Experimental therapy of human endometrial cancers with a targeted cytotoxic bombesin analog AN-215: Low induction of multidrug resistance proteins

Jörg B. Engel, Andrew V Schally, Gabor Halmos, Benjamin Baker, Attila Nagy, Gunhild Keller

Research output: Contribution to journalArticle

10 Citations (Scopus)

Abstract

In this study we have investigated the efficacy and toxicity of targeted cytotoxic bombesin (BN) analog AN-215 and its effects on the expression of three multidrug resistance proteins in experimental human endometrial cancers. Nude mice bearing HEC-1A, RL-95-2 and AN3CA tumours were treated with AN-215 and its cytotoxic radical (AN-201). The BN receptor expression in tumours was followed by RT-PCR analysis and radioligand binding assays. Expression of drug resistance proteins MDR-1, MRP-1 and BCRP were measured by realtime PCR. AN-215 significantly (P < 0.05) inhibited the growth of HEC-1A, RL-95-2 and AN3CA tumours while AN-201 was ineffective. The expression of BN receptors was demonstrated in all three tumour models. AN-215 caused a lower induction of MDR-1 in HEC-1A and RL-95-2 cancers than AN-201. MRP-1 and BCRP were not induced by AN-215 or AN-201. Thus, targeted chemotherapy with AN-215 powerfully inhibits the growth of human BN receptor-positive endometrial cancers.

Original languageEnglish
Pages (from-to)1824-1830
Number of pages7
JournalEuropean Journal of Cancer
Volume41
Issue number12
DOIs
StatePublished - Aug 1 2005
Externally publishedYes

Fingerprint

P-Glycoproteins
Bombesin
Investigational Therapies
Endometrial Neoplasms
Bombesin Receptors
Neoplasms
Polymerase Chain Reaction
Radioligand Assay
Growth
Drug Resistance
Nude Mice
AN 215
Drug Therapy
AN 204

Keywords

  • Bombesin/GRP receptor
  • Endometrial cancer
  • Multidrug resistance
  • Targeted chemotherapy
  • Targeted cytotoxic bombesin analog AN-215

ASJC Scopus subject areas

  • Cancer Research
  • Hematology
  • Oncology

Cite this

Experimental therapy of human endometrial cancers with a targeted cytotoxic bombesin analog AN-215 : Low induction of multidrug resistance proteins. / Engel, Jörg B.; Schally, Andrew V; Halmos, Gabor; Baker, Benjamin; Nagy, Attila; Keller, Gunhild.

In: European Journal of Cancer, Vol. 41, No. 12, 01.08.2005, p. 1824-1830.

Research output: Contribution to journalArticle

Engel, Jörg B. ; Schally, Andrew V ; Halmos, Gabor ; Baker, Benjamin ; Nagy, Attila ; Keller, Gunhild. / Experimental therapy of human endometrial cancers with a targeted cytotoxic bombesin analog AN-215 : Low induction of multidrug resistance proteins. In: European Journal of Cancer. 2005 ; Vol. 41, No. 12. pp. 1824-1830.
@article{0f65140fb24443a5ba3d6b36f77fe71c,
title = "Experimental therapy of human endometrial cancers with a targeted cytotoxic bombesin analog AN-215: Low induction of multidrug resistance proteins",
abstract = "In this study we have investigated the efficacy and toxicity of targeted cytotoxic bombesin (BN) analog AN-215 and its effects on the expression of three multidrug resistance proteins in experimental human endometrial cancers. Nude mice bearing HEC-1A, RL-95-2 and AN3CA tumours were treated with AN-215 and its cytotoxic radical (AN-201). The BN receptor expression in tumours was followed by RT-PCR analysis and radioligand binding assays. Expression of drug resistance proteins MDR-1, MRP-1 and BCRP were measured by realtime PCR. AN-215 significantly (P < 0.05) inhibited the growth of HEC-1A, RL-95-2 and AN3CA tumours while AN-201 was ineffective. The expression of BN receptors was demonstrated in all three tumour models. AN-215 caused a lower induction of MDR-1 in HEC-1A and RL-95-2 cancers than AN-201. MRP-1 and BCRP were not induced by AN-215 or AN-201. Thus, targeted chemotherapy with AN-215 powerfully inhibits the growth of human BN receptor-positive endometrial cancers.",
keywords = "Bombesin/GRP receptor, Endometrial cancer, Multidrug resistance, Targeted chemotherapy, Targeted cytotoxic bombesin analog AN-215",
author = "Engel, {J{\"o}rg B.} and Schally, {Andrew V} and Gabor Halmos and Benjamin Baker and Attila Nagy and Gunhild Keller",
year = "2005",
month = "8",
day = "1",
doi = "10.1016/j.ejca.2005.04.031",
language = "English",
volume = "41",
pages = "1824--1830",
journal = "European Journal of Cancer",
issn = "0959-8049",
publisher = "Elsevier Limited",
number = "12",

}

TY - JOUR

T1 - Experimental therapy of human endometrial cancers with a targeted cytotoxic bombesin analog AN-215

T2 - Low induction of multidrug resistance proteins

AU - Engel, Jörg B.

AU - Schally, Andrew V

AU - Halmos, Gabor

AU - Baker, Benjamin

AU - Nagy, Attila

AU - Keller, Gunhild

PY - 2005/8/1

Y1 - 2005/8/1

N2 - In this study we have investigated the efficacy and toxicity of targeted cytotoxic bombesin (BN) analog AN-215 and its effects on the expression of three multidrug resistance proteins in experimental human endometrial cancers. Nude mice bearing HEC-1A, RL-95-2 and AN3CA tumours were treated with AN-215 and its cytotoxic radical (AN-201). The BN receptor expression in tumours was followed by RT-PCR analysis and radioligand binding assays. Expression of drug resistance proteins MDR-1, MRP-1 and BCRP were measured by realtime PCR. AN-215 significantly (P < 0.05) inhibited the growth of HEC-1A, RL-95-2 and AN3CA tumours while AN-201 was ineffective. The expression of BN receptors was demonstrated in all three tumour models. AN-215 caused a lower induction of MDR-1 in HEC-1A and RL-95-2 cancers than AN-201. MRP-1 and BCRP were not induced by AN-215 or AN-201. Thus, targeted chemotherapy with AN-215 powerfully inhibits the growth of human BN receptor-positive endometrial cancers.

AB - In this study we have investigated the efficacy and toxicity of targeted cytotoxic bombesin (BN) analog AN-215 and its effects on the expression of three multidrug resistance proteins in experimental human endometrial cancers. Nude mice bearing HEC-1A, RL-95-2 and AN3CA tumours were treated with AN-215 and its cytotoxic radical (AN-201). The BN receptor expression in tumours was followed by RT-PCR analysis and radioligand binding assays. Expression of drug resistance proteins MDR-1, MRP-1 and BCRP were measured by realtime PCR. AN-215 significantly (P < 0.05) inhibited the growth of HEC-1A, RL-95-2 and AN3CA tumours while AN-201 was ineffective. The expression of BN receptors was demonstrated in all three tumour models. AN-215 caused a lower induction of MDR-1 in HEC-1A and RL-95-2 cancers than AN-201. MRP-1 and BCRP were not induced by AN-215 or AN-201. Thus, targeted chemotherapy with AN-215 powerfully inhibits the growth of human BN receptor-positive endometrial cancers.

KW - Bombesin/GRP receptor

KW - Endometrial cancer

KW - Multidrug resistance

KW - Targeted chemotherapy

KW - Targeted cytotoxic bombesin analog AN-215

UR - http://www.scopus.com/inward/record.url?scp=23644432193&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=23644432193&partnerID=8YFLogxK

U2 - 10.1016/j.ejca.2005.04.031

DO - 10.1016/j.ejca.2005.04.031

M3 - Article

C2 - 16051478

AN - SCOPUS:23644432193

VL - 41

SP - 1824

EP - 1830

JO - European Journal of Cancer

JF - European Journal of Cancer

SN - 0959-8049

IS - 12

ER -