Effect of luteinizing hormone-releasing hormone analogs containing cytotoxic radicals on growth of estrogen-independent MXT mouse mammary carcinoma in vivo.

Abstract	Cytotoxic luteinizing hormone-releasing hormone (LH-RH) analogs, AJ-004 (agonist [D-Lys6]LH-RH linked to methotrexate (MTX)), T-98 ([D-Lys6]LH-RH coupled to glutaryl-2-(hydroxymethyl)anthraquinone) (G-HMAQ) and T-121/B (antagonist containing two residues of G-HMAQ) were tested in female BDF1 mice bearing MXT ((3.2)/Ovex) estrogen-independent mammary tumors. All three cytotoxic LH-RH analogs, administered from Alzet Osmotic Minipumps for 3 weeks, produced a significant inhibition of tumor growth. The effects of T-98 and T-121/B were superior to those obtained by treatment with equimolar doses of cytotoxic moiety anthraquinone or the LH-RH carrier alone. We assume that cytotoxic LH-RH analogs have a combined hormonal and cytotoxic activity with a reduced toxicity after administration in vivo. This is the first demonstration of in vivo tumor inhibition by targeted LH-RH analogs bearing cytotoxic radicals.
Authors	K Szepeshazi, A V Schally, A Juhasz, A Nagy, T Janaky
Journal	Anti-cancer drugs (Anticancer Drugs) Vol. 3 Issue 2 Pg. 109-16 (Apr 1992) ISSN: 0959-4973 [Print] England
PMID	1388062 (Publication Type: Journal Article, Research Support, U.S. Gov't, Non-P.H.S., Research Support, U.S. Gov't, P.H.S.)
Chemical References	Anthraquinones Receptors, LH Triptorelin Pamoate glutaryl-2-(hydroxymethyl)anthraquinone Gonadotropin-Releasing Hormone Luteinizing Hormone Growth Hormone Methotrexate
Topics	Amino Acid Sequence Animals Anthraquinones (administration & dosage, pharmacology) Binding Sites Body Weight (drug effects) Cell Division (drug effects) Female Gonadotropin-Releasing Hormone (administration & dosage, analogs & derivatives, antagonists & inhibitors, pharmacology) Growth Hormone (blood) Kinetics Luteinizing Hormone (blood) Mammary Neoplasms, Experimental (drug therapy, pathology) Methotrexate (administration & dosage, pharmacology) Mice Mice, Inbred Strains Molecular Sequence Data Ovary (anatomy & histology) Receptors, LH (metabolism) Triptorelin Pamoate Uterus (anatomy & histology)

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 graph!