Design and Synthesis of Redox Stable Analogues of Sunflower Trypsin Inhibitors (SFTI-1) on Solid Support, Potent Inhibitors of Matriptase

Design and Synthesis of Redox Stable Analogues of Sunflower Trypsin Inhibitors (SFTI-1) on Solid Support, Potent Inhibitors of Matriptase

Matriptase is a member of the emerging class of type II transmembrane serine proteases. It was found that the sunflower trypsin inhibitor (SFTI-1), isolated from sunflower seeds, inhibits matriptase with a subnanomolar K i of 0.92 nM. On the basis of this result, we designed and synthesized its prot...

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Veröffentlicht in:Organic letters 2007-01, Vol.9 (1), p.9-12
Hauptverfasser: Jiang, Sheng, Li, Peng, Lee, Sheau-Ling, Lin, Cheng Yong, Long, Ya-Qiu, Johnson, Michael D, Dickson, Robert B, Roller, Peter P
Format: Artikel
Sprache:eng
Schlagworte:
Cyclization
Drug Design
Helianthus - chemistry
Molecular Structure
Oxidation-Reduction
Peptides - chemical synthesis
Peptides - chemistry
Peptides - pharmacology
Serine Endopeptidases - metabolism
Serine Proteinase Inhibitors - chemical synthesis
Serine Proteinase Inhibitors - chemistry
Serine Proteinase Inhibitors - pharmacology
Trypsin Inhibitors - chemistry
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Zusammenfassung:Matriptase is a member of the emerging class of type II transmembrane serine proteases. It was found that the sunflower trypsin inhibitor (SFTI-1), isolated from sunflower seeds, inhibits matriptase with a subnanomolar K i of 0.92 nM. On the basis of this result, we designed and synthesized its proteolytically stable analogues, SFTI-2 and SFTI-3. SFTI-3 exhibited very good binding affinity to matriptase, and it was metabolically stable.
ISSN:1523-7060
1523-7052
DOI:10.1021/ol0621497