Abstract
Thrombin activates protease-activated receptor-1 (PAR-1) through binding to exosite I and the active site to promote tumor growth. We have developed a new class of anti-cancer glyco-peptides to target exosite I selectively without affecting the active-site-mediated coagulation activity and showed the importance of glycans for the stability and anti-cancer activity of the glyco-peptides.
MeSH terms
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Animals
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology
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Antineoplastic Agents / therapeutic use*
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Cell Line, Tumor
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Drug Design
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Glycopeptides / chemistry
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Glycopeptides / pharmacology
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Glycopeptides / therapeutic use*
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Humans
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Mice, SCID
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Neoplasms / drug therapy*
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Neoplasms / metabolism
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Neoplasms / pathology
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Receptor, PAR-1 / metabolism*
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Thrombin / chemistry
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Thrombin / metabolism*
Substances
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Antineoplastic Agents
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Glycopeptides
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Receptor, PAR-1
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Thrombin