Based on these in vitro data, GPR173 likely constrains the pro-proliferative, pro-migratory, and pro-invasive phenotypes of TNBC cells by enhancing GnRHR signaling. These findings highlight GnRHR and GPR173 as potential therapeutic targets for TNBC.
These findings suggest that GnRHR expression in mast cells promotes their supportive role in pregnancy establishment by increasing the LIF, MMP-9, and CXCL16 productions, recruiting trophoblasts and NK cells.
This restored gene expression, and preserved ovarian structure. These results highlight the potential of HSP as a protective agent against CP-induced ovarian damage and infertility, offering promising implications for female fertility preservation during chemotherapy.
9 months ago
Preclinical • Journal
|
TP53 (Tumor protein P53) • NFKB1 (Nuclear factor of kappa light polypeptide gene enhancer in B-cells 1) • GNRHR (Gonadotropin Releasing Hormone Receptor) • CDKN1A (Cyclin-dependent kinase inhibitor 1A)
Finally, we demonstrated significant silencing of CSNK2A1, an oncogene overexpressed in ovarian cancer, in the ovarian cancer cell line OVCAR3. Our findings establish the use of a tandem peptide with cell-targeting and membrane-disruptive abilities as a delivery platform for nucleic acid therapies.
This study highlights the advantages of easy customization of payloads and targeting peptides, requiring only a simple coating process that doesn't need specialized expertise. Its flexibility and efficiency enhance the potential for precision therapies, making it ideal for translational applications in treating reproductive-related cancers, GnRH-associated diseases, and other conditions.
Development of functional imaging targeting aberrant GPCRs should be useful for identification and for specific therapies of this wide spectrum of tumours. The aim of this review is to show that the regulation of endocrine tumours by aberrant GPCR is not restricted to cortisol-secreting adrenal lesions, but also occurs in tumours of several other organs.
over 1 year ago
Review • Journal
|
SSTR (Somatostatin Receptor) • GNRHR (Gonadotropin Releasing Hormone Receptor) • SSTR5 (Somatostatin Receptor 5) • GPRC6A (G Protein-Coupled Receptor Class C Group 6 Member A) • DRD2 (Dopamine Receptor D2)
The increased GH response to LHRH is associated with the gonadotroph-related characteristics. This response may reflect the biological characteristics of somatotroph tumors.
Administration of kaempferol alone or with vitamin E can mitigate lead acetate-induced testicular toxicity in rats via its antioxidant and anti-inflammatory properties. The current research is the first to demonstrate that kaempferol can exert a preventive role in testicular dysfunction.
Their in vitro binding affinities range from 0.06 to 3.42 nM, with six of them (con2-con7) demonstrating higher affinities for GnRH than the established drug leuprolide (0.64 nM). Among the mitoxantrone based GnRH conjugates, con3 and con7 show the highest affinities at 0.07 and 0.06 nM, respectively, while the disulfide bond present in the conjugates is found to be readily reduced by the thioredoxin (Trx) system. These findings are promising for further pharmacological evaluation of the synthesized conjugates with the prospect of performing future clinical studies.
over 2 years ago
Journal
|
GNRHR (Gonadotropin Releasing Hormone Receptor)
|
mitoxantrone • leuprolide acetate for depot suspension
On the contrary, its metabolite, GnRH-(1-5), behaves divergently from its parental peptide through putative orphan G-protein coupled receptor (oGPCR), GPR101. In this review, we will focus on the potential roles of GnRH-(1-5) in the periphery with an emphasis on its effects on endometrial cancer progression.
Another recent approach based on this knowledge was the use of GnRH peptides for developing specific targeted therapies, improving the delivery and accumulation of drugs in tumoral cells, and decreasing most side effects of current treatments. In this review, we discuss the conventional uses of GnRH analogs, together with the recent advances in GnRH-based drug delivery for ovarian, breast, and prostatic cancer cells.