News Column

New Proteomics Findings from University of Illinois Discussed

May 27, 2014

By a News Reporter-Staff News Editor at Life Science Weekly -- Investigators publish new report on Proteomics. According to news reporting from Urbana, Illinois, by NewsRx journalists, research stated, "This study was aimed at developing a triazine-based modular platform for targeted PET imaging. We synthesized mono- or bis-cyclo(RGDfK) linked triazine-based conjugates specifically targeting integrin alpha(v)beta(3) receptors."

The news correspondents obtained a quote from the research from the University of Illinois, "The core molecules could be easily linked to targeting peptide and radiolabeled bifunctional chelator. The spacer core molecule was synthesized in 2 or 3 steps in 64-80% yield, and the following conjugation reactions with cyclo(RGDfK) peptide or bifunctional chelator were accomplished using 'click' chemistry or amidation reactions. The DOTA-TZ-Bis-cyclo(RGDfK) 13 conjugate was radiolabeled successfully with Cu-64(OAc)(2) using a microfluidic method, resulting in higher specific activity with above 95% labeling yields compared to conventional radiolabeling (SA ca. 850 vs 600 Ci/mmol). The dimeric cyclo(RGDfK) peptide was found to display significant bivalency effect using I-125-Echistatin binding assay with IC50 value as 178.5 +/- 57.1 nM, which displayed a 3.6-fold enhancement of binding affinity compared to DOTA-TZ-cyclo(RGDfK) 14 conjugate on U87MG human glioblastoma cell. Biodistribution of all four conjugates in female athymic nude mice were evaluated."

According to the news reporters, the research concluded: "DOTA-'Click'-cyclo(RGDfK) 15 had the highest tumor uptake among these four at 4 h p.i. with 1.90 +/- 0.65%ID/g, while there was no clear bivalency effect for DOTA-TZ-BisRGD in vivo, which needs further experiments to address the unexpected questions."

For more information on this research see: Triazine-Based Tool Box for Developing Peptidic PET Imaging Probes: Syntheses, Microfluidic Radio labeling, and Structure-Activity Evaluation. Bioconjugate Chemistry, 2014;25(4):761-772. Bioconjugate Chemistry can be contacted at: Amer Chemical Soc, 1155 16TH St, NW, Washington, DC 20036, USA. (American Chemical Society -; Bioconjugate Chemistry -

Our news journalists report that additional information may be obtained by contacting H.R. Li, University of Illinois, Dept. of Chem & Biomol Engn, Urbana, IL 61801, United States. Additional authors for this research include H.Y. Zhou, S. Krieger, J.J. Parry, J.J. Whittenberg, A.V. Desai, B.E. Rogers, P.J.A. Kenis and D.E. Reichert (see also Proteomics).

Keywords for this news article include: Urbana, Illinois, Peptides, Proteins, Proteomics, United States, North and Central America

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Source: Life Science Weekly

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