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Journal archive > 2010 > N 2 March-April

NEW NON-PEPTIDE INHIBITORS OF?FURIN

V. K. Kibirev1, T. V. Osadchuk1, O.?B.?Vadzyuk2, M. M. Garazd1

1Institute of Bioorganic Chemistry and Petrochemistry, Natioal Аcademy of Sciences of Ukraine, Kyiv;
2Palladin Institute of Biochemistry, National Academy of Sciences of Ukraine, Kyiv;
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Furin, a human subtilisin-related proprotein convertase, is the most important pharmaceutical target because it plays a vital role in development of numerous disease processes. To identify a new class of small non-peptide inhibitors of furin we performed a study of several flavonoids and some natural products. Glycosylated flavonoids: rutin, naringin, baikalin and methylhesperidin were shown to inhibit furin at pH 7.2 reversibly and competitively with Ki ~ 80–200 µM. The Ki values­ were derived from Dixon and/or Eadie-Hofstee plots using fluorogenic substrate Boc-Arg-Val-Arg-Arg-AMC. Although studied flavonoids display only a temperate furin inhibition, they may serve as a great potential for the future development of more potent non-peptide inhibitors against furin.

Key words: furin, inhibitors of furin, flavonoids, rutin, naringin, baikalin, methylhesperidin.

The original article in Russian is available for download in PDF format.

© The Ukrainian Biochemical Journal