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Licarbazepine During the course of our ACK inhibitor program
2023-12-05

During the course of our ACK1 inhibitor program, a high-throughput screening (HTS) campaign of our internal sample collection was conducted. A series of -aryl pyrimidine-5-carboxamides of the general structure () was identified. Earlier studies of the structure–activity relationship (SAR) of ident
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For the NSCLC patients with EGFR activating mutations EGFR T
2023-12-05

For the NSCLC patients with EGFR-activating mutations, EGFR-TKIs (gefitinib and erlotinib) are effective clinical therapies [21], [22]. However, approximately 10% of patients harboring EGFR-sensitizing mutations exhibit intrinsic resistance, and up to 40% do not attain a major response to treatment
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br Aurora kinases br Wnt signaling pathway The signal
2023-12-05

Aurora kinases Wnt signaling pathway The signal transduction pathway of Wnt/β-catenin signaling pathway plays an important role in embryogenesis to control cell differentiation and tumorigenesis [39]. A recent report indicates that 90% of colorectal cancer occur due to the activation of the Wn
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AP was originally described as a heterodimer of
2023-12-04

AP-1 was originally described as a heterodimer of the bZIP proteins c-Jun and c-Fos. The experiments described here showed that stimulation of TRPV1 channels induced the expression of both of these classical constituents of AP-1. The essential role of both proteins was analyzed in a series of experi
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Necrostatin 2 The regulation of gene expression by
2023-12-04

The regulation of gene expression by glucocorticoids can be mediated either by the canonical mechanism that involves the interaction of the glucocorticoid receptor (GR), a transcription factor activated by the hormone, with glucocorticoid response element (Ye et al., 2007), or by the non-canonical m
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br Concluding remarks and future perspectives While the
2023-12-04

Concluding remarks and future perspectives While the rational engineering of protein-based switches has yet to be fully developed, emerging empirical rules facilitate the construction of tailor-engineered guanylate cyclase with custom input and output parameters. Both in the context of molecula
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Introduction Aldose reductase ALR is the first
2023-12-04

Introduction Aldose reductase (ALR2) is the first enzyme of the polyol pathway that catalyzes the reduction of glucose to sorbitol utilizing NADPH as a cofactor. The intracellular accumulation of sorbitol, due to increased aldose reductase activity at high blood glucose levels, such as those occurr
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Involvement of Adiponectin in the regulation of imatinib
2023-12-04

Involvement of Adiponectin in the regulation of imatinib resistance in human CML cells has not been hitherto examined. Therefore, in this study, we first established imatinib-resistant K562 CML cells, and then evaluated the effect of Adiponectin in reversing imatinib resistance. The data presented h
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hydroxydopamine OHDA is a selective catecholaminergic neurot
2023-12-04

6-hydroxydopamine (6-OHDA) is a selective catecholaminergic neurotoxin mainly used to generate lesions in the nigrostriatal pathway in rats (Ungerstedt, 1968). The most common use of 6-OHDA is via unilateral injection into the rat medial forebrain bundle (MFB). DA depletion, nigral DA cell loss, and
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br Experimental section br Results and discussion br
2023-12-04

Experimental section Results and discussion Conclusions We present a simple, sensitive and selective assay of ADA activity and its inhibitor using the enzyme catalyzed reaction and the different interaction intensity of dye-labeled AD aptamer, aptamer/AD complex with GO. The as-proposed met
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Our published data showed that in mouse
2023-12-04

Our published data showed that, in mouse heart, the protein level of WDR1 was highest during the embryonic stage, but became progressively decreased to a constant level from birth to adulthood (Yuan et al., 2014), indicating an important role of WDR1 in embryonic heart development. However, function
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MicroRNA miRNA is an abundant group of
2023-12-04

MicroRNA (miRNA) is an abundant group of small (22-nucleotide) noncoding RNA molecules that directly binds with 3′ untranslated region (UTR) of target messenger RNAs (mRNAs) to regulate gene expression, playing an important role in variety of biological processes including cell proliferation, apopt
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In an attempt to complete
2023-12-04

In an attempt to complete the overview of resistance mechanisms in Spanish codling moth populations, the aims of the present work were to assess the actual occurrence of AChE and kdr mutations in codling moth field populations from different pome fruit-growing areas of Spain, concurrently with the f
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The scattering operators associated to are
2023-12-04

The scattering operators associated to are defined as follows: for any and , , , there exists a unique solution to the following equation such that Then the scattering operator is defined by Here is an elliptic pseudodifferential operator of order , which is conformally covariant on the boundary.
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Macrophage polarization is linked to activation of the
2023-12-04

Macrophage polarization is linked to activation of the ligand-dependent transcription factor PPARγ. Recently, Odegaard et al. demonstrated with a macrophage-specific deletion of PPARγ in mice that alternative macrophage activation is impaired [14]. We provided evidence that contact to apoptotic phen
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