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J Med Chem. 2004 Sep 23;47(20):4971-4.

Molecular design of cholesterols as inhibitors of DNA polymerase alpha.

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Frontier Research Center for Genome & Drug Discovery, Department of Applied Biological Science, Faculty of Science and Technology, and Faculty of Pharmaceutical Sciences, Tokyo University of Science, 2641 Yamazaki, Noda-shi, Chiba-ken 278-8510, Japan.


The triterpenoid structure is a promising motif for the molecular design of DNA polymerase inhibitors.(1) In this study, 2-(cholesteryloxy)acetic acid (3), 2-(cholestanyl)acetic acid (7), and 2-(stigmasteryl)acetic acid (11) were found to selectively affect only DNA polymerase alpha (pol.alpha). The presence of a carboxyl group at position 28 appears to be essential for the inhibition of the pol.alpha activity. With pol.alpha, these compounds acted by competing with the template-primer DNA and noncompetitively with the substrate.

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