Please use this identifier to cite or link to this item: https://doi.org/10.7150/thno.49716
Title: Putting the BRK on breast cancer: From molecular target to therapeutics
Authors: Ang, Hui Li
Yuan, Yi 
Lai, Xianning 
Tan, Tuan Zea 
Wang, Lingzhi 
Huang, Benjamin BoJun
Pandey, Vijay
Huang, Ruby Yun-Ju
Lobie, Peter E 
Goh, Boon Cher 
Sethi, Gautam 
Yap, Celestial T 
Chan, Ching Wan 
Lee, Soo Chin 
Kumar, Alan Prem 
Keywords: Science & Technology
Life Sciences & Biomedicine
Medicine, Research & Experimental
Research & Experimental Medicine
Breast tumor kinase (BRK)
hallmarks of cancer
chemical inhibitors
molecular inhibitors
meta-analysis
PROTEIN-TYROSINE KINASE
MAMMARY EPITHELIAL-CELLS
LONG-TERM SURVIVAL
SH2-KINASE LINKER
SIGNALING PATHWAY
OLEANOLIC ACID
SH3 DOMAIN
FACTOR-I
PTK6
GROWTH
Issue Date: 1-Jan-2021
Publisher: IVYSPRING INT PUBL
Citation: Ang, Hui Li, Yuan, Yi, Lai, Xianning, Tan, Tuan Zea, Wang, Lingzhi, Huang, Benjamin BoJun, Pandey, Vijay, Huang, Ruby Yun-Ju, Lobie, Peter E, Goh, Boon Cher, Sethi, Gautam, Yap, Celestial T, Chan, Ching Wan, Lee, Soo Chin, Kumar, Alan Prem (2021-01-01). Putting the BRK on breast cancer: From molecular target to therapeutics. THERANOSTICS 11 (3) : 1115-1128. ScholarBank@NUS Repository. https://doi.org/10.7150/thno.49716
Abstract: BReast tumor Kinase (BRK, also known as PTK6) is a non-receptor tyrosine kinase that is highly expressed in breast carcinomas while having low expression in the normal mammary gland, which hints at the oncogenic nature of this kinase in breast cancer. In the past twenty-six years since the discovery of BRK, an increasing number of studies have strived to understand the cellular roles of BRK in breast cancer. Since then, BRK has been found both in vitro and in vivo to activate a multitude of oncoproteins to promote cell proliferation, metastasis, and cancer development. The compelling evidence concerning the oncogenic roles of BRK has also led, since then, to the rapid and exponential development of inhibitors against BRK. This review highlights recent advances in BRK biology in contributing to the “hallmarks of cancer”, as well as BRK’s therapeutic significance. Importantly, this review consolidates all known inhibitors of BRK activity and highlights the connection between drug action and BRK-mediated effects. Despite the volume of inhibitors designed against BRK, none have progressed into clinical phase. Understanding the successes and challenges of these inhibitor developments are crucial for the future improvements of new inhibitors that can be clinically relevant.
Source Title: THERANOSTICS
URI: https://scholarbank.nus.edu.sg/handle/10635/237218
ISSN: 1838-7640
DOI: 10.7150/thno.49716
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