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 (US) |
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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 |
Keywords
- Breast cancer
- LH-RH receptors
- Targeted chemotherapeutic agents
ASJC Scopus subject areas
- Cancer Research
- Molecular Biology
- Oncology