Synthesis and Characterization of Luteinizing Hormone-Releasing Hormone (LHRH)-Functionalized Mini-Dendrimers

DOI: 10.4236/ijoc.2013.31006   PDF   HTML   XML   3,612 Downloads   6,239 Views   Citations


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.

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A. Rafiee, F. Mansfeld, P. Moyle and I. Toth, "Synthesis and Characterization of Luteinizing Hormone-Releasing Hormone (LHRH)-Functionalized Mini-Dendrimers," International Journal of Organic Chemistry, Vol. 3 No. 1, 2013, pp. 51-57. doi: 10.4236/ijoc.2013.31006.

Conflicts of Interest

The authors declare no conflicts of interest.


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