Abstract
Luteinizing hormone-releasing hormone (LHRH) is the key regulator of the hypothalamic-pituitary-gonadal (HPG) axis, which is responsible for the development and functioning of the reproductive system. Delivery of a continuous supply of LHRH agonists causes down-regulation of the LHRH receptors, resulting in a marked decrease in androgens in males and estrogens in females. LHRH analogues are widely used in the treatment of various diseases, including prostate and breast cancer, and reproductive disorders, such as infertility and precocious puberty. However, they require parenteral administration, and no oral formulations are currently available. We synthesized two types of LHRH mini-dendrimers using thioether ligation, aiming to enhance the stability and bioavailability of the peptide drug while maintaining its biologically active conformation. These two compounds include a poly-lysine core conjugated to either the C-terminus of LHRH or a D-amino acid in position 6 of the LHRH sequence. The synthesized dendrimers were analysed using dynamic light scattering, and showed particle sizes of 155 and 115 nm, respectively. The nanometer size, well-defined structure and water solubility of these dendritic analogues make them excellent candidates for further exploration in oral peptide drug delivery.
Highlights
Luteinizing hormone-releasing hormone (LHRH), known as gonadotropin-releasing hormone (GnRH), is the central regulator of the hormones of the hypothalamic-pituitary-gonadal (HPG) axis, which controls and regulates reproductive function [1]
Luteinizing hormone-releasing hormone (LHRH) is the key regulator of the hypothalamic-pituitary-gonadal (HPG) axis, which is responsible for the development and functioning of the reproductive system
It is transported to the anterior pituitary where it activates its receptor, resulting in the production and secretion of the gonadotropins follicle-stimulating hormone (FSH) and luteinizing hormone (LH)
Summary
Luteinizing hormone-releasing hormone (LHRH), known as gonadotropin-releasing hormone (GnRH), is the central regulator of the hormones of the hypothalamic-pituitary-gonadal (HPG) axis, which controls and regulates reproductive function [1] This decapeptide is released from neurons of the hypothalamus into the portal vascular system in synchronized pulses. Continuous supply of LHRH, as opposed to the naturally occurring pulsatile pattern, causes downregulation of the LHRH receptors, resulting in a marked decrease in androgens in males and estrogens in females. This has been exploited in the treatment of hormone-
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