PMID: 11930107Apr 4, 2002Paper

Melanin affinity of N-(2-diethylaminoethyl)-4-iodobenzamide, an effective melanoma imaging agent

Melanoma Research
Pierre LabarreJ C Madelmont

Abstract

The cellular uptake and incorporation in macromolecules of iodine-125 labelled N-(2-diethylaminoethyl)-4-iodobenzamide ([125I]BZA), a melanoma imaging agent, was studied using human melanoma cells M3Dau (amelanotic) and M4Beu (melanotic). The interaction between [125I]BZA and synthetic melanin was examined in various conditions of incubation. The results showed that uptake was high only for M4Beu, whereas the incorporation in trichloroacetic acid-precipitable proteins was very low for both model cell lines, with no correlation with melanin content. Experiments with synthetic melanin showed that BZA binding to melanin was saturable and reversible, and involved several types of interaction. The influence of the ionic environment indicated that electrostatic forces play a role in the affinity, and the decrease in binding produced by the presence of an alcohol in the medium suggested that hydrophobic interactions may be involved in the binding mechanism. This was supported by the Scatchard analysis, which revealed two classes of binding sites, and the determination of two association constants (K1 = 3.9 +/- 1.9 x 106/M and K2 = 2.9 +/- 0.9 x 104/M). The affinity of BZA for melanin might explain the good results obtained in a phase ...Continue Reading

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Citations

Jun 19, 2012·European Journal of Nuclear Medicine and Molecular Imaging·Latifa Rbah-VidalJean-Michel Chezal
Oct 14, 2008·Nuclear Medicine and Biology·Xiang LiuAndrew Katsifis
Nov 3, 2009·Cancer Biotherapy & Radiopharmaceuticals·Elisabeth Miot-NoiraultNicole Moins
Jan 25, 2006·Melanoma Research·Martin M Edreira, Oscar R Pozzi
Mar 28, 2015·Journal of Materials Chemistry. B, Materials for Biology and Medicine·Audrey ParatDelphine Felder-Flesch
Aug 21, 2013·Organic & Biomolecular Chemistry·Mathieu AndréEmmanuelle Mounetou
Sep 18, 2009·Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine·Gang RenZhen Cheng

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