Gonadotropin-releasing hormone receptors as molecular therapeutic targets in prostate cancer: Current options and emerging strategies

2013 ◽  
Vol 39 (6) ◽  
pp. 647-663 ◽  
Author(s):  
Patrizia Limonta ◽  
Marilena Manea
Keyword(s):  
Prostate Cancer ◽  
Hormone Receptors ◽  
Therapeutic Targets ◽  
Gonadotropin Releasing Hormone ◽  
Releasing Hormone ◽  
Molecular Therapeutic ◽  
Molecular Therapeutic Targets

scholarly journals Gonadotropin-Releasing Hormone Receptors in Prostate Cancer: Molecular Aspects and Biological Functions

2020 ◽  
Vol 21 (24) ◽  
pp. 9511
Author(s):  
Fabrizio Fontana ◽  
Monica Marzagalli ◽  
Marina Montagnani Marelli ◽  
Michela Raimondi ◽  
Roberta Moretti ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Clinical Trials ◽  
Hormone Receptors ◽  
Early Stage ◽  
Disease Free Survival ◽  
Gonadotropin Releasing Hormone ◽  
Gnrh Agonists ◽  
Castration Resistant Prostate Cancer ◽  
Releasing Hormone ◽  
Reproductive Axis

Pituitary Gonadotropin-Releasing Hormone receptors (GnRH-R) mediate the activity of the hypothalamic decapeptide GnRH, thus playing a key role in the regulation of the reproductive axis. Early-stage prostate cancer (PCa) is dependent on serum androgen levels, and androgen-deprivation therapy (ADT), based on GnRH agonists and antagonists, represents the standard therapeutic approach for PCa patients. Unfortunately, the tumor often progresses towards the more aggressive castration-resistant prostate cancer (CRPC) stage. GnRH receptors are also expressed in CRPC tissues, where their binding to both GnRH agonists and antagonists is associated with significant antiproliferative/proapoptotic, antimetastatic and antiangiogenic effects, mediated by the Gαi/cAMP signaling cascade. GnRH agonists and antagonists are now considered as an effective therapeutic strategy for CRPC patients with many clinical trials demonstrating that the combined use of these drugs with standard therapies (i.e., docetaxel, enzalutamide, abiraterone) significantly improves disease-free survival. In this context, GnRH-based bioconjugates (cytotoxic drugs covalently linked to a GnRH-based decapeptide) have been recently developed. The rationale of this treatment is that the GnRH peptide selectively binds to its receptors, delivering the cytotoxic drug to CRPC cells while sparing nontumor cells. Some of these compounds have already entered clinical trials.

scholarly journals Endocrine and molecular milieus of ovarian follicles are diversely affected by human chorionic gonadotropin and gonadotropin-releasing hormone in prepubertal and mature gilts

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Adam J. Ziecik ◽  
Jan Klos ◽  
Katarzyna Gromadzka-Hliwa ◽  
Mariola A. Dietrich ◽  
Mariola Slowinska ◽  
...  
Keyword(s):  
Chorionic Gonadotropin ◽  
Human Chorionic Gonadotropin ◽  
Hormone Receptors ◽  
Cell Function ◽  
Ovarian Follicle ◽  
Molecular Transport ◽  
Gonadotropin Releasing Hormone ◽  
Matrix Remodeling ◽  
Releasing Hormone ◽  
Serum Gonadotropin

AbstractDifferent strategies are used to meet optimal reproductive performance or manage reproductive health. Although exogenous human chorionic gonadotropin (hCG) and gonadotropin-releasing hormone (GnRH) agonists (A) are commonly used to trigger ovulation in estrous cycle synchronization, little is known about their effect on the ovarian follicle. Here, we explored whether hCG- and GnRH-A-induced native luteinizing hormone (LH) can affect the endocrine and molecular milieus of ovarian preovulatory follicles in pigs at different stages of sexual development. We collected ovaries 30 h after hCG/GnRH-A administration from altrenogest and pregnant mare serum gonadotropin (eCG)-primed prepubertal and sexually mature gilts. Several endocrine and molecular alternations were indicated, including broad hormonal trigger-induced changes in follicular fluid steroid hormones and prostaglandin levels. However, sexual maturity affected only estradiol levels. Trigger- and/or maturity-dependent changes in the abundance of hormone receptors (FSHR and LHCGR) and proteins associated with lipid metabolism and steroidogenesis (e.g., STAR, HSD3B1, and CYP11A1), prostaglandin synthesis (PTGS2 and PTGFS), extracellular matrix remodeling (MMP1 and TIMP1), protein folding (HSPs), molecular transport (TF), and cell function and survival (e.g., VIM) were observed. These data revealed different endocrine properties of exogenous and endogenous gonadotropins, with a potent progestational/androgenic role of hCG and estrogenic/pro-developmental function of LH.

Demonstration of gonadotropin releasing-hormone receptors on gonadotrophs and somatotrophs of the goldfish: an electron microscope study

1991 ◽  
Vol 36 (3) ◽  
pp. 369-378 ◽  
Author(s):  
Harry Cook ◽  
John W. Berkenbosch ◽  
Mark J. Fernhout ◽  
Kei-Li Yu ◽  
Richard E. Peter ◽  
...  
Keyword(s):  
Electron Microscope ◽  
Microscope Study ◽  
Electron Microscope Study ◽  
Hormone Receptors ◽  
Gonadotropin Releasing Hormone ◽  
Releasing Hormone
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