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Title: Highly potent metallopeptide analogues of luteinizing hormone-releasing hormone

Metal complexes related to the cytotoxic complexes cisplatin (cis-diamminedichloroplatinum(II)) and transbis(salicylaldoximato)copper(II) were incorporated into suitably modified luteinizing hormone-releasing hormone (LH-RH) analogues containing D-lysine at position 6. Some of the metallopeptides thus obtained proved to be highly active LH-RH agonists or antagonists. Most metallopeptide analogues of LH-RH showed high affinities for the membrane receptors of rat pituitary and human breast cancer cells. Some of these metallopeptides had cytotoxic activity against human breast cancer and prostate cancer and prostate cancer cell lines in vitro. Such cytostatic metallopeptides could be envisioned as targeted chemotherapeutic agents in cancers that contain receptors for LH-RH-like peptides.
Authors:
; ; ; ; ; ; ;  [1]
  1. (Tulane Univ. School of Medicine, New Orleans, LA (USA))
Publication Date:
OSTI Identifier:
7191552
Resource Type:
Journal Article
Resource Relation:
Journal Name: Proceedings of the National Academy of Sciences of the United States of America; (USA); Journal Volume: 86:16
Country of Publication:
United States
Language:
English
Subject:
59 BASIC BIOLOGICAL SCIENCES; AMINO ACIDS; METALLOPROTEINS; CROSS-LINKING; RECEPTORS; IODINE 125; LH; LIBERINS; LIQUID COLUMN CHROMATOGRAPHY; LYSINE; MAMMARY GLANDS; MOLECULAR STRUCTURE; PLATINUM COMPOUNDS; TUMOR CELLS; ANIMAL CELLS; BETA DECAY RADIOISOTOPES; BODY; CARBOXYLIC ACIDS; CHEMICAL REACTIONS; CHROMATOGRAPHY; DAYS LIVING RADIOISOTOPES; ELECTRON CAPTURE RADIOISOTOPES; GLANDS; GONADOTROPINS; HORMONES; INTERMEDIATE MASS NUCLEI; IODINE ISOTOPES; ISOTOPES; MEMBRANE PROTEINS; NUCLEI; ODD-EVEN NUCLEI; ORGANIC ACIDS; ORGANIC COMPOUNDS; ORGANS; PEPTIDE HORMONES; PITUITARY HORMONES; POLYMERIZATION; PROTEINS; RADIOISOTOPES; SEPARATION PROCESSES; TRANSITION ELEMENT COMPOUNDS 550201* -- Biochemistry-- Tracer Techniques