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br Introduction Breast cancer is the most
2024-09-29

Introduction Breast cancer is the most frequently occurring cancer in women, and despite the development of new therapies there has been little decline in the mortality rate over the past decade (Siegel et al., 2015). This is partly due to the genetic diversity of breast cancers, such that there
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ALK fusion positive NSCLC is clinically actionable because
2024-09-29

ALK fusion-positive NSCLC is clinically actionable because it can be targeted by several FDA-approved drugs, including the first generation TKI crizotinib, which is a dual inhibitor to MET and ALK [15], and the second generation inhibitors, alectinib and ceritinib, both of which are highly-selective
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The inflammatory cytokine IL is an additional factor
2024-09-29

The inflammatory cytokine IL-6 is an additional factor that has been hypothesized to contribute to epinephrine-mediated repression of drug detoxifying proteins such as CYP3A4 (Aninat et al., 2008). Indeed, this CYP is well-known to be repressed by IL-6 (Dickmann et al., 2011) and epinephrine has pre
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br Discussion Mycobacterium tuberculosis infection is a main
2024-09-29

Discussion Mycobacterium tuberculosis infection is a main threat to mankind, with one third of the world population being infected. [9] Over nine million new cases of tuberculosis and two million deaths from this disease occur yearly worldwide. [10] The rising incidence of tuberculosis over the l
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br Clinical realities br Commentary on uses of
2024-09-29

Clinical realities Commentary on uses of selective 17,20 lyase inhibitors If continued monitoring of these same parameters along with tracking of circulating ACTH in human trials confirms these new drugs are the long sought after 17,20 lyase inhibitors, then we may for the first time be able t
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Imatinib is a well known anticancer drug used in
2024-09-28

Imatinib is a well-known anticancer drug used in Chronic Myeloid Leukemia (CML) against the altered expression/activity of tyrosine kinase resulting from the fusion of BCR-ABL in leukemic blasts. It has been demonstrated that Imatinib can induce autophagy in BCR-ABL expressing UK 356618 (K562 cell l
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Screening a selection of analogues from this library against
2024-09-28

Screening a selection of analogues from this library against the panel of 26 kinases (16, 22, and 24 were screened at 30 μM due to poor solubility; 17 tested at 100 μM) generally demonstrated an increase in activity compared to sodium channel 3 (Fig. 3, Fig. 6). The benzamide analogue 16 demonstrat
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Fencilli et al reported derivatives of
2024-09-28

Fencilli et al. reported derivatives of PHA-680626 (15) which demonstrated strong anti-proliferative activity against large group of leukaemia cell lines including IM-resistant BAF3 cells expressing mutants like T315I, M351T and E255K. Decrease in Histone H3 phosphorylation led to induction of endo-
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With regard to the first question subcellular fractionation
2024-09-28

With regard to the first question, subcellular fractionation studies revealed that BDK and PPM1K are clearly detectable in both the mitochondrial and cytosolic subcellular fractions, thus making it possible for these enzymes to interact with both the BCKDH and ACL substrates. The preferential presen
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Secondly leptin has been shown to enhance aromatase
2024-09-28

Secondly, leptin has been shown to enhance aromatase mRNA expression, aromatase content and its enzymatic activity in epithelial breast cancer mecamylamine by inducing promoters II and I.3 via an enhanced binding of transcription activator protein 1 (AP-1) complex to specific DNA sites in the promo
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br Material and methods br Results br Discussion
2024-09-28

Material and methods Results Discussion Didox was originally created asa cytostatic drug to inhibit cancer cell proliferation by antagonizing RNR [11]. When used to target highly proliferative cells, Didox has extensive activity in vitro and in vivo. It has also been employed in clinical st
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The regulation of gene expression by glucocorticoids can be
2024-09-28

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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Although the gene that encodes DHFR has been
2024-09-28

Although the gene that encodes DHFR has been strongly conserved during evolution, subtle differences in the active sites of bacterial, human and parasite N-Nonyldeoxynojirimycin have been exploited to develop DHFR inhibitors specific to particular pathogens 1, 3. For example, pyrimethamine and cyclo
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br Experimental procedures br Results br Discussion Our biop
2024-09-28

Experimental procedures Results Discussion Our biophysical and cellular analyses of mutant Aβ1–42 peptides support a role of the N-terminus of Aβ in peptide aggregation and toxicity. We demonstrate that double mutations constructed to humanize the rodent Aβ1–42 sequence result in a signific
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The decreased AR mediated response has been attributed to
2024-09-28

The decreased βAR-mediated response has been attributed to different mechanisms, including an attenuation of PKA activation, an impaired generation of cyclic AMP, a reduced receptor density, and a less efficient coupling to adenylyl-cyclase [10]. However, currently there is no single molecular or ce
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