"目录号: HY-13716
GPCR/G ProteinAutophagy-
Noscapine是一种口服止咳药, 主要通过其 σ受体激动剂活性调节, 且Noscapine具有抗癌活性。
Sigma ReceptorAutophagy
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生物活性
Description
Noscapine is an orally administrable drug used worldwide for cough suppression, primarily mediated by its σ-receptor agonist activity, and possess anticancer activity.Target: σ-receptorin vitro: Noscapine is a phthalideisoquinoline alkaloid from opium, is a recently discovered anticancer drug and is currently under investigation in phase-I/II clinical trials for the treatment of leukemia and lymphoma. Noscapine causes few or no side effects and has been widely used as a cough suppressant in developing countries. Noscapine has been demonstrated to interact with microtubules. Interestingly, unlike many other microtubule-targeting agents such as Paclitaxel and Nocodazole, Noscapine does not obviously affect the total amount of microtubule polymers in cells; instead, it significantly increases the time microtubules spend in the pause state. The alteration of microtubule dynamics then activates the spindle checkpoint and arrests cell cycle progression at mitosis, leading to apoptotic cell death.
Clinical Trial
NCT00912899
Cougar Biotechnology, Inc.
Refractory Multiple Myeloma
December 2007
Phase 1
NCT00183950
University of Southern California
Non-Hodgkin's Lymphoma-Chronic Lymphocytic Leukemia
March 2000
Phase 1-Phase 2
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References
[1].Yang Y, et al. CYLD Regulates Noscapine Activity in Acute Lymphoblastic Leukemia via a Microtubule-Dependent Mechanism. Theranostics. 2015 Mar 2;5(7):656-666.