An approach for differentiating isozymes. Construction of libraries containing short aromatic peptides as part of a method to design selective inhibitors against lipases

作者：Park Sangeun; Yu Jaehoon^*

来源：Bioorganic & Medicinal Chemistry Letters, 2012, 22(9): 3147-3151.

DOI：10.1016/j.bmcl.2012.03.048

• Lipase
• Peptidyl substrate
• Selective inhibitor
• Fingerprint
• Isozymes

Through synthesis and assays of peptidyl substrates, we could select substrates having peptidyl complementary against lipases. The best substrate showed 20-fold improved K-m relative to non-peptidyl substrate. Using this information, we generated selective inhibitors. Lipase activities with peptidyl substrates were represented as fingerprints. Differences in fingerprints reflect different structures near active site of lipases, could be used for generating selective inhibitors.

• 出版日期2012-5-1