ReviewDrug discovery today. Technologies2019
A critical evaluation of the approaches to targeted protein degradation for drug discovery.
Review in Drug discovery today. Technologies, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
22 citing papers in PubMed.
- Halofuginone is a Molecular Glue Degrader of Integrin β4.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2026Article
- Recent advances in targeting protein degradation for tumor immunotherapy.Journal of hematology & oncology · 2025Review
- Targeting RBM39 suppresses tumor growth and sensitizes osteosarcoma cells to cisplatin.Oncogene · 2025Article
- Molecular glue-mediated targeted protein degradation: A novel strategy in small-molecule drug development.iScience · 2024Review
- Revisiting the antiangiogenic mechanisms of fluorinated thalidomide derivatives.Bioorganic & medicinal chemistry letters · 2024Article
- Methotrexate-based PROTACs as DHFR-specific chemical probes.Cell chemical biology · 2024Article
- The era of high-quality chemical probes.RSC medicinal chemistry · 2022Article
- SimPLIT: Simplified Sample Preparation for Large-Scale Isobaric Tagging Proteomics.Journal of proteome research · 2022Article
- Profiling of diverse tumor types establishes the broad utility of VHL-based ProTaCs and triages candidate ubiquitin ligases.iScience · 2022Article
- Roles of Cullin-RING Ubiquitin Ligases in Cardiovascular Diseases.Biomolecules · 2022Review
- Target 2035 - update on the quest for a probe for every protein.RSC medicinal chemistry · 2022Article
- Targeting the "undruggable" RAS with biologics.Advances in cancer research · 2022Review
- A Computational Investigation of In Vivo Cytosolic Protein Delivery for Cancer Therapy.Pharmaceutics · 2021Article
- Inhibitors of Cyclin-Dependent Kinases: Types and Their Mechanism of Action.International journal of molecular sciences · 2021Review
- A kinetic proofreading model for bispecific protein degraders.Journal of pharmacokinetics and pharmacodynamics · 2021Article
- On the correlation of cereblon binding, fluorination and antiangiogenic properties of immunomodulatory drugs.Biochemical and biophysical research communications · 2021Article
- High-Throughput Detection of Ligand-Protein Binding Using a SplitLuc Cellular Thermal Shift Assay.Methods in molecular biology (Clifton, N.J.) · 2021Article
- Understanding the Metabolism of Proteolysis Targeting Chimeras (PROTACs): The Next Step toward Pharmaceutical Applications.Journal of medicinal chemistry · 2020Article
- Article
- Systematic exploration of different E3 ubiquitin ligases: an approach towards potent and selective CDK6 degraders.Chemical science · 2020Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
3 authors.
Funding
Abstract
There is a great deal of excitement around the concept of targeting proteins for degradation as an alternative to conventional inhibitory small molecules and antibodies. Protein degradation can be undertaken by bifunctional molecules that bind the target for ubiquitin mediated degradation by complexing them with Cereblon (CRBN), von Hippel-Lindau or other E-3 ligases. Alternatively, E-3 ligase receptors such as CRBN or DCAF15 can also be used as a 'template' to bind IMiD or sulphonamide like compounds to degrade multiple context specific proteins by the selected E-3 ligases. The 'template approach' results in the degradation of neo-substrates, some of which would be difficult to drug using conventional approaches. The chemical properties necessary for drug discovery, the rules by which neo-substrates are selected by E-3 ligase receptors and defining the optimal components of the ubiquitin proteasome for protein degradation are still to be fully elucidate. Theis review will aim to critically evaluate the different approaches and principles emerging for targted protein degradation.
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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.