ArticleArchives of biochemistry and biophysics2011
Identification of novel small molecules that inhibit protein-protein interactions between MAGE and KAP-1.
Article in Archives of biochemistry and biophysics, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed.
- TIF1 Family Proteins as Modulators of Cell Death: Mechanisms and Therapeutic Opportunities.Biomolecules · 2026Review
- Inhibition of multiple staphylococcal growth states by a small molecule that disrupts membrane fluidity and voltage.mSphere · 2024Article
- Melanoma Antigen Family A (MAGE A) as Promising Biomarkers and Therapeutic Targets in Bladder Cancer.Cancers · 2024Review
- The Melanoma-Associated Antigen Family A (MAGE-A): A Promising Target for Cancer Immunotherapy?Cancers · 2023Review
- Discovery and Structural Basis of the Selectivity of Potent Cyclic Peptide Inhibitors of MAGE-A4.Journal of medicinal chemistry · 2022Article
- KAP1 is an antiparallel dimer with a functional asymmetry.Life science alliance · 2019Article
- Functional and mechanistic studies reveal MAGEA3 as a pro-survival factor in pancreatic cancer cells.Journal of experimental & clinical cancer research : CR · 2019Article
- Epigenetic regulation of MAGE family in human cancer progression-DNA methylation, histone modification, and non-coding RNAs.Clinical epigenetics · 2018Review
- A Comprehensive Guide to the MAGE Family of Ubiquitin Ligases.Journal of molecular biology · 2017Review
- MAGE proteins regulate KRAB zinc finger transcription factors and KAP1 E3 ligase activity.Archives of biochemistry and biophysics · 2014Article
- KAPtain in charge of multiple missions: Emerging roles of KAP1.World journal of biological chemistry · 2014Review
- Germ cell proteins in melanoma: prognosis, diagnosis, treatment, and theories on expression.Journal of skin cancer · 2012Article
- MAGE I transcription factors regulate KAP1 and KRAB domain zinc finger transcription factor mediated gene repression.PloS one · 2011Article
Corrections and comments
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Authors and funding
6 authors.
Funding
Abstract
The Class I MAGE proteins are normally expressed only in developing germ cells but are often aberrantly expressed in malignancies, particularly melanoma, making them good therapeutic targets. MAGE proteins promote tumor survival by binding to the RBCC region of KAP-1 and suppressing p53. Although, suppression of MAGE expression, by RNA interference, relieves p53 suppression and inhibits tumor growth, its therapeutic uses are limited by lack of methods for systemic delivery of small interfering RNA. To overcome this barrier, we sought to discover chemical compounds that inhibit binding between MAGE and KAP-1 proteins. Based on previously published effects of MAGE suppression, we developed a strategy for screening a small molecule library based on selective death of MAGE positive cells, activation of p53 and lack of caspase activity. We screened the Maybridge HitFinder library of compounds and eight compounds fulfilled these criteria. Seven of these compounds interfered with co-precipitation of MAGE and KAP-1, and three interfered with binding of MAGE and KAP-1 in a mammalian two hybrid assay. We now report identification of three potential compounds that interfere with MAGE/KAP-1 binding and can be developed as novel chemo-therapeutic agents for treatment of advanced melanoma and other cancers.
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