Abstract
Recently, we developed two new cytotoxic analogs of luteinizing hormone-releasing hormone (LH-RH), AN-152 in which doxorubicin (DOX) is linked to [D-Lys6]LH-RH, and AN-207 which consists of 2-pyrrolino-DOX coupled to [D-Lys6]LH-RH. In this study, we examined binding of AN-152 and AN-207 to membranes of human breast cancer specimens and MCF-7 and MDA-MB-231 human breast cancer lines. Both cytotoxic analogs displayed IC50 values in the nanomolar concentration range (IC50=2-13 nM). Using radioligand binding studies, we characterized the receptors for LH-RH on membranes of breast cancers. In addition, the expression of mRNA for LH-RH receptors in MCF-7 and MDA-MB-231 cell lines was demonstrated by reverse transcription-polymerase chain reaction (RT-PCR). These highly active cytotoxic analogs of LH-RH have been designed as targeted chemotherapeutic agents for the treatment of various cancers expressing receptors for LH-RH. Copyright (C) 1999.
| Original language | English |
|---|---|
| Pages (from-to) | 129-136 |
| Number of pages | 8 |
| Journal | Cancer Letters |
| Volume | 136 |
| Issue number | 2 |
| DOIs | |
| State | Published - Mar 1 1999 |
| Externally published | Yes |
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Keywords
- Breast cancer
- LH-RH receptors
- Targeted chemotherapeutic agents
ASJC Scopus subject areas
- Cancer Research
- Molecular Biology
- Oncology
Cite this
Cytotoxic analogs of luteinizing hormone-releasing hormone bind with high affinity to human breast cancers. / Halmos, Gabor; Nagy, Attila; Lamharzi, Najib; Schally, Andrew V.
In: Cancer Letters, Vol. 136, No. 2, 01.03.1999, p. 129-136.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Cytotoxic analogs of luteinizing hormone-releasing hormone bind with high affinity to human breast cancers
AU - Halmos, Gabor
AU - Nagy, Attila
AU - Lamharzi, Najib
AU - Schally, Andrew V
PY - 1999/3/1
Y1 - 1999/3/1
N2 - Recently, we developed two new cytotoxic analogs of luteinizing hormone-releasing hormone (LH-RH), AN-152 in which doxorubicin (DOX) is linked to [D-Lys6]LH-RH, and AN-207 which consists of 2-pyrrolino-DOX coupled to [D-Lys6]LH-RH. In this study, we examined binding of AN-152 and AN-207 to membranes of human breast cancer specimens and MCF-7 and MDA-MB-231 human breast cancer lines. Both cytotoxic analogs displayed IC50 values in the nanomolar concentration range (IC50=2-13 nM). Using radioligand binding studies, we characterized the receptors for LH-RH on membranes of breast cancers. In addition, the expression of mRNA for LH-RH receptors in MCF-7 and MDA-MB-231 cell lines was demonstrated by reverse transcription-polymerase chain reaction (RT-PCR). These highly active cytotoxic analogs of LH-RH have been designed as targeted chemotherapeutic agents for the treatment of various cancers expressing receptors for LH-RH. Copyright (C) 1999.
AB - Recently, we developed two new cytotoxic analogs of luteinizing hormone-releasing hormone (LH-RH), AN-152 in which doxorubicin (DOX) is linked to [D-Lys6]LH-RH, and AN-207 which consists of 2-pyrrolino-DOX coupled to [D-Lys6]LH-RH. In this study, we examined binding of AN-152 and AN-207 to membranes of human breast cancer specimens and MCF-7 and MDA-MB-231 human breast cancer lines. Both cytotoxic analogs displayed IC50 values in the nanomolar concentration range (IC50=2-13 nM). Using radioligand binding studies, we characterized the receptors for LH-RH on membranes of breast cancers. In addition, the expression of mRNA for LH-RH receptors in MCF-7 and MDA-MB-231 cell lines was demonstrated by reverse transcription-polymerase chain reaction (RT-PCR). These highly active cytotoxic analogs of LH-RH have been designed as targeted chemotherapeutic agents for the treatment of various cancers expressing receptors for LH-RH. Copyright (C) 1999.
KW - Breast cancer
KW - LH-RH receptors
KW - Targeted chemotherapeutic agents
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UR - http://www.scopus.com/inward/citedby.url?scp=0032935902&partnerID=8YFLogxK
U2 - 10.1016/S0304-3835(98)00316-4
DO - 10.1016/S0304-3835(98)00316-4
M3 - Article
C2 - 10355741
AN - SCOPUS:0032935902
VL - 136
SP - 129
EP - 136
JO - Cancer Letters
JF - Cancer Letters
SN - 0304-3835
IS - 2
ER -