Abstract
A doxorubicin and [D-Lys(6)]Luteinizing Hormone-Releasing Hormone (LH-RH) conjugate, AN-152, was designed to target LH-RH receptor positive cells. AN-152 is more potent against a specific group of cancers than doxorubicin and has less peripheral toxicity. This therapy is potentially efficacious against many other types of malignancies. Here, AN-152 was tested on oral (KB) and laryngeal (HEp-2) carcinoma cells. LH-RH receptor presence was demonstrated by displacement binding assays. Cells were treated with 10 nM EGF or left untreated, then exposed to 0-10 microM AN-152. Cytotoxicity was assessed by MTT assay to determine ED(50) values. AN-152 association with the cells was monitored using two-photon laser scanning microscopy. AN-152 was more potent than doxorubicin in both KB and HEp-2 cell lines (P<0.05). Up-regulation of LH-RH receptors by epidermal growth factor (EGF) increased the entry and potency of AN-152 in KB cells, but not in HEp-2 cells. This novel approach may be effective against a variety of cancers.
| Original language | English |
|---|---|
| Pages (from-to) | 657-663 |
| Number of pages | 7 |
| Journal | Oral Oncology |
| Volume | 38 |
| Issue number | 7 |
| State | Published - Oct 1 2002 |
| Externally published | Yes |
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ASJC Scopus subject areas
- Oncology
Cite this
A conjugate of doxorubicin and an analog of Luteinizing Hormone-Releasing Hormone shows increased efficacy against oral and laryngeal cancers. / Krebs, Linda J.; Wang, Xiaopeng; Nagy, Attila; Schally, Andrew V; Prasad, Paras N.; Liebow, Charles.
In: Oral Oncology, Vol. 38, No. 7, 01.10.2002, p. 657-663.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - A conjugate of doxorubicin and an analog of Luteinizing Hormone-Releasing Hormone shows increased efficacy against oral and laryngeal cancers.
AU - Krebs, Linda J.
AU - Wang, Xiaopeng
AU - Nagy, Attila
AU - Schally, Andrew V
AU - Prasad, Paras N.
AU - Liebow, Charles
PY - 2002/10/1
Y1 - 2002/10/1
N2 - A doxorubicin and [D-Lys(6)]Luteinizing Hormone-Releasing Hormone (LH-RH) conjugate, AN-152, was designed to target LH-RH receptor positive cells. AN-152 is more potent against a specific group of cancers than doxorubicin and has less peripheral toxicity. This therapy is potentially efficacious against many other types of malignancies. Here, AN-152 was tested on oral (KB) and laryngeal (HEp-2) carcinoma cells. LH-RH receptor presence was demonstrated by displacement binding assays. Cells were treated with 10 nM EGF or left untreated, then exposed to 0-10 microM AN-152. Cytotoxicity was assessed by MTT assay to determine ED(50) values. AN-152 association with the cells was monitored using two-photon laser scanning microscopy. AN-152 was more potent than doxorubicin in both KB and HEp-2 cell lines (P<0.05). Up-regulation of LH-RH receptors by epidermal growth factor (EGF) increased the entry and potency of AN-152 in KB cells, but not in HEp-2 cells. This novel approach may be effective against a variety of cancers.
AB - A doxorubicin and [D-Lys(6)]Luteinizing Hormone-Releasing Hormone (LH-RH) conjugate, AN-152, was designed to target LH-RH receptor positive cells. AN-152 is more potent against a specific group of cancers than doxorubicin and has less peripheral toxicity. This therapy is potentially efficacious against many other types of malignancies. Here, AN-152 was tested on oral (KB) and laryngeal (HEp-2) carcinoma cells. LH-RH receptor presence was demonstrated by displacement binding assays. Cells were treated with 10 nM EGF or left untreated, then exposed to 0-10 microM AN-152. Cytotoxicity was assessed by MTT assay to determine ED(50) values. AN-152 association with the cells was monitored using two-photon laser scanning microscopy. AN-152 was more potent than doxorubicin in both KB and HEp-2 cell lines (P<0.05). Up-regulation of LH-RH receptors by epidermal growth factor (EGF) increased the entry and potency of AN-152 in KB cells, but not in HEp-2 cells. This novel approach may be effective against a variety of cancers.
UR - http://www.scopus.com/inward/record.url?scp=0036781141&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=0036781141&partnerID=8YFLogxK
M3 - Article
C2 - 12353491
AN - SCOPUS:0036781141
VL - 38
SP - 657
EP - 663
JO - Oral Oncology
JF - Oral Oncology
SN - 1368-8375
IS - 7
ER -