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Updated: Jul 16, 2026

Efficient Construction of Drug-like Bispirocyclic Scaffolds Via Organocatalytic Cycloadditions of α-Imino γ-Lactones and Alkylidene Pyrazolones
Published on: February 7, 2019
Construction of di-scFv through a trivalent alkyne-azide 1,3-dipolar cycloaddition
Arutselvan Natarajan1, Wenjun Du, Cheng-Yi Xiong
1Radiodiagnosis and Therapy, Molecular Cancer Institute, University of California, Davis Medical Center, 1508 Alhambra Boulevard, Sacramento, CA 95816, USA.
Abstract:
Heterofunctional azide and alkyne PEG-linkers have been synthesized and site specifically conjugated to scFv via a reactive thiol functionality; two scFv were coupled by copper catalyzed 1,3-dipolar cycloaddition to make divalent scFv (di-scFv) with an inter-scFv distance defined to provide divalent binding; antigen binding was maintained for the di-scFv construct and increased several times compared to that of the parent scFv; the cycloaddition reaction reported herein represents an important ligation strategy to covalently link macromolecular proteins and retain sensitive structural conformations.
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