Effect of lipidated gonadotropin-releasing hormone peptides on receptor mediated binding and uptake into prostate cancer cells in vitro.

Abstract

Gonadotropin-releasing hormone (GnRH) receptors are overexpressed on many cancer cells but not on primary cell lines. This study was designed to investigate the targeting ability and uptake of dendritic lipidated [Gln(1)]-GnRH peptide analogues on receptor-positive prostate cancer PC-3 cells relative to receptor-negative ovarian carcinoma SKOV-3 cells for potential application in drug delivery. Direct antiproliferative effect of these was investigated on three GnRH-receptor positive cancer cells, PC-3, LNCaP and DU145. A significant dose dependent growth inhibitory effect was produced in DU145 cells by 5 dendrimers giving an IC50 value of 22-35 μM. All compounds were non-toxic to the normal peripheral blood mononuclear cells.

FROM THE CLINICAL EDITOR:

This study demonstrates the use of specific dendritic lapidated GnRH analogues in growth inhibition of GnRH receptor positive prostate cancer cell lines, suggesting potential future clinical use of this or similar strategies to address GnRH receptor positive cancer cells.

• Authors: Rachel Stephenson, Pegah Varamini, Neville Butcher, Rodney Minchin, Istvan Toth
• Journal: Nanomedicine : nanotechnology, biology, and medicine (Nanomedicine) Vol. 10 Issue 8 Pg. 1799-808 (Nov 2014) ISSN: 1549-9642 [Electronic] United States
• PMID: 25014892 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2014 Elsevier Inc. All rights reserved.

Chemical References

• Peptides
• Receptors, LHRH
• Gonadotropin-Releasing Hormone

Topics

• Cell Line, Tumor
• Gonadotropin-Releasing Hormone (chemistry)
• Humans
• Male
• Peptides (chemistry, metabolism)
• Receptors, LHRH (metabolism)