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
Deutsche Nationalbibliothek Frankfurt am Main
Extent
Online-Ressource
Language
Englisch

Bibliographic citation
Facile Synthesis of Homodimeric Protein Ligands ; day:17 ; month:08 ; year:2023 ; extent:6
ChemBioChem ; (17.08.2023) (gesamt 6)

Creator
Gui, Weijun
Kodadek, Thomas

DOI
10.1002/cbic.202300392
URN
urn:nbn:de:101:1-2023081815113118901127
Rights
Open Access; Der Zugriff auf das Objekt ist unbeschränkt möglich.
Last update
14.08.2025, 11:02 AM CEST

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Associated

  • Gui, Weijun
  • Kodadek, Thomas

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