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br Rationale and hypothesis To discover an allosteric inhibi
2021-08-12

Rationale and hypothesis To discover an allosteric inhibitor of EGFR, Jia et al. (2016) screened a library of 2.5 million compounds at 1 μM ATP concentration in opposition the purified EGFR L858R/T790M mutant enzyme. 1322 best hits were found from this round of screening. The pinnacle hits had be
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The thermal behavior of the UV sensitive nanocomposites was
2021-08-12

The thermal behavior of the UV-sensitive nanocomposites was investigated by DSC before and after irradiation in an extended temperature range (from −40 to 250 °C). Fig. 4a shows the thermograms of the non-irradiated GNP-DNA/PDMS nanocomposites in comparison with a neat PDMS sample. The filler-loaded
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br Materials and methods br Results
2021-08-12

Materials and methods Results Discussion GOS potently inhibited SRD5A1 in COS-1 cells (Fig. 4A) and rat Leydig cells (Fig. 4B), possibly attenuating testosterone activation into DHT. It has been reported that gossypol inhibited human SRD5A1 with IC50 of 7 × 10−6 M [28]. Interestingly, gossy
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The overall poor outcomes in
2021-08-12

The overall poor outcomes in ESCC are thought because of a combination of late diagnosis, aggressiveness of the disease, and a lack of effective treatment strategies for systemic disease. Several molecular pathways, such as epidermal growth factor receptor, vascular endothelial growth factor, and p5
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The authors gratefully acknowledge financial support from
2021-08-12

The authors gratefully acknowledge financial support from the State of São Paulo Research Foundation (FAPESP, Fundação de Amparo à Pesquisa do Estado de São Paulo), grants 2013/07600-3 and 2013/25658-9, and the National Council for Scientific and Technological Development (CNPq, Conselho Nacional de
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br Conclusions Taken together a distinct contrast is observe
2021-08-11

Conclusions Taken together, a distinct contrast is observed between ERK1/2 phosphorylation in hypothalamic and extra-hypothalamic sodium butyrate regions. The hypothalamus is the only brain region where ERK1/2 phosphorylation was increased 15minutes after the OF stressor. In SD rats CRFR1 expres
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Cancer has been linked to both genetic and epigenetic change
2021-08-11

Cancer has been linked to both genetic and epigenetic changes. Epigenetic modifications, mainly DNA methylation at CpG dinucleotides, affect the regulation of gene transcription without altering the gene's sequence. Short sequences rich in CpG dinucleotides (i.e., CpG islands) are often found in the
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Tanshinone I More importantly Santagata et al have suggested
2021-08-11

More importantly, Santagata et al. have suggested a new breast cancer subtyping method according to ER, androgen receptor (AR), and VDR with a higher prognostic value than the ordinarily used method based on ER, progesterone receptor (PR) and Her2 (Santagata et al., 2014). This implies that such com
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br Membrane receptor Indirect non
2021-08-11

Membrane receptor: Indirect non-genomic signaling As mentioned above, not all DL-Menthol responses fit the classical genomic model of steroid action. The observation of excessively fast estrogen-induced biological responses led to the development of the hypothesis that estrogen could be acting b
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PBMC derived macrophages not only express EBI but also
2021-08-11

PBMC-derived macrophages not only express EBI2 but also have the ability to respond to their natural agonist 7α,25-OHC by activating downstream signal transduction pathways. In line with previous findings, our data confirm that receptor stimulation induces calcium mobilization which can be blocked b
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Alpha SYN has no direct effect on
2021-08-11

Alpha-SYN has no direct effect on forskolin-induced CREB phosphorylation, but rather blocks the stimulation of CRE-mediated transcription in the nucleus. Previously we suggested that α-SYN can enter the nucleus and is present in both cytosolic and nuclear fractions without direct interaction between
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In the past few years DNA templated fluorescent
2021-08-11

In the past few years, DNA-templated fluorescent metal nanoparticles have been developed as ideal alternatives to organic dyes due to their facile synthetic process, outstanding optical properties, ultrafine size, and fine biological compatibility. Since the first successful demonstration of DNA-tem
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The ribosomal synthesis of D proteins is not
2021-08-11

The ribosomal synthesis of D-proteins is not currently feasible; the best effort undertaken so far was limited to the translational incorporation of two D-amino acids into the nascent protein chain by means of modified ribosomes (Dedkova et al., 2006). We therefore apply solid-phase peptide synthesi
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In anticipation of an approach based on modification of the
2021-08-11

In anticipation of an approach based on modification of the cyclohexylacetic ABT-737 subunit of 1 as a means of improving permeability, a set of analogs were prepared to map out the optimum display of the acidic functionality. Homologated acids 25 and 26 were found to be equipotent to 1, although t
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DDR distribution in healthy fibrotic and inflamed tissues
2021-08-11

DDR1 distribution in healthy, fibrotic and inflamed tissues Whereas we can easily mine publicly available databases to infer DDR1 expression profile in different tissues (as reported in Fig. 1), fine comprehension of DDR1 biology has been hampered by the absence of a commercially available specific
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