Molecular Cancer Therapeutics Targeting the PI3-Kinase Pathway in Cancer
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Platelet 12-lipoxygenase (P-12-LOX) is overexpressed in different types of cancers and the level of expression is correlated with grade. Arachidonic acid is metabolized by 12-LOX to 12(S)HETE, and this metabolite is involved in cancer progression by modulating cell proliferation in multiple cancer related pathways inducing angiogenesis and metastasis. Thus, inhibition of P-12-LOX can reduce these two processes. Using a homology model of the three-dimensional structure of human P-12-LOX (green structure), we performed computational docking of curcumin derivatives to identify novel inhibitors (magenta and green stick models in the ribbon model of P-12-LOX). From a set of the curcuminoids that were successfully docked and selected for testing, two were found to inhibit human lipoxygenase better than curcumin. For details, see Jankun et al. in this issue.



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Cancer Research Clinical Cancer Research
Cancer Epidemiology Biomarkers & Prevention Molecular Cancer Therapeutics
Molecular Cancer Research Cell Growth & Differentiation
Copyright © 2007 by the American Association for Cancer Research.