ArticleNature protocols2012
Oxime-based linker libraries as a general approach for the rapid generation and screening of multidentate inhibitors.
Article in Nature protocols, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed.
- Identification of multidentate tyrosyl-DNA phosphodiesterase 1 (TDP1) inhibitors that simultaneously access the DNA, protein and catalytic-binding sites by oxime diversification.RSC chemical biology · 2023Article
- Applications and Limitations of Oxime-Linked "Split PROTACs".Chembiochem : a European journal of chemical biology · 2022Article
- Review
- Application of Post Solid-Phase Oxime Ligation to Fine-Tune Peptide-Protein Interactions.Molecules (Basel, Switzerland) · 2020Review
- Targeting Protein-Protein Interactions of Tyrosine Phosphatases with Microarrayed Fragment Libraries Displayed on Phosphopeptide Substrate Scaffolds.ACS combinatorial science · 2019Article
- A new synthetic pathway based on one-pot sequential aza-Michael addition and photoCuAAC click reactions.RSC advances · 2019Article
- Application of oxime-diversification to optimize ligand interactions within a cryptic pocket of the polo-like kinase 1 polo-box domain.Bioorganic & medicinal chemistry letters · 2016Article
- Structural analysis of human dual-specificity phosphatase 22 complexed with a phosphotyrosine-like substrate.Acta crystallographica. Section F, Structural biology communications · 2015Article
- Synthetic derivatives of the SUMO consensus sequence provide a basis for improved substrate recognition.Bioorganic & medicinal chemistry letters · 2015Article
- Peptide-functionalized oxime hydrogels with tunable mechanical properties and gelation behavior.Biomacromolecules · 2013Article
- Structure of the Trypanosoma cruzi protein tyrosine phosphatase TcPTP1, a potential therapeutic target for Chagas' disease.Molecular and biochemical parasitology · 2013Article
- Using a build-and-click approach for producing structural and functional diversity in DNA-targeted hybrid anticancer agents.Journal of medicinal chemistry · 2012Article
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Authors and funding
6 authors.
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Abstract
The described oxime-based library protocol provides detailed procedures for the linkage of aminooxy functionality with aldehyde building blocks that result in the generation of libraries of multidentate inhibitors. Synthesis of inhibitors for protein tyrosine phosphatases (PTPs) and antagonists directed against the human tumor susceptibility gene 101 (TSG101) are shown as examples. Three steps are involved: (i) the design and synthesis of aminooxy platforms; (ii) tethering with aldehydes to form oxime-based linkages with sufficient purity; and (iii) direct in vitro biological evaluation of oxime products without purification. Each coupling reaction is (i) performed in capped microtubes at room temperature (20-23 °C); (ii) diluted for inhibitory evaluation; and (iii) screened with targets in microplates to provide IC(50) or K(d) values. The synthesis of the aminooxy platforms takes 3-5 d; tethering with the aldehydes takes 24 h; and inhibition assay of enzymes and protein-protein interactions takes 30 min and 2 h, respectively.
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