fsh-α

MHY1485 is an mTOR activator that is cell-permeable. MHY1485 inhibits autophagosome and lysosome fusion, leading to accumulation of LC3II proteins and increased autophagosomes, thereby inhibiting cellular autophagy.

Relugolix (RVT-601) is an orally available, non-peptide gonadotropin-releasing hormone (GnRH or luteinizing hormone-releasing hormone (LHRH)) antagonist, with potential antineoplastic activity. Relugolix competitively binds to and blocks the GnRH receptor in the anterior pituitary gland, which both prevents GnRH binding to the GnRH receptor and inhibits the secretion and release of both luteinizing hormone (LH) and follicle stimulating hormone (FSH). In males, the inhibition of LH secretion prevents the release of testosterone from Leydig cells in the testes. Since testosterone is required to sustain prostate growth, reducing testosterone levels may inhibit hormone-dependent prostate cancer cell proliferation.

Cyclofenil is an estrogen antagonist, has anti-dengue-virus activity

Histrelin (Supprelin LA) acetate is a nonapeptide analog of gonadotropin-releasing hormone (GnRH) with added potency. It is considered a GnRH agonist. Histrelin is used in the treatment of hormone-sensitive cancers of the prostate in men and uterine fibroids in women.

FSH receptor antagonist 1 (compound 10) is a potent antagonist of the G(s) protein-coupled human follicle-stimulating hormone (FSH) receptor. It exhibits an IC50 value of 28 nM in cell lines expressing the human FSH receptor. This compound significantly inhibits follicle growth and ovulation in in vitro mouse models.

FSH receptor-binding inhibitor fragment (bi-10) is a potent antagonist that inhibits the binding of follicle-stimulating hormone (FSH) to its receptor (FSHR), modifying FSH activity at the receptor level. It suppresses ovulation and induces follicular atresia in mice. Furthermore, this compound holds potential for curbing ovarian cancer carcinogenesis by reducing the overexpression of FSHR and estrogen receptor beta (ERβ) in the ovaries [1].

ML224 (NCGC00242364) is a TSHR antagonist for the treatment of Graves' orbital disease and Graves' hyperthyroidism.

FSHR agonist 1, an allosteric agonist of the follicle-stimulating hormone receptor (FSHR), exhibits high affinity, with a pEC50 of 7.72. It forms extensive interactions with the transmembrane domain (TMD) to directly activate FSHR.

hFSH-β-(33-53) TFA, a thiol-containing peptide representing the second follicle-stimulating hormone receptor (FSHR) binding domain, acts as an FSHR antagonist, preventing FSH from binding to its receptor and partially promoting estradiol synthesis in Sertoli cells [1] [2] [3].