Antiproliferative and GH-inhibitory activity of chimeric peptides consisting of GHRP-6 and somatostatin.
Chimeric peptides consisting of growth hormone releasing peptide (GHRP-6) linked to somatostatin (6-11) via an amide bond to provide the effector parts of both the peptides were synthesized. The anti-proliferative, cytotoxic, and GH-inhibitory activities of these chimeric peptides were determined in vitro in the rat pituitary adenoma cell line GH3. One of the chimeric peptides, GSD, exhibited significantly greater (p < 0.001) anti-neoplastic and GH-inhibitory activity, as compared to RC-160. The hybrid peptides displayed high affinity binding to somatostatin receptors on GH3 cells. The bioactivity of GSD was found to be mediated by the stimulation of tyrosine phosphatase, involving a cGMP-dependent pathway, through pertussis toxin-sensitive G-proteins. Such potent GH-inhibitory chimeric peptides may be of potential importance in the therapy of acromegaly, as well as provide novel tools to study the regulation of GH secretion by GHRP and somatostatin.[1]References
- Antiproliferative and GH-inhibitory activity of chimeric peptides consisting of GHRP-6 and somatostatin. Dasgupta, P., Singh, A.T., Mukherjee, R. Biochem. Biophys. Res. Commun. (1999) [Pubmed]
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