Effective treatment of experimental U-87MG human glioblastoma in nude mice with a targeted cytotoxic bombesin analogue, AN-215

Some brain tumours, such as glioblastomas express high levels of receptors for bombesin/gastrin releasing peptide. We investigated whether bombesin/gastrin releasing peptide receptors found in glioblastoma cell lines can be utilised for targeting of a cytotoxic bombesin analogue, AN-215 consisting o...

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Bibliographic Details
Published in:British journal of cancer 2002-04, Vol.86 (8), p.1322-1327
Main Authors: Szereday, Z, Schally, A V, Nagy, A, Plonowski, A, Bajo, A M, Halmos, G, Szepeshazi, K, Groot, K
Format: Article
Language:English
Subjects:
Animals
Antineoplastic agents
Biological and medical sciences
Biomedical and Life Sciences
Biomedicine
Bombesin - adverse effects
Bombesin - analogs & derivatives
Bombesin - pharmacology
Bombesin - therapeutic use
Brain cancer
Brain research
Cancer Research
Cancer therapies
Cell Division - drug effects
Chemotherapy
Cytotoxicity
Doxorubicin - adverse effects
Doxorubicin - analogs & derivatives
Doxorubicin - pharmacology
Doxorubicin - therapeutic use
Drug dosages
Drug Resistance
Epidemiology
Experimental Therapeutics
Glioblastoma - drug therapy
Glioblastoma - genetics
Glioblastoma - pathology
Humans
Medical research
Medical sciences
Mice
Mice, Nude
Molecular Medicine
Neoplasm Transplantation
Oncology
Pharmacology. Drug treatments
Polypeptides
R&D
Receptors, Bombesin - antagonists & inhibitors
Receptors, Bombesin - genetics
Research & development
Reverse Transcriptase Polymerase Chain Reaction
RNA, Messenger - genetics
RNA, Messenger - metabolism
Tumor Cells, Cultured
Tumors
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Summary:Some brain tumours, such as glioblastomas express high levels of receptors for bombesin/gastrin releasing peptide. We investigated whether bombesin/gastrin releasing peptide receptors found in glioblastoma cell lines can be utilised for targeting of a cytotoxic bombesin analogue, AN-215 consisting of a potent derivative of doxorubicin, 2-pyrrolino-doxorubicin (AN-201) linked to a bombesin-like peptide carrier. This study reports the effect of AN-215 on the growth of U-87MG human glioblastomas xenografted into nude mice. High affinity binding of AN-215 to U-87MG tumours was characterised by an IC 50 value of 4.0±0.1 n M , as determined by radioreceptor assays. mRNA analyses revealed the presence of mRNA for BN receptor subtypes 1 and 2. Treatment with AN-215 significantly ( P
ISSN:0007-0920
1532-1827
DOI:10.1038/sj.bjc.6600235