Tailored Bioorthogonal and Bioconjugate Chemistry: A Source of Inspiration for Developing Kinetic Target-Guided Synthesis Strategies

Kinetic target-guided synthesis (KTGS) is a promising tool for the discovery of biologically active compounds. It relies on the identification of potent ligands that are covalently assembled by the biological targets themselves from a pool of reagents. Significant effort is devoted to developing new...

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Bibliographic Details
Published in:Bioconjugate chemistry 2021-01, Vol.32 (1), p.63-72
Main Authors: Lossouarn, Alexis, Renard, Pierre-Yves, Sabot, Cyrille
Format: Article
Language:English
Subjects:
Bioactive compounds
Biocompatibility
Biological activity
Chemical reactions
Chemical Sciences
Dynamic stability
Organic chemistry
Reagents
Toolkits
Topical Review
Topology
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Summary:Kinetic target-guided synthesis (KTGS) is a promising tool for the discovery of biologically active compounds. It relies on the identification of potent ligands that are covalently assembled by the biological targets themselves from a pool of reagents. Significant effort is devoted to developing new KTGS strategies; however, only a handful of biocompatible reactions are available, which may be insufficient to meet the specificities (stability, dynamics, active site topology, etc.) of a wide range of biological targets with therapeutic potential. This Topical Review proposes a retrospective analysis of existing KTGS ligation tools, in terms of their kinetics and analogy with other biocompatible reactions, and provides new clues to expand the KTGS toolkit. By way of examples, a nonexhaustive selection of such chemical ligation tools belonging to different classes of reactions as promising candidate reactions for KTGS are suggested.
ISSN:1043-1802
1520-4812
DOI:10.1021/acs.bioconjchem.0c00568