Precise structural elucidation of dehydroaltenusin, a specific inhibitor of mammalian DNA polymerase alpha

Bioorganic & Medicinal Chemistry
Shinji KamisukiF Sugawara

Abstract

The X-ray crystal structure of dehydroaltenusin, a specific inhibitor of mammalian DNA polymerase alpha, has previously been reported. We show that dehydroaltenusin exists in an equilibrium mixture of two tautomers possessing gamma-lactone or delta-lactone in polar solvents by NMR experiments. Acetylation of dehydroaltenusin afforded two types of diacetates and two types of monoacetate, possessing gamma-lactone or delta-lactone, respectively. The inhibitory activities of these acetate derivatives against DNA polymerase alpha were all much weaker than that of dehydroaltenusin.

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Citations

Jun 9, 2009·Bioscience, Biotechnology, and Biochemistry·Yoshiyuki Mizushina
Jul 9, 2011·Bioscience, Biotechnology, and Biochemistry·Masaharu TakemuraTeruyoshi Oshima
Sep 20, 2011·Expert Opinion on Investigational Drugs·Yoshiyuki MizushinaHiromi Yoshida
Nov 23, 2006·Biochemical and Biophysical Research Communications·Naoki MaedaYoshiyuki Mizushina
Jul 4, 2009·Journal of Natural Products·Martina Altemöller, Joachim Podlech

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