title: 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.
  
  
  BACKGROUND
  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.affiliation: School of Chemistry and Molecular Biosciences, The University of Queensland, St. Lucia, QLD, Australia.
authors.forename: Rachel
authors.initials: R
authors.lastname: Stephenson
authors.affiliation: School of Chemistry and Molecular Biosciences, The University of Queensland, St. Lucia, QLD, Australia.
authors.forename: Pegah
authors.initials: P
authors.lastname: Varamini
authors.affiliation: School of Biomedical Sciences, The University of Queensland, St. Lucia, QLD, Australia.
authors.forename: Neville
authors.initials: N
authors.lastname: Butcher
authors.affiliation: School of Biomedical Sciences, The University of Queensland, St. Lucia, QLD, Australia.
authors.forename: Rodney
authors.initials: R
authors.lastname: Minchin
authors.affiliation: School of Chemistry and Molecular Biosciences, The University of Queensland, St. Lucia, QLD, Australia; School of Pharmacy, The University of Queensland, Woollongabba, QLD, Australia. Electronic address: i.toth@uq.edu.au.
authors.forename: Istvan
authors.initials: I
authors.lastname: Toth
mesh_terms: D045744:Cell Line, Tumor; D007987:Gonadotropin-Releasing Hormone / Q000737:chemistry*; D006801:Humans; D008297:Male; D010455:Peptides / Q000737:chemistry* / Q000378:metabolism*; D011966:Receptors, LHRH / Q000378:metabolism*
chemical_list: D010455:Peptides; D011966:Receptors, LHRH; D007987:Gonadotropin-Releasing Hormone
keywords: Gonadotropin-releasing hormone; Lipoamino acid; Prostate cancer; Solid phase peptide synthesis; Targeting