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1: Bioorg Med Chem Lett. 2006 Feb 15;16(4):923-7. Epub 2005 Nov 21.Click here to read Links

Inhibition of DNA helicases with DNA-competitive inhibitors.

Dubaele S, Jahnke W, Schoepfer J, Fuchs J, Chène P.

Novartis Institutes for Biomedical Research, Oncology Research, CH-4002 Basel, Switzerland.

Helicases form an attractive protein family for drug discovery because they are involved in various human diseases. In this report, we show that it is possible to inhibit both the ATPase and the helicase activities of a DNA helicase with dibenzothiepins that bind at its nucleic acid binding site. These results suggest a drug discovery strategy to inhibit DNA helicases.

PMID: 16300943 [PubMed - indexed for MEDLINE]