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Design, Synthesis, and Biological Evaluation of Potent Photoaffinity Probes of Oleanolic Acid.
MedLine Citation:
PMID:  22931495     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
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.
Authors:
Liying Zhang; Jizhe Dong; Yingxia Zhang; Jun Liu; Luyong Zhang; Hongbin Sun
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2012-8-17
Journal Detail:
Title:  Medicinal chemistry (Shariqah (United Arab Emirates))     Volume:  -     ISSN:  1875-6638     ISO Abbreviation:  Med Chem     Publication Date:  2012 Aug 
Date Detail:
Created Date:  2012-8-30     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  101240303     Medline TA:  Med Chem     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Affiliation:
State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 21009, China. junliu@cpu.edu.cn; hbsun2000@yahoo.com.
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