Please use this identifier to cite or link to this item: https://doi.org/10.3390/biom9100550
Title: Brusatol, a nrf2 inhibitor targets stat3 signaling cascade in head and neck squamous cell carcinoma
Authors: Rangappa, K.S.
Lee, J.H.
Rangappa, S.
Mohan, C.D.
Basappa, Laboratory of Chemical Biology, Department of Studies in Organic Chemistry, University of Mysore, Manasagangotri, Mysore, 570006, India.
Sethi, G. 
Lin, Z.-X.
Ahn, K.S.
Keywords: Apoptosis
Brusatol
HNSCC
STAT3 inhibitor
Issue Date: 2019
Publisher: MDPI AG
Citation: Rangappa, K.S., Lee, J.H., Rangappa, S., Mohan, C.D., Basappa, Laboratory of Chemical Biology, Department of Studies in Organic Chemistry, University of Mysore, Manasagangotri, Mysore, 570006, India., Sethi, G., Lin, Z.-X., Ahn, K.S. (2019). Brusatol, a nrf2 inhibitor targets stat3 signaling cascade in head and neck squamous cell carcinoma. Biomolecules 9 (10) : 550. ScholarBank@NUS Repository. https://doi.org/10.3390/biom9100550
Rights: Attribution 4.0 International
Abstract: STAT3 is a latent transcription factor that plays a vital role in the transmission of extracellular signal from receptors to the nucleus. It has been regarded as a master transcription factor due to its role in the regulation of a broad spectrum of genes, which can contribute to oncogenesis. Persistent activation of STAT3 and deregulation of its signaling has been observed in various human cancers including head and neck squamous cell carcinoma (HNSCC). In the present work, we identified brusatol (BT) as a potential blocker of STAT3 signaling pathway in diverse HNSCC cells. The data from the cell-based experiments suggested that BT-induced cytotoxicity and abrogated the activation of STAT3 and that of upstream kinases such as JAK1, JAK2, and Src. It reduced the levels of nuclear STAT3 and its DNA binding ability. BT treatment increased annexin-V-positive cells, promoted procaspase-3 and PARP cleavage, and downregulated the mRNA and protein expression of diverse proteins (Bcl-2, Bcl-xl, survivin) in HNSCC cells. Taken together, brusatol can function as a promising inhibitor targeting STAT3 signaling pathway in HNSCC. © 2019 by the authors.
Source Title: Biomolecules
URI: https://scholarbank.nus.edu.sg/handle/10635/209547
ISSN: 2218-273X
DOI: 10.3390/biom9100550
Rights: Attribution 4.0 International
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