Large Protein Assemblies for High-Relaxivity Contrast Agents: The Case of Gadolinium-Labeled Asparaginase

Bioconjug Chem. 2022 Dec 21;33(12):2411-2419. doi: 10.1021/acs.bioconjchem.2c00506. Epub 2022 Dec 2.

Abstract

Biologics are emerging as the most important class of drugs and are used to treat a large variety of pathologies. Most of biologics are proteins administered in large amounts, either by intramuscular injection or by intravenous infusion. Asparaginase is a large tetrameric protein assembly, currently used against acute lymphoblastic leukemia. Here, a gadolinium(III)-DOTA derivative has been conjugated to asparaginase, and its relaxation properties have been investigated to assess its efficiency as a possible theranostic agent. The field-dependent 1H longitudinal relaxation measurements of water solutions of gadolinium(III)-labeled asparaginase indicate a very large increase in the relaxivity of this paramagnetic protein complex with respect to small gadolinium chelates, opening up the possibility of its use as an MRI contrast agent.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Asparaginase*
  • Chelating Agents
  • Contrast Media*
  • Gadolinium
  • Magnetic Resonance Imaging / methods

Substances

  • Contrast Media
  • Asparaginase
  • Gadolinium
  • Chelating Agents