HOMEPRODUCTSSERVICESCOMPANYCONTACTFAQResearchDictionaryPharmaMobileSign Up FREE or Login

In vivo studies of the new gonadotropin-releasing hormone antagonist--copolymer conjugates having antitumor activity.

Abstract
The aim of the study was to test in vivo the gonadotropin-releasing hormone (GnRH) antagonists and their conjugates showing antitumor activities in vitro. The in vivo experiments with the human GnRH antagonist MI-1544 (Ac-D-Trp1,3,D-Cpa2,D-Lys6,D-Ala10)-GnRH, the chicken GnRH antagonist MI-1892 (Ac-D-Trp1,3,D-Cpa2,Lys5,/beta-Asp(DEA)/6,Gln8,D-Al a10)-GnRH, and their copolymer conjugates were carried out on MCF-7 and MDA-MB-231 human breast tumors xenografted in immunosuppressed CBA/Ca HRIJ-T6 female mice and on MXT mouse mammary tumors in BDF1 mice. The P-X-1544 and P-X-1892 conjugates were prepared by coupling the GnRH antagonists to macromolecule copolymer through biodegradable spacers. MI-1544 and its conjugate had strong, whereas MI-1892 and its conjugate had slight, castration effect in rats. All of them showed selective antitumor activity. The conjugates, given daily, inhibited both types of xenografts by 42 to 49%. Their activity was stronger in MXT mammary tumor (72 to 61%). The in vivo effect of GnRH antagonists was largely increased by coupling them to nonbiodegradable macromolecule carriers of polyanionic character. P-X-1544 and P-X-1892 GnRH antagonist-macromolecule conjugates might become important therapeutic agents for the treatment of breast cancer.
AuthorsB Vincze, I Pályi, D Gaál, J Pató, M Móra, I Mezõ, I Teplán, J Seprõdi
JournalCancer detection and prevention (Cancer Detect Prev) Vol. 20 Issue 2 Pg. 153-9 ( 1996) ISSN: 0361-090X [Print] UNITED STATES
PMID8706041 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Antineoplastic Agents, Hormonal
  • Drug Carriers
  • Hormone Antagonists
  • MI 1892
  • P-X 1544
  • P-X 1892
  • Gonadotropin-Releasing Hormone
  • MI 1544
Topics
  • Animals
  • Antineoplastic Agents, Hormonal (therapeutic use)
  • Breast Neoplasms (drug therapy)
  • Disease Progression
  • Drug Carriers
  • Female
  • Gonadotropin-Releasing Hormone (analogs & derivatives, antagonists & inhibitors, pharmacology, therapeutic use)
  • Hormone Antagonists (therapeutic use)
  • Humans
  • Mammary Neoplasms, Experimental
  • Mice
  • Mice, Inbred CBA
  • Neoplasm Transplantation
  • Thymectomy
  • Transplantation, Heterologous

Join CureHunter, for free Research Interface BASIC access!

Take advantage of free CureHunter research engine access to explore the best drug and treatment options for any disease. Find out why thousands of doctors, pharma researchers and patient activists around the world use CureHunter every day.
Realize the full power of the drug-disease research network!


Choose Username:
Email:
Password:
Verify Password: