Melanocortin peptides
containing a 3-(2-naphthyl)-
d
-alanine
residue in position 7 (DNal(2′)
7
), reported as melanocortin-3
receptor (MC3R) subtype-specific agonists in two separate publications,
were found to lack significant MC3R agonist activity. The cell lines
used at the University of Arizona for pharmacological characterization
of these peptides, consisting of HEK293 cells stably transfected with
human melanocortin receptor subtypes MC1R, MC3R, MC4R, or MC5R, were
then obtained and characterized by quantitative polymerase chain reaction
(PCR). While the MC1R cell line correctly expressed only hMCR1, the
three other cell lines were mischaracterized with regard to receptor
subtype expression. The demonstration that a 3-(2-naphthyl)-
d
-alanine residue in position 7, irrespective of the melanocortin
peptide template, results primarily in the antagonism of MC3R and
MC4R then allowed us to search the published literature for additional
errors. The erroneously characterized DNal(2′)
7
-containing
peptides date back to 2003; thus, our analysis suggests that systematic
mischaracterization of the pharmacological properties of melanocortin
peptides occurred.
Melanocortin peptides containing a D-naphthylalanine residue in position 7 (DNal(2')7), reported as melanocortin-3 receptor (MC3R) subtype-specific agonists in two separate publications, were found to lack significant MC3R agonist activity. The cell lines used at the University of Arizona for pharmacological characterization of these peptides, consisting of HEK293 cells stably transfected with human melanocortin receptor subtypes MC1R, MC3R, MC4R, or MC5R, were then obtained and characterized by quantitative PCR. While the MC1R cell line correctly expressed only the hMCR1, the three other cell lines were mischaracterized with regard to receptor subtype expression. Demonstration that a D-naphthylalanine residue in position 7, irrespective of the melanocortin peptide template, results primarily in antagonism of the MC3R and MC4R, then allowed us to search the published literature for additional errors. The erroneously characterized DNal(2')7-containing peptides date back to 2003; thus, our analysis suggests that systematic mischaracterization of the pharmacological properties of melanocortin peptides occurred.
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