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A peptide hormone
Ghrelin is an endogenous gastrointestinal hormone and neuropeptide that binds to the growth hormone (GH) secretagogue receptor (GHS-R). Ghrelin requires an n-octanoyl modification at serine 3 for binding to the growth hormone (GH) secretagogue receptor (GHS-R). (Des-octanoyl)-ghrelin (human) is a form of ghrelin that is lacking the octanoyl group at serine 3. It is located in the mouse stomach and is expressed at a lower level than octanoyl ghrelin. (Des-octanoyl)-ghrelin activates GHS-R by only 41% when used at 10 µM (IC50 = >10,000 nM; EC50 = >10,000 nM for increasing calcium accumulation). It induces bone marrow adipogenesis in rat models of growth hormone deficiency. (Des-octanoyl)-ghrelin also inhibits cell proliferation in estrogen-dependent MCF-7 breast cancer cells (EC50 = 0.81 µM) but induces proliferation of a somatotroph pituitary tumor cell line, an effect that can be blocked by MAPK, PKC, and tyrosine kinase inhibitors.
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