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Science 17 April 1970:
Vol. 168. no. 3929, pp. 378 - 380
DOI: 10.1126/science.168.3929.378
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Articles

Inhibition of Phosphofructokinase by Quinone Methide and agr-Methylene Lactone Tumor Inhibitors

Ronald L. Hanson 1, Henry A. Lardy 1, and S. Morris Kupchan 2

1 Institute for Enzyme Research, University of Wisconsin, Madison 53706
2 Department of Pharmaceutical Chemistry, University of Wisconsin

The plant-derived tumor inhibitors taxodone, taxodione, vernolepin, eupacunin, and euparotin acetate each inhibit the sulfhydryl enzyme, phosphofructokinase. The substrates, fructose-6-phosphate and adenosine triphosphate, protect the enzyme from this, inhibition as does the addition of dithiothreitol to the inhibitors. Incubation of taxodione with phosphofructokinase is associated with the loss of about one sulfhydryl group per inhibitor molecule, and the substrates protect six sulfhydryl groups per protomer of 93,000 daltons.


THIS ARTICLE HAS BEEN CITED BY OTHER ARTICLES:
Sesquiterpene antitumor agents: inhibitors of cellular metabolism.
K. Lee, I. Hall, E. Mar, C. Starnes, S. ElGebaly, T. Waddell, R. HADGRAFT, C. Ruffner, and I Weidner (1977)
Science 196, 533-536
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Selective Alkylation: A Biomimetic Reaction of the Antileukemic Triptolides?.
S. M. Kupchan and R. M. Schubert (1974)
Science 185, 791-793
   Abstract »    PDF »


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