10-21-2008, 11:40 AM
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#2
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Senior Member
Join Date: Feb 2008
Location: South East Wisconsin
Posts: 3,431
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From pubmed:
- 1: Cancer Lett. 2008 Oct 4. [Epub ahead of print]
Links
- Synthesis and anti-cancer activity of covalent conjugates of artemisinin and a transferrin-receptor targeting peptide.
Oh S, Kim BJ, Singh NP, Lai H, Sasaki T.
Department of Chemistry, University of Washington, Box 351700, Seattle, WA 98195-1700, USA.
Artemisinin, a natural product isolated from Artemisia annua L., shows a unique anti-cancer activity by an iron dependent mechanism. Artemisinin was covalently conjugated to a transferrin-receptor targeting peptide, HAIYPRH that binds to a cavity on the surface of transferrin receptor. This enables artemisinin to be co-internalized with receptor-bound transferrin. The iron released from transferrin can activate artemisinin to generate toxic radical species to kill cells. The artemisinin-peptide conjugates showed potent anti-cancer activity against Molt-4 leukemia cells with a significantly improved cancer/normal cells selectivity.
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