ArticleProceedings of the National Academy of Sciences of the United States of America1997
A versatile synthetic dimerizer for the regulation of protein-protein interactions.
Article in Proceedings of the National Academy of Sciences of the United States of America, 1997. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 64 papers.
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Who cites it
64 citing papers in PubMed, 205 citations in OpenAlex.
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- Discovery of DCAF16 Binders for Targeted Protein Degradation.ACS chemical biology · 2025Article
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- Regulation of autophagy by VPS34 branched ubiquitination controls proteostasis and liver metabolism.Molecular & cellular oncology · 2021Article
- Induced Dimerization Tools to Deplete Specific Phosphatidylinositol Phosphates.Methods in molecular biology (Clifton, N.J.) · 2021Article
- PHOTACs enable optical control of protein degradation.Science advances · 2020Article
- Electrophilic PROTACs that degrade nuclear proteins by engaging DCAF16.Nature chemical biology · 2019Article
- A split fluorescent reporter with rapid and reversible complementation.Nature communications · 2019Article
- Calibration-free In Vitro Quantification of Protein Homo-oligomerization Using Commercial Instrumentation and Free, Open Source Brightness Analysis Software.Journal of visualized experiments : JoVE · 2018Article
- FKBP Ligands-Where We Are and Where to Go?Frontiers in pharmacology · 2018Review
- nandb-number and brightness in R with a novel automatic detrending algorithm.Bioinformatics (Oxford, England) · 2017Article
4 more citing papers are in PubMed but not listed here.
Corrections and comments
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Authors and funding
11 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The use of low molecular weight organic compounds to induce dimerization or oligomerization of engineered proteins has wide-ranging utility in biological research as well as in gene and cell therapies. Chemically induced dimerization can be used to activate intracellular signal transduction pathways or to control the activity of a bipartite transcription factor. Dimerizer systems based on the natural products cyclosporin, FK506, rapamycin, and coumermycin have been described. However, owing to the complexity of these compounds, adjusting their binding or pharmacological properties by chemical modification is difficult. We have investigated several families of readily prepared, totally synthetic, cell-permeable dimerizers composed of ligands for human FKBP12. These molecules have significantly reduced complexity and greater adaptability than natural product dimers. We report here the efficacies of several of these new synthetic compounds in regulating two types of protein dimerization events inside engineered cells--induction of apoptosis through dimerization of engineered Fas proteins and regulation of transcription through dimerization of transcription factor fusion proteins. One dimerizer in particular, AP1510, proved to be exceptionally potent and versatile in all experimental contexts tested.
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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.