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Chembiochem. 2011 Jul 25;12(11):1767-73. doi: 10.1002/cbic.201100007. Epub 2011 Jun 10.

Triptolide directly inhibits dCTP pyrophosphatase.

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1
Department of Molecular, Cellular and Developmental Biology, Yale University, P. O. Box 208103, New Haven, CT 06520-8103, USA. tcorson@iupui.edu

Abstract

Triptolide is a potent natural product, with documented antiproliferative, immunosuppressive, anti-inflammatory, antifertility, and antipolycystic kidney disease effects. Despite a wealth of knowledge about the biology of this compound, direct intracellular target proteins have remained elusive. We synthesized a biotinylated photoaffinity derivative of triptolide, and used it to identify dCTP pyrophosphatase 1 (DCTPP1) as a triptolide-interacting protein. Free triptolide interacts directly with recombinant DCTPP1, and inhibits the enzymatic activity of this protein. Triptolide is thus the first dCTP pyrophosphatase inhibitor identified, and DCTPP1 is a biophysically validated target of triptolide.

PMID:
21671327
PMCID:
PMC3503517
DOI:
10.1002/cbic.201100007
[Indexed for MEDLINE]
Free PMC Article
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