ArticleChemical communications (Cambridge, England)2021
Traceless Staudinger ligation enabled parallel synthesis of proteolysis targeting chimera linker variants.
Article in Chemical communications (Cambridge, England), 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
What it found
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The trial behind it
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Who cites it
14 citing papers in PubMed, 38 citations in OpenAlex.
- Synthesis, biological evaluation and clinical trials of Cereblon-based PROTACs.Communications chemistry · 2025Review
- PROTAC-Based Antivirals for Respiratory Viruses: A Novel Approach for Targeted Therapy and Vaccine Development.Microorganisms · 2025Review
- Next steps for targeted protein degradation.Cell chemical biology · 2025Review
- Property-based optimisation of PROTACs.RSC medicinal chemistry · 2025Article
- Click chemistry in the development of PROTACs.RSC chemical biology · 2024Review
- Rapid PROTAC Discovery Platform: Nanomole-Scale Array Synthesis and Direct Screening of Reaction Mixtures.ACS medicinal chemistry letters · 2023Article
- Late-stage synthesis of heterobifunctional molecules for PROTAC applications via ruthenium-catalysed C‒H amidation.Nature communications · 2023Article
- DNA framework-engineered chimeras platform enables selectively targeted protein degradation.Nature communications · 2023Article
- Targeted Protein Degradation: Clinical Advances in the Field of Oncology.International journal of molecular sciences · 2022Review
- PROTACs for BRDs proteins in cancer therapy: a review.Journal of enzyme inhibition and medicinal chemistry · 2022Review
- A Versatile and Sustainable Multicomponent Platform for the Synthesis of Protein Degraders: Proof-of-Concept Application to BRD4-Degrading PROTACs.Journal of medicinal chemistry · 2022Article
- Applications and Limitations of Oxime-Linked "Split PROTACs".Chembiochem : a European journal of chemical biology · 2022Article
- A platform for the rapid synthesis of proteolysis targeting chimeras (Rapid-TAC) under miniaturized conditions.European journal of medicinal chemistry · 2022Article
- Unraveling the Role of Linker Design in Proteolysis Targeting Chimeras.Journal of medicinal chemistry · 2021Review
Corrections and comments
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
A parallel, one-pot assembly approach to proteolysis targeting chimeras (PROTACs) is demonstrated utilizing activated esters generated in situ, and traceless Staudinger ligation chemistry. The method described allows for rapid structure-activity relationship studies of PROTAC linker variants. Two previously studied systems, cereblon and BRD4 degraders, are examined as test cases for the synthetic method. The two related strategies to assemble PROTAC linker variants discussed can accommodate the chromotographic separations capabilities of labs of many sizes and incorporates commercially available degrader building blocks, thereby easing synthetic entry into PROTAC chemical space.
Identifiers
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.