Identification of Small Molecule Inhibitors of Pre - mRNA
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چکیده
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The Biflavonoid Isoginkgetin Is a General Inhibitor of Pre-mRNA Splicing*S⃞
Membrane-permeable compounds that reversibly inhibit a particular step in gene expression are highly useful tools for cell biological and biochemical/structural studies. In comparison with other gene expression steps where multiple small molecule effectors are available, very few compounds have been described that act as general inhibitors of pre-mRNA splicing. Here we report construction and v...
متن کاملIdentification of Small Molecule Inhibitors of Pre-mRNA Splicing*
Eukaryotic pre-mRNA splicing is an essential step in gene expression for all genes that contain introns. In contrast to transcription and translation, few well characterized chemical inhibitors are available with which to dissect the splicing process, particularly in cells. Therefore, the identification of specific small molecules that either inhibit or modify pre-mRNA splicing would be valuabl...
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Small molecule inhibitors of pre-mRNA splicing are important tools for identifying new spliceosome assembly intermediates, allowing a finer dissection of spliceosome dynamics and function. Here, we identified a small molecule that inhibits human pre-mRNA splicing at an intermediate stage during conversion of pre-catalytic spliceosomal B complexes into activated Bact complexes. Characterization ...
متن کاملIdentification of small molecule inhibitors of the Lin28-mediated blockage of pre-let-7g processing† †Electronic supplementary information (ESI) available: Additional control binding experiments, IC50 determining binding experiments, chemical structures and control Dicer processing experiments. See DOI: 10.1039/c6ob01945e Click here for additional data file.
The protein Lin28 and microRNA let-7 play critical roles in mammalian development and human disease. Lin28 inhibits let-7 biogenesis through direct interaction with let-7 precursors (pre-let-7). Accumulating evidence in vitro and in vivo suggests this interaction plays a dominant role in embryonic stem cell self-renewal and tumorigenesis. Thus the Lin28-let-7 interaction might be an attractive ...
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