Dynamic combinatorial chemistry as an instrument for developing heparin antidotes

Authors

  • Daniel Carbajo Institut de Química Avançada de Catalunya (IQAC-CSIC). Departament de Química Biològica. Grup de Química Supramolecular
  • Ignacio Alfonso Institut de Química Avançada de Catalunya (IQAC-CSIC). Departament de Química Biològica. Grup de Química Supramolecular

  • DOI: 10.2436/20.2003.01.159

Keywords:

Dynamic combinatorial chemistry, heparin, molecular recognition, antidotes, glycosaminoglycans, blood coagulation

Abstract

Dynamic combinatorial chemistry is a useful approach to the identification of ligands to complex and structure-elusive targets. Heparin-like macromolecules are widely used in hospitals as anticoagulant drugs. However, the search for heparin antidotes based on small molecules to control blood coagulation still remains a challenging task due to the peculiar physicochemical properties of this anionic polysaccharide. This article presents a compendium of our efforts to apply dynamic combinatorial chemistry in order to identify ligands to heparin assembled from extremely simple building blocks; to optimize them subsequently in order for them to act as true heparin antidotes; and finally to explore their activity against the full range of heparinoids.

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Published

2026-01-26

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Section

Articles