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The N6-methyladenosine (m6A)-forming enzyme METTL3 controls myeloid differentiation of normal and leukemia cells
TLDR
It is shown that shRNA-mediated depletion of the m6A-forming enzyme METTL3 in human hematopoietic stem/progenitor cells (HSPCs) promotes cell differentiation, coupled with reduced cell proliferation, and this results provide a rationale for the therapeutic targeting of MET TL3 in myeloid leukemia.
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Transformation of the intestinal epithelium by the MSI2 RNA binding protein
The MSI2 RNA binding protein is a potent oncogene playing key roles in hematopoietic stem cell homeostasis and malignant hematopoiesis. Here we demonstrate that MSI2 is expressed in the intestinal…
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Transport of Lamivudine [(-)-β-l-2′,3′-Dideoxy-3′-thiacytidine] and High-Affinity Interaction of Nucleoside Reverse Transcriptase Inhibitors with Human Organic Cation Transporters 1, 2, and 3
TLDR
Data reveal that NRTIs experience a high-affinity interaction with hOCTs, suggesting a putative role for these drugs as modulators of hO CT activity, and 3TC is a novel substrate for hOcts and the inhibition of its uptake at low concentrations of ABC and AZT could have implications for the pharmacokinetics of 3TC.
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The Msi Family of RNA-Binding Proteins Function Redundantly as Intestinal Oncoproteins.
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PI3K inhibition results in enhanced estrogen receptor function and dependence in hormone receptor–positive breast cancer
TLDR
It is proposed that increased ER transcriptional activity may be a reactive mechanism that limits the activity of PI3K inhibitors and that combinedPI3K and ER inhibition is a rational approach to target these tumors.
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Expression and Functionality of Anti-Human Immunodeficiency Virus and Anticancer Drug Uptake Transporters in Immune Cells
TLDR
In immune cells, hOCTs showed a more heterogeneous expression profile and a lower activity than human nucleoside transporters (hNTs), although up-regulation of hO CTs also occurred upon lymphocyte activation, and overall, the expression and activity of most of the studied transporter emphasize their relevance in relation to anti-HIV and anticancer therapies.
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Drug uptake transporters in antiretroviral therapy.
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Functional screen of MSI2 interactors identifies an essential role for SYNCRIP in myeloid leukemia stem cells
TLDR
SYNCRIP is identified as a new RBP that controls the myeloid leukemia stem cell program and it is proposed that targeting these RBP complexes might provide a novel therapeutic strategy in leukemia.
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Peptidomimetic blockade of MYB in acute myeloid leukemia
TLDR
A peptidomimetic inhibitor is developed that prevents the interaction of the trans-activation domain of MYB with the KIX domain of CBP/P300 and inhibits leukaemia growth.
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A 1536-well fluorescence polarization assay to screen for modulators of the MUSASHI family of RNA-binding proteins.
TLDR
An in vitro strategy to identify MSI specific inhibitors using an FP HTS platform, which will facilitate novel drug discovery for this class of RBPs is developed.
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