ArticleJournal of medicinal chemistry2010
Identification of non-peptide malignant brain tumor (MBT) repeat antagonists by virtual screening of commercially available compounds.
Article in Journal of medicinal chemistry, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed.
- Studies on the syntheses of β-carboline alkaloids brevicarine and brevicolline.Beilstein journal of organic chemistry · 2025Article
- Chemical tools targeting readers of lysine methylation.Current opinion in chemical biology · 2023Review
- Multitargeting nature of muscarinic orthosteric agonists and antagonists.Frontiers in physiology · 2022Review
- LEDGINs, Inhibitors of the Interaction Between HIV-1 Integrase and LEDGF/p75, Are Potent Antivirals with a Potential to Cure HIV Infection.Advances in experimental medicine and biology · 2021Article
- Developing Spindlin1 small-molecule inhibitors by using protein microarrays.Nature chemical biology · 2017Article
- A Structural Perspective on Readout of Epigenetic Histone and DNA Methylation Marks.Cold Spring Harbor perspectives in biology · 2016Review
- Identification of a fragment-like small molecule ligand for the methyl-lysine binding protein, 53BP1.ACS chemical biology · 2015Article
- High-throughput screening identifies small molecules that enhance the pharmacological effects of oligonucleotides.Nucleic acids research · 2015Article
- Towards understanding methyllysine readout.Biochimica et biophysica acta · 2014Review
- Readers of histone methylarginine marks.Biochimica et biophysica acta · 2014Review
- Writing and rewriting the epigenetic code of cancer cells: from engineered proteins to small molecules.Molecular pharmacology · 2013Review
- Assessment of free energy predictors for ligand binding to a methyllysine histone code reader.Journal of computational chemistry · 2012Article
- Structure-based virtual screening for drug discovery: a problem-centric review.The AAPS journal · 2012Review
- Small-molecule ligands of methyl-lysine binding proteins.Journal of medicinal chemistry · 2011Article
- Biophysical probes reveal a "compromise" nature of the methyl-lysine binding pocket in L3MBTL1.Journal of the American Chemical Society · 2011Article
- Drug discovery toward antagonists of methyl-lysine binding proteins.Current chemical genomics · 2011Article
- Methods for Activity Analysis of the Proteins that Regulate Histone Methylation.Current chemical genomics · 2011Article
Corrections and comments
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Authors and funding
6 authors.
Funding
Abstract
The malignant brain tumor (MBT) repeat is an important epigenetic-code "reader" and is functionally associated with differentiation, gene silencing, and tumor suppression. (1-3) Small molecule probes of MBT domains should enable a systematic study of MBT-containing proteins and potentially reveal novel druggable targets. We designed and applied a virtual screening strategy that identified potential MBT antagonists in a large database of commercially available compounds. A small set of virtual hits was purchased and submitted to experimental testing. Nineteen of the purchased compounds showed a specific dose-dependent protein binding and will provide critical structure-activity information for subsequent lead generation and optimization.
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Registered trials
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