ArticleScience advances2021
Targeting oncoproteins with a positive selection assay for protein degraders.
Article in Science advances, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers.
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Who cites it
24 citing papers in PubMed, 45 citations in OpenAlex.
- Positive selection screen identifies natural product β-catenin inactivators.Proceedings of the National Academy of Sciences of the United States of America · 2026Article
- Leveraging high-throughput proteomics and AI-based protein folding to accelerate VAV1 molecular glue discovery.Nature communications · 2026Article
- Oncogenic Gα signaling requires AP-3-dependent recruitment to the endolysosomal compartment.Proceedings of the National Academy of Sciences of the United States of America · 2026Article
- A rapid imaging-based screen for induced-proximity degraders identifies a potent degrader of oncoprotein SKP2.Nature biotechnology · 2026Article
- Ratiometric transcriptional activation by protein degradation.bioRxiv : the preprint server for biology · 2026Article
- Target agnostic cellular screening in the era of chemically induced proximity.RSC medicinal chemistry · 2025Review
- Optimization and Evaluation of Complementary Degrader Discovery Assays for Application in Screening.ACS pharmacology & translational science · 2025Article
- Beyond the G-Loop: CRBN Molecular Glues Potently Target VAV1 via a Novel SH3 RT-Loop Degron.bioRxiv : the preprint server for biology · 2025Article
- Next steps for targeted protein degradation.Cell chemical biology · 2025Review
- Extrapolating Lessons from Targeted Protein Degradation to Other Proximity-Inducing Drugs.ACS chemical biology · 2024Review
- Total loss ofProceedings of the National Academy of Sciences of the United States of America · 2024Article
- Mammalian SWI/SNF complex activity regulates POU2F3 and constitutes a targetable dependency in small cell lung cancer.Cancer cell · 2024Article
- Distinct Regulation of ASCL1 by the Cell Cycle and Chemotherapy in Small Cell Lung Cancer.Molecular cancer research : MCR · 2024Article
- Article
- Novel approaches to targeted protein degradation technologies in drug discovery.Expert opinion on drug discovery · 2023Review
- E3-Specific Degrader Discovery by Dynamic Tracing of Substrate Receptor Abundance.Journal of the American Chemical Society · 2023Article
- nuPRISM: Microfluidic Genome-Wide Phenotypic Screening Platform for Cellular Nuclei.ACS central science · 2022Article
- USP13 promotes deubiquitination of ZHX2 and tumorigenesis in kidney cancer.Proceedings of the National Academy of Sciences of the United States of America · 2022Article
- Inhibition of Karyopherin β1-Mediated Nuclear Import Disrupts Oncogenic Lineage-Defining Transcription Factor Activity in Small Cell Lung Cancer.Cancer research · 2022Article
- Regulation of neuroendocrine plasticity by the RNA-binding protein ZFP36L1.Nature communications · 2022Article
Corrections and comments
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Authors and funding
26 authors at 6 institutions in 1 country.
Funding
Abstract
Most intracellular proteins lack hydrophobic pockets suitable for altering their function with drug-like small molecules. Recent studies indicate that some undruggable proteins can be targeted by compounds that can degrade them. For example, thalidomide-like drugs (IMiDs) degrade the critical multiple myeloma transcription factors IKZF1 and IKZF3 by recruiting them to the cereblon E3 ubiquitin ligase. Current loss of signal ("down") assays for identifying degraders often exhibit poor signal-to-noise ratios, narrow dynamic ranges, and false positives from compounds that nonspecifically suppress transcription or translation. Here, we describe a gain of signal ("up") assay for degraders. In arrayed chemical screens, we identified novel IMiD-like IKZF1 degraders and Spautin-1, which, unlike the IMiDs, degrades IKZF1 in a cereblon-independent manner. In a pooled CRISPR-Cas9-based screen, we found that CDK2 regulates the abundance of the ASCL1 oncogenic transcription factor. This methodology should facilitate the identification of drugs that directly or indirectly degrade undruggable proteins.
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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.