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Synthesis of novel cyclic NGR/RGD peptide analogs via on resin click chemistry.

ABSTRACT: Targeted drug deliveries as well as high resolution imaging of cancerous tissues and organs via specific cancer cell markers have become important in chemotherapeutic interventions of cancer treatment. Short peptides such as RGD and NGR are showing promising results for targeted drug delivery and in vivo imaging. We have applied on resin Huisgen's 1,3-dipolar cycloaddition to synthesize new cyclic RGD and NGR peptide analogs. Preliminary binding assays of these new analogs by fluorescence polarization indicates specific binding to purified CD13 (Aminopeptidase N) and cell lysates from MCF-7 and SKOV-3 cancer cell lines.

SUBMITTER: Metaferia BB

PROVIDER: S-EPMC3472425 | biostudies-literature | 2010 Dec

REPOSITORIES: biostudies-literature

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Synthesis of novel cyclic NGR/RGD peptide analogs via on resin click chemistry.

Metaferia Belhu B BB Rittler Matthew M Gheeya Jinesh S JS Lee Albert A Hempel Heidi H Plaza Alberto A Stetler-Stevenson William G WG Bewley Carole A CA Khan Javed J

Bioorganic & medicinal chemistry letters 20101021 24

Targeted drug deliveries as well as high resolution imaging of cancerous tissues and organs via specific cancer cell markers have become important in chemotherapeutic interventions of cancer treatment. Short peptides such as RGD and NGR are showing promising results for targeted drug delivery and in vivo imaging. We have applied on resin Huisgen's 1,3-dipolar cycloaddition to synthesize new cyclic RGD and NGR peptide analogs. Preliminary binding assays of these new analogs by fluorescence polari ...[more]

PMID: 21050757

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