Synthesis of novel cyclic NGR/RGD peptide analogs via on resin click chemistry.
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.
Pediatric Oncology Branch, National Cancer Institute, National Institutes of Health, Bethesda, MD 20892, USA.
Belhu B
BB
Metaferia
Matthew
M
Rittler
Jinesh S
JS
Gheeya
Albert
A
Lee
Heidi
H
Hempel
Alberto
A
Plaza
William G
WG
Stetler-Stevenson
Carole A
CA
Bewley
Javed
J
Khan
D018826:CD13 Antigens / Q000737:chemistry / Q000378:metabolism; D045744:Cell Line, Tumor; D057930:Click Chemistry; D003500:Cyclization; D004337:Drug Carriers / Q000737:chemistry; D005454:Fluorescence Polarization; D006801:Humans; D010456:Peptides, Cyclic / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000737:chemistry; D011485:Protein Binding; D012117:Resins, Synthetic / Q000737:chemistry*
D004337:Drug Carriers; D010456:Peptides, Cyclic; D012117:Resins, Synthetic; C507169:cyclic arginine-glycine-aspartic acid peptide; D018826:CD13 Antigens