Lipoamino acid-modified GnRH analogs with receptor-mediated antiproliferative activity in prostate and ovarian cancer cells
نویسندگان
چکیده
Gonadotropin-releasing hormone (GnRH) analogs (e.g., triptorelin) are developed to treat hormone-dependent reproductive cancers. However, these lack a significant direct antitumor activity make them suitable for hormone-refractory In this study, we examined different biological properties of lipid-modified GnRH analogs, with/without D-amino acid substitution at position 6 in prostate and ovarian cancer cells. We revealed that the improved metabolic stability due lipid-modification played pivotal role enhancing receptor-mediated antiproliferative up 4.5-fold higher than triptorelin. Furthermore, comparable FSH release LH pituitary cells triptorelin was observed, indicating an specificity and/or binding affinity receptors. confirmed important sex steroids lipopeptides, which were contrasting The superior over commercial peptides renders promises developing new receptor ligands -refractory cancers, as well emerging targeting moieties delivery anticancer agents receptor-overexpressing
منابع مشابه
GnRH Glycolipids with In Vitro Gonadotropin Hormone Releasing Properties and Direct Antiproliferative Activity on Prostate and Ovarian Cancer Cells
متن کامل
Vanadium Complexes with Maltol and Deferiprone Ligands: Synthesis, Characterization and In vitro Antiproliferative Activity toward Different Cancer Cells
In a systematic effort to identify a potent antiproliferative agent, four complexes of vanadium containing maltol and deferiprone ligands were synthesized and evaluated for their cytotoxic activity against five human and animal cancer cell lines, including human breast cancer cells (MCF-7), human cervix epithelial carcinoma (HeLa), human colon cancer cell line (HT-29), human leukemia cell line ...
متن کاملNew Tripentone Analogs with Antiproliferative Activity.
Tripentones represent an interesting class of compounds due to their significant cytotoxicity against different human tumor cells in the submicro-nanomolar range. New tripentone analogs, in which a pyridine moiety replaces the thiophene ring originating the fused azaindole system endowed with anticancer activity viz 8H-thieno[2,3-b]pyrrolizinones, were efficiently synthesized in four steps with...
متن کاملType I gonadotropin-releasing hormone receptor mediates the antiproliferative effects of GnRH-II on prostate cancer cells.
BACKGROUND GnRH-II has been shown to exert a strong antiproliferative action on tumors of the female reproductive system. The data so far reported on the effects of GnRH-II on prostate cancer growth are controversial. Moreover, it is still unclear through which receptor [type I or type II GnRH-receptor (GnRH-R)] GnRH-II might modulate cancer cell proliferation. OBJECTIVE The objective of this...
متن کاملRole of gonadotropin-releasing hormone (GnRH) in ovarian cancer
The expression of GnRH (GnRH-I, LHRH) and its receptor as a part of an autocrine regulatory system of cell proliferation has been demonstrated in a number of human malignant tumors, including cancers of the ovary. The proliferation of human ovarian cancer cell lines is time- and dose-dependently reduced by GnRH and its superagonistic analogs. The classical GnRH receptor signal-transduction mech...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
ژورنال
عنوان ژورنال: Medicinal Chemistry Research
سال: 2021
ISSN: ['1554-8120', '1054-2523']
DOI: https://doi.org/10.1007/s00044-021-02755-0