ArticleBiopolymers2011
Transcriptional tools: Small molecules for modulating CBP KIX-dependent transcriptional activators.
Article in Biopolymers, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed, 17 citations in OpenAlex.
- Discovery of peptidomimetic inhibitors of CREB/CBP by targeting hydrophobic grooves on the surface of the CBP KIX domain.Acta pharmaceutica Sinica. B · 2025Article
- Group 3 medulloblastoma transcriptional networks collapse under domain specific EP300/CBP inhibition.Nature communications · 2024Article
- Rational peptide design for inhibition of the KIX-MLL interaction.Scientific reports · 2023Article
- Targeting Unoccupied Surfaces on Protein-Protein Interfaces.Journal of the American Chemical Society · 2017Article
- The 9aaTAD Transactivation Domains: From Gal4 to p53.PloS one · 2016Article
- Protein lysine acetylation by p300/CBP.Chemical reviews · 2015Review
- Prepaying the entropic cost for allosteric regulation in KIX.Proceedings of the National Academy of Sciences of the United States of America · 2014Article
- The role of HTS in drug discovery at the University of Michigan.Combinatorial chemistry & high throughput screening · 2014Review
- Sequence and expression analyses of KIX domain proteins suggest their importance in seed development and determination of seed size in rice, and genome stability in Arabidopsis.Molecular genetics and genomics : MGG · 2013Article
- Sekikaic acid and lobaric acid target a dynamic interface of the coactivator CBP/p300.Angewandte Chemie (International ed. in English) · 2012Article
- Profiling the dynamic interfaces of fluorinated transcription complexes for ligand discovery and characterization.ACS chemical biology · 2012Article
- Enzyme inhibition by allosteric capture of an inactive conformation.Journal of molecular biology · 2011Article
Corrections and comments
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
Previously it was demonstrated that amphipathic isoxazolidines are able to functionally replace the transcriptional activation domains of endogenous transcriptional activators. In addition, in vitro binding studies suggested that a key binding partner of these molecules is the CREB Binding Protein (CBP), more specifically the KIX domain within this protein. Here we show that CBP plays an essential role in the ability of isoxazolidine transcriptional activation domains to activate transcription in cells. Consistent with this model, isoxazolidines are able to function as competitive inhibitors of the activators MLL and Jun, both of which utilize a binding interaction with KIX to up-regulate transcription. Further, modification of the N2 side chain produced three analogs with enhanced potency against Jun-mediated transcription, although increased cytotoxicity was also observed. Collectively these small KIX-binding molecules will be useful tools for dissecting the role of the KIX domain in a variety of pathological processes.
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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.