Phage display selection on whole cells yields a peptide specific for melanocortin receptor 1

Michael Szardenings (Corresponding Author), Susanna Törnroth, Felikss Mutulis, Ruta Muceniece, Kari Keinänen, Arja Kuusinen, Jarl Wikberg

Research output: Contribution to journalArticleScientificpeer-review

82 Citations (Scopus)


A phage display system for the selection of peptides binding to heterologously expressed human melanocortin receptor 1 on the surface of insect cells has been established. It could be shown that phage particles displaying the natural ligand α-melanocyte-stimulating hormone bind selectively to cells expressing this receptor and that these phages exhibit biological activity on mouse B16F1 melanoma cells. Insect cells were superior to other cell lines tested and have been used to select binders from a small library, in which critical determinants (Phe7-Arg8-Trp9) were kept, whereas the flanking regions where allowed to variate freely. One peptide displaying little similarity with native hormone was found that binds to the receptor also in its free form with an affinity of 7 nm. It showed a remarkable selectivity for this receptor, because it binds to the other melanocortin receptor subtypes with a maximum affinity of 21 μm. This is the first time phage display has been used successfully with G-protein-coupled receptors lacking an extracellular binding domain.

Original languageEnglish
Pages (from-to)27943-27948
JournalJournal of Biological Chemistry
Issue number44
Publication statusPublished - 1997
MoE publication typeA1 Journal article-refereed


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