FMP Publications

Our publications are recorded in a searchable database since 2010, updates will be added regularly.

All :: 2016, 2017
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Urolinin: The First Linear Peptidic Urotensin-II Receptor Agonist
Bandholtz(*), S., Erdmann(*), S., von Hacht(*), J. L., Exner(*), S., Krause, G., Kleinau(*), G.; Grotzinger(*), C.
Journal of medicinal chemistry, 59:10100-10112

Tags: Structural Bioinformatics and Protein Design (Krause, G.)

Abstract: This study investigated the role of individual U-II amino acid positions and side chain characteristics important for U-IIR activation. A complete permutation library of 209 U-II variants was studied in an activity screen that contained single substitution variants of each position with one of the other 19 proteinogenic amino acids. Receptor activation was measured using a cell-based high-throughput fluorescence calcium mobilization assay. We generated the first complete U-II substitution map for U-II receptor activation, resulting in a detailed view into the structural features required for receptor activation, accompanied by complementary information from receptor modeling and ligand docking studies. On the basis of the systematic SAR study of U-II, we created 33 further short and linear U-II variants from eight to three amino acids in length, including d- and other non-natural amino acids. We identified the first high-potency linear U-II analogues. Urolinin, a linear U-II agonist (nWWK-Tyr(3-NO2)-Abu), shows low nanomolar potency as well as improved metabolic stability.

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Leibniz-Forschungsinstitut für Molekulare Pharmakologie im Forschungsverbund Berlin e.V. (FMP)
Campus Berlin-Buch
Robert-Roessle-Str. 10
13125 Berlin, Germany
+4930 94793 - 100 
+4930 94793 - 109 (Fax)

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