Abstract
Cyclopamine is a naturally occurring steroidal alkaloid that attenuates the Hedgehog signaling pathway by inhibiting the Smoothened receptor. The Hedgehog pathway plays an important role in many human cancers. Cyclopamine has served as a pivotal tool compound in elucidating the pharmacological effect of the Hedgehog signaling pathway, however, due to its poor solubility, stability, and moderate activity, its clinical development has been impeded. Significant efforts were made to overcome the shortcomings of cyclopamine, giving which results cultivated in the identification of IPI- 926, a derivative of cyclopamine, which proceeded to clinical trials.
Keywords: Antagonist, cancer therapy, cyclopamine, steroidal alkaloid, sonic hedgehog, smoothened.
Current Topics in Medicinal Chemistry
Title:Cyclopamine, a Naturally Occurring Alkaloid, and Its Analogues May Find Wide Applications in Cancer Therapy
Volume: 13 Issue: 17
Author(s): Haikuo Ma, Huan-Qiu Li and Xiaohu Zhang
Affiliation:
Keywords: Antagonist, cancer therapy, cyclopamine, steroidal alkaloid, sonic hedgehog, smoothened.
Abstract: Cyclopamine is a naturally occurring steroidal alkaloid that attenuates the Hedgehog signaling pathway by inhibiting the Smoothened receptor. The Hedgehog pathway plays an important role in many human cancers. Cyclopamine has served as a pivotal tool compound in elucidating the pharmacological effect of the Hedgehog signaling pathway, however, due to its poor solubility, stability, and moderate activity, its clinical development has been impeded. Significant efforts were made to overcome the shortcomings of cyclopamine, giving which results cultivated in the identification of IPI- 926, a derivative of cyclopamine, which proceeded to clinical trials.
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Cite this article as:
Ma Haikuo, Li Huan-Qiu and Zhang Xiaohu, Cyclopamine, a Naturally Occurring Alkaloid, and Its Analogues May Find Wide Applications in Cancer Therapy, Current Topics in Medicinal Chemistry 2013; 13 (17) . https://dx.doi.org/10.2174/15680266113139990153
DOI https://dx.doi.org/10.2174/15680266113139990153 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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