Design, Synthesis, and Biological Evaluation of Potent Photoaffinity Probes of Oleanolic Acid

Title:Design, Synthesis, and Biological Evaluation of Potent Photoaffinity Probes of Oleanolic Acid

Volume: 9 Issue: 2

Author(s): Liying Zhang, Jizhe Dong, Yingxia Zhang, Jun Liu, Luyong Zhang and Hongbin Sun

Affiliation:

Keywords: Binding affinity, Glycogen phosphorylase, Oleanolic acid, Photoaffinity probes, Target proteins

Abstract: To study the target proteins of oleanolic acid, a series of novel photoaffinity probes were designed and synthesized. Their affinity for the target proteins was evaluated in an enzyme inhibition assay against glycogen phosphorylase, a known target protein of oleanolic acid. Among these compounds, probe 2 exhibited the most potent activity with an IC50 value of 5.98 μM, which was about 2.5-fold more potent than its parent compound oleanolic acid. The results showed that the synthesized photoaffinity probes retained the binding affinity for their target proteins, and might be used as powerful tools to fish out the target proteins of oleanolic acid.

Cite this article as:

Zhang Liying, Dong Jizhe, Zhang Yingxia, Liu Jun, Zhang Luyong and Sun Hongbin, Design, Synthesis, and Biological Evaluation of Potent Photoaffinity Probes of Oleanolic Acid, Medicinal Chemistry 2013; 9 (2) . https://dx.doi.org/10.2174/1573406411309020012