This heterobifunctional, PEGylated crosslinker features a carboxylic acid at one end and propargyl group at the other for reaction with azide-containing compounds using click chemistry. The hydrophillic PEG linker facilitates solubility in biological applications. Propargyl-PEG4-acid can be used for bioconjugation or as a building block for synthesis of small molecules, conjugates of small molecules and/or biomolecules, or other tool compounds for chemical biology and medicinal chemistry that require ligation. Examples of applications include its synthetic incorporation into antibody-drug conjugates or proteolysis-targeting chimeras (PROTAC® molecules) for targeted protein degradation.
Archiv der Pharmazie, 348(10), 689-703 (2015-09-04)
A Cu-mediated azide-alkyne click chemistry protocol was employed for the synthesis of a focused library of novel 1,2,3-triazolyl conjugates bearing various carbohydrate-steroid/triterpenoid entities. The immunogenicity of these compounds was examined initially by ex vivo assays. The lead compound 15g was
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