Hormone Antagonists

Luteinizing hormone-releasing hormone antagonists.

BACKGROUND Luteinizing hormone-releasing hormone (LH-RH) plays a central role in the vertebrate reproduction by regulating gonadal activity. Based on its binding to pituitary LH-RH receptors, as well as to LH-RH receptors expressed on cancer cells, LH-RH agonists and antagonists have been developed for different therapeutic applications. OBJECTIVE/METHOD Here we give an overview of the most r...

Calcium antagonists and hormone release.

Antitumorigenic actions of growth hormone-releasing hormone antagonists.

I a recent issue of PNAS, Kiaris et al. (1) reported that JV-1-36, a growth hormone-releasing hormone (GHRH) receptor antagonist, dramatically suppresses the proliferation of human small lung cell carcinoma cell lines grown in athymic nude mice and in culture. The antitumorigenic action of JV-1-36 is consistent with previous reports from the same laboratory demonstrating the effectiveness of th...

Effects of growth hormone antagonists on 3T3-F442A preadipocyte differentiation.

We have previously shown that a bovine (b) GH antagonist, bGH-M8, which possesses three amino acid substitutions in its third alpha-helix, inhibits mouse 3T3-F442A preadipocyte differentiation. In the current studies, we used the bGH and human (h) GH analogs with single amino acid substitution, bGH-G119R and hGH-G120R, for determining their biological activity using the preadipocyte differentia...

Rational discovery of novel nuclear hormone receptor antagonists.

Nuclear hormone receptors (NRs) are potential targets for therapeutic approaches to many clinical conditions, including cancer, diabetes, and neurological diseases. The crystal structure of the ligand binding domain of agonist-bound NRs enables the design of compounds with agonist activity. However, with the exception of the human estrogen receptor-alpha, the lack of antagonist-bound "inactive"...