ArticleADMET & DMPK2021
Are we ready to design oral PROTACs®?
Article in ADMET & DMPK, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed, 21 citations in OpenAlex.
- Protacs in oral cancer: degrading oncogenic drivers for next-generation therapy.Frontiers in oral health · 2026Review
- Inhibition of equilibrative nucleoside transporters 1 and 2 by proteolysis-targeting chimeras (PROTACs).The Journal of pharmacology and experimental therapeutics · 2025Article
- Nucleic acid-encoded antibody gene transfer-next generation of antibody therapies.Drug delivery · 2025Review
- PROTAC-PatentDB: A PROTAC Patent Compound Dataset.Scientific data · 2025Article
- Recent Advances in the Development of Pro-PROTAC for Selective Protein Degradation.Pharmaceutics · 2025Review
- Linker Methylation as a Strategy to Enhance PROTAC Oral Bioavailability: Insights from Molecular Properties and Conformational Analysis.Journal of medicinal chemistry · 2025Article
- Tissue distribution and retention drives efficacy of rapidly clearing VHL-based PROTACs.Communications medicine · 2024Article
- An updated review of small-molecule HPK1 kinase inhibitors (2016-present).Future medicinal chemistry · 2024Review
- Complete elimination of estrogen receptor α by PROTAC estrogen receptor α degrader ERD-148 in breast cancer cells.Breast cancer research and treatment · 2024Article
- Targeted Protein Degradation: Advances, Challenges, and Prospects for Computational Methods.Journal of chemical information and modeling · 2023Review
- Discovery of ARD-2051 as a Potent and Orally Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of Androgen Receptor for the Treatment of Advanced Prostate Cancer.Journal of medicinal chemistry · 2023Article
- Uncovering the Kinetic Characteristics and Degradation Preference of PROTAC Systems with Advanced Theoretical Analyses.JACS Au · 2023Article
- Designing Soluble PROTACs: Strategies and Preliminary Guidelines.Journal of medicinal chemistry · 2022Article
- Novel Design Strategies to Enhance the Efficiency of Proteolysis Targeting Chimeras.ACS pharmacology & translational science · 2022Review
- New therapeutic modalities in drug discovery and development: Insights & opportunities.ADMET & DMPK · 2021Article
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
PROTACs® are expected to strongly impact the future of drug discovery. Therefore, in this work we firstly performed a statistical study to highlight the distribution of E3 ligases and POIs collected in PROTAC-DB, the main online database focused on degraders. Moreover, since the emerging technology of protein degradation deals with large and complex chemical structures, the second part of the paper focuses on how to set up a property-based design strategy to obtain oral degraders. For this purpose, we calculated a pool of seven previously ad hoc selected 2D descriptors for the 2258 publicly available degraders in PROTAC-DB (average values: MW= 972.9 Da, nC= 49.5, NAR= 4.5, PHI= 17.3, nHDon= 4.5, nHAcc= 17.7 and TPSA= 240 Å
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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.