ArticleJournal of the American Chemical Society2009
Discovery of inhibitors of aberrant gene transcription from Libraries of DNA binding molecules: inhibition of LEF-1-mediated gene transcription and oncogenic transformation.
Article in Journal of the American Chemical Society, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed, 37 citations in OpenAlex.
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- Discovery and Structure-Activity Relationships of the Neoseptins: A New Class of Toll-like Receptor-4 (TLR4) Agonists.Journal of medicinal chemistry · 2016Article
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- Discovery libraries targeting the major enzyme classes: the serine hydrolases.Bioorganic & medicinal chemistry letters · 2014Article
- Inhibition of adenovirus replication by a trisubstituted piperazin-2-one derivative.Antiviral research · 2014Article
- Comprehensive peptidomimetic libraries targeting protein-protein interactions.Accounts of chemical research · 2012Article
- Discovery of HIV fusion inhibitors targeting gp41 using a comprehensive α-helix mimetic library.Bioorganic & medicinal chemistry letters · 2012Article
- Design and synthesis of a bivalent ligand to explore the putative heterodimerization of the mu opioid receptor and the chemokine receptor CCR5.Organic & biomolecular chemistry · 2012Article
- Expanding the repertoire of natural product-inspired ring pairs for molecular recognition of DNA.Organic letters · 2011Article
- Design, synthesis, and validation of a β-turn mimetic library targeting protein-protein and peptide-receptor interactions.Journal of the American Chemical Society · 2011Article
- Identification of broad-based HIV-1 protease inhibitors from combinatorial libraries.The Biochemical journal · 2010Article
- Semi-automated high-throughput fluorescent intercalator displacement-based discovery of cytotoxic DNA binding agents from a large compound library.Bioorganic & medicinal chemistry letters · 2010Article
- Small molecule inhibitors of Myc/Max dimerization and Myc-induced cell transformation.Bioorganic & medicinal chemistry letters · 2009Article
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
The screening of a >9000 compound library of synthetic DNA binding molecules for selective binding to the consensus sequence of the transcription factor LEF-1 followed by assessment of the candidate compounds in a series of assays that characterized functional activity (disruption of DNA-LEF-1 binding) at the intended target and site (inhibition of intracellular LEF-1-mediated gene transcription) resulting in a desired phenotypic cellular change (inhibit LEF-1-driven cell transformation) provided two lead compounds: lefmycin-1 and lefmycin-2. The sequence of screens defining the approach assures that activity in the final functional assay may be directly related to the inhibition of gene transcription and DNA binding properties of the identified molecules. Central to the implementation of this generalized approach to the discovery of DNA binding small molecule inhibitors of gene transcription was (1) the use of a technically nondemanding fluorescent intercalator displacement (FID) assay for initial assessment of the DNA binding affinity and selectivity of a library of compounds for any sequence of interest, and (2) the technology used to prepare a sufficiently large library of DNA binding compounds.
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What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.