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Identification of disulfide isomerase ERp57 as a target for small molecule cardioprotective agents
Guozhen Cui1,2; Luchen Shan3; Ivan Keung Chu4; Guohui Li4; George Pak Heng Leung5; Yuqiang Wang3; Yiu Wa KWAN6; Shun Wan CHAN7; Maggie Pui Man Hoi1; Simon Ming Yuen Lee1
2015-08-14
Source PublicationRSC Advances
ISSN20462069
Volume5Issue:91Pages:74605-74610
Abstract

We previously reported a novel danshensu analogue known as ADTM, which exhibited strong protective effects against oxidative stress-induced cellular injury and acute ischemic myocardial infarct in rat; however, the exact protein target of ADTM has not been fully characterized. In the present study, a biotin-conjugated ADTM analogue (BAA) was employed as molecular probe to identify its protein targets. BAA exhibited similar protective effect against oxidative stress-induced cell injury in H9c2 cardiomyoblast. A chemical proteomic approach identified ERp57 as the specific target for BAA. Further evaluation with Western blot and immunofluorescence staining assays confirmed the direct interactions between BAA and ERp57. Moreover, BAA displayed potent inhibitory effect on the catalytic activity of ERp57 in the insulin reduction assay. Molecular docking showed that BAA bound at the active site of ERp57. These data suggested that ERp57 is a potential target of cardioprotective danshensu analogues, and provided the basis for the further optimization of the cardioprotective compounds.

DOI10.1039/c5ra08551a
URLView the original
Language英语
WOS Research AreaChemistry
WOS SubjectChemistry, Multidisciplinary
WOS IDWOS:000361116500057
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Cited Times [WOS]:8   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionInstitute of Chinese Medical Sciences
Affiliation1.State Key Laboratory of Quality Research in Chinese Medicine and Institute of Chinese Medical Sciences, University of Macau, Macao, China
2.Department of Bioengineering, Zhuhai Campus of Zunyi Medical University, Zhuhai, Guangdong, China
3.Institute of New Drug Research, Collage of Pharmacy, Jinan University, Guangzhou, China
4.Department of Chemistry, The University of Hong Kong, Hong Kong, China
5.Department of Pharmacology and Pharmacy, Li Ka Shing Faculty of Medicine, The University of Hong Kong, Hong Kong, China
6.School of Biomedical Sciences, The Chinese University of Hong Kong, Hong Kong, China
7.State Key Laboratory of Chinese Medicine and Molecular Pharmacology, Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hong Kong, China
First Author AffilicationInstitute of Chinese Medical Sciences
Recommended Citation
GB/T 7714
Guozhen Cui,Luchen Shan,Ivan Keung Chu,et al. Identification of disulfide isomerase ERp57 as a target for small molecule cardioprotective agents[J]. RSC Advances,2015,5(91):74605-74610.
APA Guozhen Cui.,Luchen Shan.,Ivan Keung Chu.,Guohui Li.,George Pak Heng Leung.,...&Simon Ming Yuen Lee.(2015).Identification of disulfide isomerase ERp57 as a target for small molecule cardioprotective agents.RSC Advances,5(91),74605-74610.
MLA Guozhen Cui,et al."Identification of disulfide isomerase ERp57 as a target for small molecule cardioprotective agents".RSC Advances 5.91(2015):74605-74610.
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