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

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:20

Article

Metaferia, Belhu B.¹  Rittler, Matthew²  Gheeya, Jinesh S.¹  Lee, Albert¹  Hempel, Heidi¹  Plaza, Alberto³  Stetler-Stevenson, William G.²  Bewley, Carole A.³  Khan, Javed¹ 

[1] NCI, Pediat Oncol Branch, NIH, Bethesda, MD 20892 USA

[2] NCI, Radiat Oncol Branch, NIH, Bethesda, MD 20892 USA

[3] NIDDK, Bioorgan Chem Lab, NIH, Bethesda, MD 20892 USA

关键词: Click chemistry;    Aminopeptidase N;    Cyclic peptides;    Targeted delivery;    Fluorescence polarization;   

DOI  :  10.1016/j.bmcl.2010.10.064

来源: Elsevier

【 摘 要 】

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. Published by Elsevier Ltd.

【 授权许可】

Free