ArticleJournal of medicinal chemistry2022
Optimizing Shape Complementarity Enables the Discovery of Potent Tricyclic BCL6 Inhibitors.
Article in Journal of medicinal chemistry, 2022. 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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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
12 citing papers in PubMed.
- KCTD1 stabilizes c-Myc to upregulate PD-L1 and suppress anti-tumor immunity in hepatocellular carcinoma.Cell death discovery · 2026Article
- Antiviral drug discovery and development: challenges and future directions.Signal transduction and targeted therapy · 2026Review
- Design and synthesis of novelFuture medicinal chemistry · 2025Article
- How CBX proteins regulate normal and leukemic blood cells.FEBS letters · 2024Review
- Relocalizing transcriptional kinases to activate apoptosis.Science (New York, N.Y.) · 2024Article
- 3D-QSAR, ADMET, and molecular docking studies of aztreonam analogs asSAGE open medicine · 2024Article
- Determination of Ligand-Binding Affinity (Journal of medicinal chemistry · 2023Article
- Rewiring cancer drivers to activate apoptosis.Nature · 2023Article
- Discovery of anJournal of medicinal chemistry · 2023Article
- 30th Annual GPPharmaceuticals (Basel, Switzerland) · 2023Article
- Discovering cell-active BCL6 inhibitors: effectively combining biochemical HTS with multiple biophysical techniques, X-ray crystallography and cell-based assays.Scientific reports · 2022Article
- Improved Binding Affinity and Pharmacokinetics Enable Sustained Degradation of BCL6Journal of medicinal chemistry · 2022Article
Corrections and comments
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Authors and funding
25 authors.
Funding
Abstract
To identify new chemical series with enhanced binding affinity to the BTB domain of B-cell lymphoma 6 protein, we targeted a subpocket adjacent to Val18. With no opportunities for strong polar interactions, we focused on attaining close shape complementarity by ring fusion onto our quinolinone lead series. Following exploration of different sized rings, we identified a conformationally restricted core which optimally filled the available space, leading to potent BCL6 inhibitors. Through X-ray structure-guided design, combined with efficient synthetic chemistry to make the resulting novel core structures, a >300-fold improvement in activity was obtained by the addition of seven heavy atoms.
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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.