Abstract
Naturally occurring isoforms of the decapeptide gonadotropin-releasing hormone (GnRH) share residues 1-4 and 9-10. lGnRH-III, the third isoform isolated in the sea lamprey has no endocrine effect in mammals but shows a direct antiproliferative effect on human breast, prostate and endometrial cancer cell lines. To investigate these features, residues 5-8 of lGnRH-III were systematically replaced with Ala. The ability of the synthetic analogs to interact with receptors on MDA-MB 231 human breast cancer cells and their effect on the growth of the same cell line were investigated. [Ala6]lGnRH- III and [Ala7]lGnRH-III have neither receptor binding nor antiproliferative activity. Replacement of His5 with Ala resulted in an analog that binds to the receptor but does not have antiproliferative activity. The results are in agreement with previous reports that modifications of Lys at position 8 are well tolerated.
| Original language | English |
|---|---|
| Pages (from-to) | 419-422 |
| Number of pages | 4 |
| Journal | Peptides |
| Volume | 26 |
| Issue number | 3 |
| DOIs | |
| State | Published - Mar 2005 |
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All Science Journal Classification (ASJC) codes
- Biochemistry
- Endocrinology
- Physiology
- Cellular and Molecular Neuroscience
Cite this
Importance of the central region of lamprey gonadotropin-releasing hormone III in the inhibition of breast cancer cell growth. / Herédi-Szabó, Krisztina; Lubke, Jeremiah; Toth, Geza; Murphy, Richard F.; Lovas, Sándor.
In: Peptides, Vol. 26, No. 3, 03.2005, p. 419-422.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Importance of the central region of lamprey gonadotropin-releasing hormone III in the inhibition of breast cancer cell growth
AU - Herédi-Szabó, Krisztina
AU - Lubke, Jeremiah
AU - Toth, Geza
AU - Murphy, Richard F.
AU - Lovas, Sándor
PY - 2005/3
Y1 - 2005/3
N2 - Naturally occurring isoforms of the decapeptide gonadotropin-releasing hormone (GnRH) share residues 1-4 and 9-10. lGnRH-III, the third isoform isolated in the sea lamprey has no endocrine effect in mammals but shows a direct antiproliferative effect on human breast, prostate and endometrial cancer cell lines. To investigate these features, residues 5-8 of lGnRH-III were systematically replaced with Ala. The ability of the synthetic analogs to interact with receptors on MDA-MB 231 human breast cancer cells and their effect on the growth of the same cell line were investigated. [Ala6]lGnRH- III and [Ala7]lGnRH-III have neither receptor binding nor antiproliferative activity. Replacement of His5 with Ala resulted in an analog that binds to the receptor but does not have antiproliferative activity. The results are in agreement with previous reports that modifications of Lys at position 8 are well tolerated.
AB - Naturally occurring isoforms of the decapeptide gonadotropin-releasing hormone (GnRH) share residues 1-4 and 9-10. lGnRH-III, the third isoform isolated in the sea lamprey has no endocrine effect in mammals but shows a direct antiproliferative effect on human breast, prostate and endometrial cancer cell lines. To investigate these features, residues 5-8 of lGnRH-III were systematically replaced with Ala. The ability of the synthetic analogs to interact with receptors on MDA-MB 231 human breast cancer cells and their effect on the growth of the same cell line were investigated. [Ala6]lGnRH- III and [Ala7]lGnRH-III have neither receptor binding nor antiproliferative activity. Replacement of His5 with Ala resulted in an analog that binds to the receptor but does not have antiproliferative activity. The results are in agreement with previous reports that modifications of Lys at position 8 are well tolerated.
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U2 - 10.1016/j.peptides.2004.10.007
DO - 10.1016/j.peptides.2004.10.007
M3 - Article
VL - 26
SP - 419
EP - 422
JO - Peptides
JF - Peptides
SN - 0196-9781
IS - 3
ER -