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Current Topics in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

Cyclopamine, a Naturally Occurring Alkaloid, and Its Analogues May Find Wide Applications in Cancer Therapy

Author(s): Haikuo Ma, Huan-Qiu Li and Xiaohu Zhang

Volume 13, Issue 17, 2013

Page: [2208 - 2215] Pages: 8

DOI: 10.2174/15680266113139990153

Price: $65

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.

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