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Small-Molecule Inhibitors of the Hedgehog Pathway

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Book cover Hedgehog signaling activation in human cancer and its clinical implications

Abstract

The causal link between uncontrolled Hedgehog (Hh) pathway activation and oncogenesis has inspired the development of small-molecule inhibitors of this developmental signaling pathway. In this chapter, we discuss how a cyclopia-inducing natural product isolated in the 1950s has engendered a pharmacopoeia of compounds that block Hh target gene expression. We describe how these Hh pathway inhibitors were discovered, their mechanisms of action, and their potential as anti-cancer agents. We also examine potential limitations of current approaches and future directions for Hh pathway-targeting chemotherapies.

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  1. Department of Chemical and Systems Biology, Stanford University School of Medicine, 269 Campus Drive, CCSR 3155, Stanford, CA, 94305, USA

    James K. Chen

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  1. Ari J. Firestone
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  2. James K. Chen
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  1. University of Texas Medical Branch, Galveston, 77555, Texas, USA

    Jingwu Xie

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Firestone, A.J., Chen, J.K. (2011). Small-Molecule Inhibitors of the Hedgehog Pathway. In: Xie, J. (eds) Hedgehog signaling activation in human cancer and its clinical implications. Springer, New York, NY. https://doi.org/10.1007/978-1-4419-8435-7_11

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