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

Sangeun Park; Jaehoon Yu

doi:10.1016/j.bmcl.2012.03.048

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

Bioorg Med Chem Lett. 2012 May 1;22(9):3147-51. doi: 10.1016/j.bmcl.2012.03.048. Epub 2012 Mar 21.

Authors

Sangeun Park¹, Jaehoon Yu

Affiliation

¹ Department of Chemistry & Education, Seoul National University, Seoul 151-742, Republic of Korea.

PMID: 22483390
DOI: 10.1016/j.bmcl.2012.03.048

Abstract

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Amino Acids, Aromatic*
Enzyme Inhibitors
Isoenzymes*
Kinetics
Lipase / antagonists & inhibitors*
Methods
Peptides*
Small Molecule Libraries / chemical synthesis*
Substrate Specificity

Substances

Amino Acids, Aromatic
Enzyme Inhibitors
Isoenzymes
Peptides
Small Molecule Libraries
Lipase