ReviewComputational and structural biotechnology journal2019
Bivalent Ligands for Protein Degradation in Drug Discovery.
Review in Computational and structural biotechnology journal, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 41 papers, 1 of them a synthesis that pooled it.
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
41 citing papers in PubMed, 1 synthesis or guideline pooled it, 114 citations in OpenAlex.
- Evolution and impact of molecular glue research: a bibliometric analysis from 2000 to 2023.Frontiers in oncology · 2024Pooled it
- Advancing PROTAC therapeutics through chemistry-guided design of smart delivery systems.Acta pharmacologica Sinica · 2026Review
- PROTAC-mediated regulation of programmed cell death: From molecular mechanisms to therapeutic breakthroughs.Innovation (Cambridge (Mass.)) · 2026Review
- Targeting ubiquitination in disease and therapy.Signal transduction and targeted therapy · 2025Review
- Rational design of the linkers in targeting chimeras.Chemical science · 2025Review
- Development of Peptidomimetic PROTACs as Potential Degraders of 3-Chymotrypsin-like Protease of SARS-CoV-2.International journal of molecular sciences · 2025Article
- Chemoproteomics-EnabledJournal of the American Chemical Society · 2025Article
- Recent advances in targeted protein degraders as potential therapeutic agents.Molecular diversity · 2024Review
- Analysis of alternative splicing in chicken macrophages infected with avian pathogenicAnimal biotechnology · 2023Article
- Molecular Glues: The Adhesive Connecting Targeted Protein Degradation to the Clinic.Biochemistry · 2023Review
- Emerging TACnology: Heterobifunctional Small Molecule Inducers of Targeted Posttranslational Protein Modifications.Molecules (Basel, Switzerland) · 2023Review
- Proteolysis-Targeting Chimeras (PROTACs) in Cancer Therapy: Present and Future.Molecules (Basel, Switzerland) · 2022Review
- Immune Pathway and Gene Database (IMPAGT) Revealed the Immune Dysregulation Dynamics and Overactivation of the PI3K/Akt Pathway in Tumor Buddings of Cervical Cancer.Current issues in molecular biology · 2022Article
- Recent Advances in PROTACs for Drug Targeted Protein Research.International journal of molecular sciences · 2022Review
- Emerging strategies to overcome resistance to third-generation EGFR inhibitors.Journal of hematology & oncology · 2022Review
- Targeted Degradation of 53BP1 Using Ubiquitin Variant Induced Proximity.Biomolecules · 2022Article
- HDAC Inhibitors: Innovative Strategies for Their Design and Applications.Molecules (Basel, Switzerland) · 2022Review
- PROTAC: targeted drug strategy. Principles and limitations.Russian chemical bulletin = Izvestiia Akademii nauk. Seriia khimicheskaia · 2022Review
- Post-Translational Modifications of BRD4: Therapeutic Targets for Tumor.Frontiers in oncology · 2022Review
- Targeting transcription cycles in cancer.Nature reviews. Cancer · 2022Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
4 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Targeting the "undruggable" proteome remains one of the big challenges in drug discovery. Recent innovations in the field of targeted protein degradation and manipulation of the ubiquitin-proteasome system open up new therapeutic approaches for disorders that cannot be targeted with conventional inhibitor paradigms. Proteolysis targeting chimeras (PROTACs) are bivalent ligands in which a compound that binds to the protein target of interest is connected to a second molecule that binds an E3 ligase via a linker. The E3 protein is usually either Cereblon or Von Hippel-Lindau. Several examples of selective PROTAC molecules with potent effect in cells and in vivo models have been reported. The degradation of specific proteins via these bivalent molecules is already allowing for the study of biochemical pathways and cell biology with more specificity than was possible with inhibitor compounds. In this review, we provide a comprehensive overview of recent developments in the field of small molecule mediated protein degradation, including transcription factors, kinases and nuclear receptors. We discuss the potential benefits of protein degradation over inhibition as well as the challenges that need to be overcome.
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What OpenQuestion holds
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.