Competitive affinity-based proteome profiling and imaging to reveal potential cellular targets of betulinic acid

作者：Guo, Haijun; Xu, Jiaqian; Hao, Piliang^*; Ding, Ke^*; Li, Zhengqiu^*

来源：Chemical communications, 2017, 53(69): 9620-9623.

DOI：10.1039/c7cc04190j

• PHOTO-CROSS-LINKERS
• MASS-SPECTROMETRY CCMS
• CHEMICAL PROTEOMICS
• KINASE INHIBITORS
• ANTITUMOR AGENTS
• SMALL MOLECULES
• IDENTIFICATION
• DERIVATIVES
• CELLS
• CHEMISTRY

Betulinic acid (BA), a pentacyclic triterpenoid natural product, has received considerable attention owing to the broad spectrum of biological activities such as anti-HIV, anti-inflammatory, and especially, antitumor. Despite numerous studies on the antitumor mechanisms over the past decade, the cellular targets in cancer cells remain obscure. Here, we developed two photoprobes, BA-1/BA-2, by attaching terminal alkyne-containing "minimalist'' tetrazole/diazirine photo-crosslinkers (L3 and L7) at the C-3 and C-28 positions of BA, respectively, based on well-established structure-activity relationships. The potential cellular targets were identified via competitive proteome profiling and bioimaging approaches.

• 出版日期2017-9-7
• 单位暨南大学; 上海科技大学