Novel Fe 3+-Based 1H MRI β-galactosidase reporter molecules

Jian Xin Yu, Praveen K. Gulaka, Li Liu, Vikram Kodibagkar, Ralph P. Mason

Research output: Contribution to journalArticle

10 Scopus citations

Abstract

There is increasing interest in the development of reporter agents to reveal enzyme activity in vivo using imaging in small animals. We have previously demonstrated the feasibility of detecting lacZ gene activity using the commercially available 3,4-cyclohexenoesculetin-β-D-galactopyranoside (S-Gal) as a 1H MRI reporter. Specifically, β-galactosidase (β-gal) releases the aglycone, which forms a magnetic resonance contrast-inducing paramagnetic precipitate in the presence of Fe 3+. Contrast was primarily T 2-weighted signal loss, but T 1 effects were also observed. Since T 1-contrast generally provides signal enhancement as opposed to loss, it appeared attractive to explore whether analogues could be generated with enhanced characteristics. We now report the design and synthesis of novel analogues together with characterization of 1H MRI contrast based on both T 1 and T 2 response to β-gal activity in vitro for the lead agent.

Original languageEnglish (US)
Pages (from-to)370-378
Number of pages9
JournalChemPlusChem
Volume77
Issue number5
DOIs
StatePublished - May 2012

Keywords

  • Enzymes
  • Hydrolases
  • NMR spectroscopy
  • Relaxivity
  • Reporter molecules

ASJC Scopus subject areas

  • Chemistry(all)

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