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Org Lett. 2006 Apr 27;8(9):1799-802.

Design and synthesis of potent cystine-free cyclic hexapeptide agonists at the human urotensin receptor.

Author information

1
Department of Chemistry, University of Pennsylvania, Philadelphia, Pennsylvania 19104, USA.

Abstract

[structure: see text] Cyclic hexapeptides, incorporating a dipeptide unit in place of the disulfide bond found in urotensin, were prepared and screened at the human urotensin receptor. The bridging dipeptide unit was found to influence dramatically the affinity for the urotensin receptor. Alanyl-N-methylalanyl and alanylprolyl dipeptide bridges failed to afford active ligands, while the alanyl-alanyl unit yielded a ligand with submicromolar affinity for the urotensin receptor. Further development led to a hexapeptide agonist with nanomolar affinity (2.8 nM).

PMID:
16623554
DOI:
10.1021/ol060278h
[Indexed for MEDLINE]

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