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rdf:type |
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lifeskim:mentions |
umls-concept:C0005919,
umls-concept:C0006142,
umls-concept:C0033684,
umls-concept:C0086418,
umls-concept:C0205251,
umls-concept:C0205263,
umls-concept:C0242640,
umls-concept:C0243071,
umls-concept:C0599894,
umls-concept:C0962326,
umls-concept:C1511636,
umls-concept:C1517004,
umls-concept:C1521840
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pubmed:issue |
4
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pubmed:dateCreated |
2005-12-2
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pubmed:abstractText |
The cytotoxic analog of bombesin (BN)/gastrin releasing peptide (GRP) AN-215 consisting of 2-pyrrolinodoxorubicin (AN-201), a superactive derivative of doxorubicin linked to a bombesin analog carrier, displays a high affinity to BN/GRP receptors and can be targeted to tumors that express these receptors. We evaluated the antitumor effect and the toxicity of AN-215 in 5 human breast cancer cell lines xenografted into nude mice. In addition, we measured the mRNA expression of multi drug resistance protein 1 (MDR-1), multi drug resistance related protein 1 (MRP-1) and breast cancer resistance protein (BCRP) by real-time PCR analysis after treatment with AN-215. All five cell lines expressed BN/GRP receptors, and AN-215 significantly (P < 0.05) inhibited tumor growth in all models, while its cytotoxic radical AN-201 had no significant effect in four models. In MX-1 tumors, AN-201 had a significantly weaker antitumor effect than AN-215. The effect of AN-215 was nullified by a blockade of BN/GRP receptors with a bombesin antagonist. Low or no induction of MDR-1, MRP-1 and BCRP occurred after treatment with AN-215. In conclusion, targeted chemotherapy with the cytotoxic BN/GRP analog AN-215 strongly inhibits breast cancers that express BN/GRP receptors and might provide a new treatment modality for mammary carcinoma.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/ABCG2 protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/AN 215,
http://linkedlifedata.com/resource/pubmed/chemical/ATP-Binding Cassette Transporters,
http://linkedlifedata.com/resource/pubmed/chemical/Antineoplastic Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Bombesin,
http://linkedlifedata.com/resource/pubmed/chemical/Doxorubicin,
http://linkedlifedata.com/resource/pubmed/chemical/Multidrug Resistance-Associated...,
http://linkedlifedata.com/resource/pubmed/chemical/Neoplasm Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/P-Glycoprotein,
http://linkedlifedata.com/resource/pubmed/chemical/RNA, Messenger,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Bombesin,
http://linkedlifedata.com/resource/pubmed/chemical/multidrug resistance-associated...
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pubmed:status |
MEDLINE
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pubmed:month |
Dec
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pubmed:issn |
1351-0088
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:volume |
12
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
999-1009
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:16322338-ATP-Binding Cassette Transporters,
pubmed-meshheading:16322338-Animals,
pubmed-meshheading:16322338-Antineoplastic Agents,
pubmed-meshheading:16322338-Bombesin,
pubmed-meshheading:16322338-Breast Neoplasms,
pubmed-meshheading:16322338-Doxorubicin,
pubmed-meshheading:16322338-Drug Resistance, Multiple,
pubmed-meshheading:16322338-Female,
pubmed-meshheading:16322338-Humans,
pubmed-meshheading:16322338-Mice,
pubmed-meshheading:16322338-Mice, Nude,
pubmed-meshheading:16322338-Multidrug Resistance-Associated Proteins,
pubmed-meshheading:16322338-Neoplasm Proteins,
pubmed-meshheading:16322338-P-Glycoprotein,
pubmed-meshheading:16322338-RNA, Messenger,
pubmed-meshheading:16322338-Receptors, Bombesin,
pubmed-meshheading:16322338-Up-Regulation,
pubmed-meshheading:16322338-Xenograft Model Antitumor Assays
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pubmed:year |
2005
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pubmed:articleTitle |
Targeted cytotoxic bombesin analog AN-215 effectively inhibits experimental human breast cancers with a low induction of multi-drug resistance proteins.
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pubmed:affiliation |
Endocrine, Polypeptide and Cancer Institute, Veterans Affairs Medical Center and Section of Experimental Medicine, Department of Medicine, Tulane University School of Medicine, New Orleans, Louisiana 70112, USA.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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