Please use this identifier to cite or link to this item: http://hdl.handle.net/10397/7995
Title: Improving anticancer activity and selectivity of camptothecin through conjugation with releasable substance P
Authors: Zhang, W
Song, J
Mu, L
Zhang, B
Liu, L
Xing, Y
Wang, K
Li, Z
Wang, R
Keywords: Anticancer
Camptothecin
Neurokinin-1 receptor
Substance P
Issue Date: 2011
Publisher: Pergamon Press
Source: Bioorganic & medicinal chemistry letters, 2011, v. 21, no. 5, p. 1452-1455 How to cite?
Journal: Bioorganic & medicinal chemistry letters 
Abstract: Substance P, an 11-residue neuropeptide, can be rapidly internalized through specific interaction with the neurokinin-1 receptor. Therefore, we designed and synthesized the substance P targeted camptothecin (CPT) conjugates via a releasable disulfide carbonate linker. All the conjugates exhibited comparable or stronger cytotoxicity to cancer cells that highly over-express neurokinin-1 receptor than free CPT. More importantly, the selectivity of conjugates was significantly improved compared with CPT. Our results indicated that these conjugates can be promising candidates for new chemotherapeutic drugs. In addition, increasing CPT loading or attachment of CPT to the C-terminal hexapeptide of substance P are useful strategies to enhance the therapeutic efficacy of substance P targeted conjugates.
URI: http://hdl.handle.net/10397/7995
ISSN: 0960-894X
EISSN: 1464-3405
DOI: 10.1016/j.bmcl.2011.01.013
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