised from human tissues suggested
2021-08-16
These data raised from human tissues suggested a potential link between TGF-β1 signaling and linear invadosome machinery that may explain TGF-β involvement in HCC progression and invasion. Using HCC cultured cells, we confirmed that TGF-β1 stimulation increases the production and secretion of collag
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A range of therapies exists for
2021-08-16
A range of therapies exists for the treatment of inflammation-driven diseases, which can be summarized as non-steroidal anti-inflammatory drugs (NSAIDs), corticoids and steroidal-related drugs (Ward et al., 2008). Despite of these notable successes, there are still major unmet medical needs in the t
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br Preparation of Recombinant Proteins br Activity Assays Th
2021-08-16
Preparation of Recombinant Proteins Activity Assays The following solvents are used in the procedures described in this section: Data Analysis Aryl radical rearrangements typically result in a large number of products being generated by Bmp7. Approaches combining mass spectrometry and NMR
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The X ray crystal structure of palbociclib bound
2021-08-16
The X-ray crystal structure of palbociclib bound to CDK6 without a DMOG (PDB ID: 5L2I) is very similar to that of the CDK6-cyclin V structure (Fig. 7B). However, the drug binds to the αCout conformation of monomeric CDK6 while it binds to the αCin conformation of the CDK6-cyclin V complex. It is li
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