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Triptolide and Its Derivatives as Cancer Therapies

Noel, Pawan, Von Hoff, Daniel D., Saluja, Ashok K., Velagapudi, Mohana, Borazanci, Erkut, Han, Haiyong·2019·Trends in Pharmacological Sciences

Abstract

Triptolide, a compound isolated from a Chinese medicinal herb, possesses potent antitumor, immunosuppressive, and anti-inflammatory properties, but is clinically limited due to its poor solubility, bioavailability, and toxicity. Recently, Minnelide, a water-soluble prodrug of triptolide, was shown to have potent antitumor activity in various preclinical cancer models. Minnelide is currently in Phase II clinical trials for treatment of advanced pancreatic cancer, which has fueled increased interest in this promising agent. Here, we review the recent advances in the biological activity of triptolide and its analogs, their mechanisms of actions, and their clinical developments. A special emphasis is given to proteins and pathways within the tumor and stromal compartments that are targeted by triptolide and its analogs as well as the ongoing clinical trials.

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Metadata

Authors
Noel, P., Von Hoff, D. D., Saluja, A. K., Velagapudi, M., Borazanci, E., & Han, H.
Venue
Trends in Pharmacological Sciences
Publisher
Elsevier BV
Published
2019-05
Volume
40
Issue
5
Pages
327-341
ISSN
0165-6147
Cited by
294
References
4
Language
en
Funders
  • Lustgarten Foundation (SU2C-AACR-DT-20-16)
  • Seena Magowitz Foundation
  • National Foundation for Cancer Research
  • American Association for Cancer Research

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Noel, P., Von Hoff, D. D., Saluja, A. K., Velagapudi, M., Borazanci, E., & Han, H. (2019). Triptolide and Its Derivatives as Cancer Therapies. Trends in Pharmacological Sciences. https://doi.org/10.1016/j.tips.2019.03.002