Novel CoA-Polyamine Conjugates for Effective Inhibition of Spermine/Spermidine-N¹-Acetyltransferase

Abstract

New mimics of the transition state of spermine/spermidine-N¹-acetyltransferase reaction were prepared starting from aminooxy analogues of spermidine or spermine and SH-CoA. The activity depended on the structure of polyamine fragment of the conjugate and best of the synthesized compounds were active at micromolar concentrations.

Keywords:

• Polyamines
• coenzyme A
• SSAT
• coenzyme-substrate inhibitors

This work was supported by the Russian Foundation for Basic Research, project No. 06-04-49638 and Academy of Finland, project no. 117436.

N. Grigorenko present address: Department of Chemistry & Biochemistry, University of Bern, Bern, Switzerland.