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AssigneeUstav Organicke Chemie A Biochemie Akademie Ved Cr, V.V.I.
InventorsLenka Maletinska, Blanka Zelezna, Miroslava Blechova, Andrea Spolcova
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Lipidated peptides, analogs of both forms of the prolactin-releasing peptide, PrRP31 and PrRP20, represent anorexigenic compounds that lower food intake and function in the brain after peripheral administration. The analogs PrRP31 and PrRP20 lipidated at the N-terminus by myristic or palmitic acids bind with high affinity to the endogenous receptor GPR10 in the rat pituitary cell line RC-4B/C and CHO cell line with transfected human receptor. These lipidated peptides also significantly decrease, in a dose-dependent manner, the food intake in fasted mice and have similar effects in comparable doses as centrally administered natural PrRP31, these effects are, however, stronger and longer lasting. Lipidation of an effective anorexigenic neuropeptide PrRP induces a central effect after peripheral administration and thus makes the lipidated analogs of PrRP a promising anti-obesity drug.
A lipidated analog of prolactin-releasing peptide having a general formula:
A lipidated analog of prolactin-releasing peptide according to any of the preceding claims, wherein the C-terminal amino acid is naphtylalanine, benzylcystein, benzylhistidine, pentafluorophenylalanine, or nitrophenyalanine.
A lipidated analog of prolactin-releasing peptide according to any of the preceding claims, wherein the fatty acid is selected from the group consisting of fatty acids with 6 to 18 carbons and fatty acids with 13 to 18 carbon atoms.
The use of the lipidated analog of prolactin-releasing peptide described in any of the preceding claims as anorexigenic agents lowering food intake after peripheral administration.
The use of the lipidated analog of prolactin-releasing peptide described in any of the preceding claims as an agent for the treatment of obesity.
A lipidated analog of prolactin-releasing peptide selected from:
A lipidated analog of prolactin-releasing peptide having the structure:
A lipidated analog of prolactin-releasing peptide according to formula:
A lipidated analog of prolactin-releasing peptide having the structure:
Dependencies are inferred from the claim text.