PMID: 11906274Mar 22, 2002Paper

Synthesis and biologic evaluation of a radioiodinated quinazolinone derivative for enzyme-mediated insolubilization therapy

Bioconjugate Chemistry
Nan-hui HoAmin I Kassis

Abstract

We have developed a new strategy that aims to concentrate therapeutic radionuclides within solid tumors. This approach, which we have named EMIT (enzyme-mediated insolubilization therapy), is a method for enzyme-dependent, site-specific, in vivo precipitation of a radioactive molecule (from a water-soluble precursor) within the extracellular space of solid tumors. The prodrug, ammonium 2-(2'-phosphoryloxyphenyl)-6-iodo-4-(3H)-quinazolinone, labeled with iodine-125 ((125)IPD) and its authentic compound labeled with iodine-127 (IPD) have been synthesized, purified, and characterized. The alkaline phosphatase (ALP)-mediated conversion of these water-soluble nonfluorescent prodrugs to the water-insoluble fluorescent species, iodine-125-labeled 2-(2'-hydroxyphenyl)-6-iodo-4-(3H)-quinazolinone ((125)ID) and its iodine-127-labeled derivative (ID), has been demonstrated in vitro. Biodistribution studies in mice indicate that both (125)IPD and (125)ID are minimally retained by most tissues and organs. In addition, following its intravenous injection in mice, (125)IPD is localized in ALP-rich regions and converted to (125)ID, which remains indefinitely within the tissues where it is produced. We believe that EMIT is a strategy that will ...Continue Reading

References

Feb 1, 1990·FASEB Journal : Official Publication of the Federation of American Societies for Experimental Biology·P D Senter
Nov 1, 1987·British Journal of Cancer·K D Bagshawe
Jan 1, 1993·Bioconjugate Chemistry·P D SenterK E Hellström
Feb 21, 1996·Journal of the National Cancer Institute·R G Melton, R F Sherwood

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Citations

Oct 13, 2007·Applied Radiation and Isotopes : Including Data, Instrumentation and Methods for Use in Agriculture, Industry and Medicine·Ketai WangAmin I Kassis
Feb 7, 2012·Chemical Biology & Drug Design·Pavel PospisilAmin I Kassis
Feb 29, 2008·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Amin I KassisS James Adelstein
May 9, 2008·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Rajiv DahiyaRakesh Yadav
Dec 12, 2007·Neuropathology : Official Journal of the Japanese Society of Neuropathology·Norbert UlfigPayam Rezaie
Dec 18, 2009·Expert Review of Molecular Diagnostics·Yongliang Yang SAmin I Kassis

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