منابع مشابه
Small Molecule Inhibition of RISC Loading
Argonaute proteins are the core components of the microRNP/RISC. The biogenesis and function of microRNAs and endo- and exo- siRNAs are regulated by Ago2, an Argonaute protein with RNA binding and nuclease activities. Currently, there are no in vitro assays suitable for large-scale screening of microRNP/RISC loading modulators. We describe a novel in vitro assay that is based on fluorescence po...
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sequence-specific posttranscriptional regulators of gene expression, acting via RNA-induced silencing complexes (RISCs). They are termed small interfering RNAs (siRNAs) and microRNAs (miRNAs). Despite initial discovery from unrelated studies, these RNA classes are related in their biogenesis and assembly into RISC RNA–protein complexes, and are able to regulate gene transcripts negatively in di...
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Downlo ent evidence suggests that several deubiquitinases (DUB) are overexpressed or activated in tumor cells any contribute to the transformed phenotype. Agents with DUB inhibitory activity may therefore have eutic value. In this study, we describe the mechanism of action of WP1130, a small molecule derived compound with Janus-activated kinase 2 (JAK2) kinase inhibitory activity. WP1130 induce...
متن کاملIn vitro reconstitution of the human RISC-loading complex.
Targeted gene silencing by RNAi requires the RNA-induced silencing complex (RISC), whose core component is the protein Argonaute (Ago) bound to a microRNA (miRNA) or an siRNA. In humans, Ago2 is loaded with miRNAs by the action of a specialized assembly called the RISC-loading complex (RLC), comprising the proteins Ago2, Dicer, and TRBP. Here we show that the human RLC assembles spontaneously i...
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Uterine proprotein convertase (PC) 6 plays a critical role in embryo implantation and is pivotal for pregnancy establishment. Inhibition of PC6 may provide a novel approach for the development of non-hormonal and female-controlled contraceptives. We investigated a class of five synthetic non-peptidic small molecule compounds that were previously reported as potent inhibitors of furin, another P...
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ژورنال
عنوان ژورنال: ACS Chemical Biology
سال: 2011
ISSN: 1554-8929,1554-8937
DOI: 10.1021/cb200253h