Design, synthesis, kinetic analysis, molecular modeling, and pharmacological evaluation of novel inhibitors of peptide amidation

Novel, rationally-designed acrylate analogs of various known dipeptide substrates were found to be mechanism-based inactivators of the enzyme peptidylglycine alpha-amidating monooxygenase (PAM, EC 1.14.17.3). This enzyme is responsible for the rate-limiting and final bioactivation step, a C-termina...

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Bibliographic Details
Main Author: Foster, Michael Scott
Published: Georgia Institute of Technology 2010
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Online Access:http://hdl.handle.net/1853/31816