A conjugate of doxorubicin and an analog of Luteinizing Hormone-Releasing Hormone shows increased efficacy against oral and laryngeal cancers.

Linda J. Krebs, Xiaopeng Wang, Attila Nagy, Andrew V Schally, Paras N. Prasad, Charles Liebow

Research output: Contribution to journalArticle

18 Citations (Scopus)

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 languageEnglish
Pages (from-to)657-663
Number of pages7
JournalOral Oncology
Volume38
Issue number7
StatePublished - Oct 1 2002
Externally publishedYes

Fingerprint

Laryngeal Neoplasms
Mouth Neoplasms
Gonadotropin-Releasing Hormone
Doxorubicin
LHRH Receptors
Epidermal Growth Factor
KB Cells
Neoplasms
lysine(6)-doxorubicin LHRH
Photons
Confocal Microscopy
Up-Regulation
Carcinoma
Cell Line

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 journalArticle

Krebs, Linda J. ; Wang, Xiaopeng ; Nagy, Attila ; Schally, Andrew V ; Prasad, Paras N. ; Liebow, Charles. / A conjugate of doxorubicin and an analog of Luteinizing Hormone-Releasing Hormone shows increased efficacy against oral and laryngeal cancers. In: Oral Oncology. 2002 ; Vol. 38, No. 7. pp. 657-663.
@article{21f6c95d5ed741b4b3f35ab938602c1e,
title = "A conjugate of doxorubicin and an analog of Luteinizing Hormone-Releasing Hormone shows increased efficacy against oral and laryngeal cancers.",
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.",
author = "Krebs, {Linda J.} and Xiaopeng Wang and Attila Nagy and Schally, {Andrew V} and Prasad, {Paras N.} and Charles Liebow",
year = "2002",
month = "10",
day = "1",
language = "English",
volume = "38",
pages = "657--663",
journal = "Oral Oncology",
issn = "1368-8375",
publisher = "Elsevier Limited",
number = "7",

}

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 -