Please use this identifier to cite or link to this item: https://doi.org/10.1016/j.canlet.2021.08.030
Title: Celastrol in cancer therapy: Recent developments, challenges and prospects
Authors: Lim, Hannah Ying
PEI SHI ONG
LINGZHI WANG
Goel, Arul
LINGWEN DING
LI ANN ANDREA WONG
Ho P.C. 
Sethi, Gautam 
Xiang, Xiaoqiang
Goh, B.C. 
Keywords: Science & Technology
Life Sciences & Biomedicine
Oncology
Celastrol
Anti-cancer activity
Pharmacokinetics
Toxicity
Translational potential
STAT3 SIGNALING PATHWAY
KAPPA-B KINASE
HEPATOCELLULAR-CARCINOMA
IN-VITRO
NUDE-MICE
ANTICANCER ACTIVITY
HSP90 INHIBITOR
PURE CELASTROL
TUMOR-GROWTH
HUMAN GLIOMA
Issue Date: 28-Nov-2021
Publisher: ELSEVIER IRELAND LTD
Citation: Lim, Hannah Ying, PEI SHI ONG, LINGZHI WANG, Goel, Arul, LINGWEN DING, LI ANN ANDREA WONG, Ho P.C., Sethi, Gautam, Xiang, Xiaoqiang, Goh, B.C. (2021-11-28). Celastrol in cancer therapy: Recent developments, challenges and prospects. CANCER LETTERS 521 : 252-267. ScholarBank@NUS Repository. https://doi.org/10.1016/j.canlet.2021.08.030
Abstract: Cancer is one of the world's biggest healthcare burdens and despite the current advancements made in treatment plans, the outcomes for oncology patients have yet to reach their full potential. Hence, there is a pressing need to develop novel anti-cancer drugs. A popular drug class for research are natural compounds, due to their multi-targeting potential and enhanced safety profile. One such promising natural bioactive compound derived from a vine, Tripterygium wilfordii is celastrol. Pre-clinical studies revolving around the use of celastrol have revealed positive pharmacological activities in various types of cancers, thus suggesting the chemical's potential anti-cancerous effects. However, despite the numerous preclinical studies carried out over the past few decades, celastrol has not reached human trials for cancer. In this review, we summarize the mechanisms and therapeutic potentials of celastrol in treatment for different types of cancer. Subsequently, we also explore the possible reasons hindering its development for human use as cancer therapy, like its narrow therapeutic window and poor pharmacokinetic properties. Additionally, after critically analysing both in vitro and in vivo evidence, we discuss about the key pathways effected by celastrol and the suitable types of cancer that can be targeted by the natural drug, thus giving insight into future directions that can be taken, such as in-depth analysis and research of the druggability of celastrol derivatives, to aid the clinical translation of this promising anti-cancer lead compound.
Source Title: CANCER LETTERS
URI: https://scholarbank.nus.edu.sg/handle/10635/204075
ISSN: 0304-3835
1872-7980
DOI: 10.1016/j.canlet.2021.08.030
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