Organic letters, 2006-04, Vol.8 (9), p.1799-1802
2006
Volltextzugriff (PDF)
Details
- Autor(en) / Beteiligte
- Titel
- Design and Synthesis of Potent Cystine-Free Cyclic Hexapeptide Agonists at the Human Urotensin Receptor
- Ist Teil von
- Organic letters, 2006-04, Vol.8 (9), p.1799-1802
- Ort / Verlag
- United States: American Chemical Society
- Erscheinungsjahr
- 2006
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- 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).
- Sprache
- Englisch
- Identifikatoren
- ISSN: 1523-7060eISSN: 1523-7052DOI: 10.1021/ol060278hTitel-ID: cdi_proquest_miscellaneous_67885907
- Format
- –
- Schlagworte
- Amino Acid Sequence, Binding Sites, Cystine - chemistry, Dipeptides - chemistry, Humans, Models, Molecular, Molecular Structure, Peptides, Cyclic - chemical synthesis, Peptides, Cyclic - chemistry, Receptors, G-Protein-Coupled - agonists, Receptors, G-Protein-Coupled - chemistry, Urotensins - agonists, Urotensins - chemistry