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Peptide mimetic of N‐terminal ghrelin enhances ghrelin‐induced growth hormone secretion and c‐Fos expression in mice
Author(s) -
Lunder Mojca,
Vodnik Miha,
Kubale Valentina,
Grgurevič Neža,
Majdič Gregor,
Štrukelj Borut
Publication year - 2018
Publication title -
journal of neuroendocrinology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.062
H-Index - 116
eISSN - 1365-2826
pISSN - 0953-8194
DOI - 10.1111/jne.12656
Subject(s) - ghrelin , orexigenic , endocrinology , medicine , peptide , receptor , peptide hormone , appetite , secretion , hormone , chemistry , biology , neuropeptide , biochemistry , neuropeptide y receptor
Orexigenic peptide ghrelin and its receptor have been extensively investigated as potential therapeutic targets, primarily because of their role in feeding initiation and growth hormone ( GH ) release. However, no specific ghrelin targeting anti‐obesity or cachexia therapeutics are available for clinical use thus far and further efforts in this direction are warranted. The present study aimed to find new peptide drug leads modulating ghrelin signal transduction. By targeting neutralising antibodies against ghrelin with phage display libraries, we aimed to identify peptides binding to the cognate receptor. Four synthetic peptides were selected and tested using calcium screening assays. The most effective competitive antagonist FSFLPPE was further tested in vivo. Administration of the peptide produced no significant effect on either food intake or GH release. Surprisingly, when co‐administered with ghrelin, the peptide significantly enhanced GH secretion and c‐Fos expression. The evidence obtained in the present study indicates that FSFLPPE might act as an ago‐allosteric modulator.