Facile Synthesis of Homodimeric Protein Ligands
Abstract: Many proteins exist as oligomers (homodimers, homotrimers, etc.). A proven strategy for the development of high affinity ligands for such targets is to link together two modest affinity ligands that allows the formation of a 2: 2 (or higher‐order) protein‐ligand complex. We report here the discovery of a convenient, “click‐like” reaction for the homodimerization of protein ligands that is efficient, operationally simple to carry out, and tolerant of many functional groups. This chemistry reduces the synthetic burden inherent in the creation of homodimeric ligands since only a single precursor is required. The utility of this strategy is demonstrated by the synthesis of homodimeric inhibitors, including PROTACs.
- Location
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Deutsche Nationalbibliothek Frankfurt am Main
- Extent
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Online-Ressource
- Language
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Englisch
- Bibliographic citation
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Facile Synthesis of Homodimeric Protein Ligands ; day:17 ; month:08 ; year:2023 ; extent:6
ChemBioChem ; (17.08.2023) (gesamt 6)
- Creator
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Gui, Weijun
Kodadek, Thomas
- DOI
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10.1002/cbic.202300392
- URN
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urn:nbn:de:101:1-2023081815113118901127
- Rights
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Open Access; Der Zugriff auf das Objekt ist unbeschränkt möglich.
- Last update
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14.08.2025, 11:02 AM CEST
Data provider
Deutsche Nationalbibliothek. If you have any questions about the object, please contact the data provider.
Associated
- Gui, Weijun
- Kodadek, Thomas