UM
Quantitative Proteomics Reveals Cellular Off-Targets of a DDR1 Inhibitor
Xu,Jiaqian1,2; Zhang,Zhang1; Lin,Ligen3; Sun,Hongyan2; White,Lorenzo V.1; Ding,Ke1; Li,Zhengqiu1
2020-04-09
Source PublicationACS Medicinal Chemistry Letters
Volume11Issue:4Pages:535-540
AbstractTarget identification of small molecules is a great challenge but an essential step in drug discovery. Here, a quantitative proteomics approach has been used to characterize the cellular targets of DR, a DDR1 inhibitor. By taking advantage of competitive affinity-based protein profiling coupled with bioimaging, Cathepsin D (CTSD) was found to be the principle off-target of DR in human cancer cells. Further findings suggest the potential of DR as a novel CTSD inhibitor for breast cancer treatment. In addition, a trans-cyclooctene (TCO) containing probe was developed to track the binding between DR and its target proteins in living systems and could be a useful tool for DDR1 detection.
Keywordbioimaging chemoproteomics DDR1 photoaffinity labeling target identification
DOI10.1021/acsmedchemlett.9b00658
URLView the original
Language英语
Fulltext Access
Citation statistics
Cited Times [WOS]:2   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionUniversity of Macau
Corresponding AuthorDing,Ke
Affiliation1.Intl. Coop. Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Development,Ministry of Education (MOE) of China,Guangzhou Key Laboratory of Precision Chemical Drug Development,School of Pharmacy,Jinan University,Guangzhou,601 Huangpu Avenue West,510632,China
2.Department of Chemistry,City University of Hong Kong,Hong Kong,83 Tat Chee Avenue,SAR 999077,Hong Kong
3.State Key Laboratory of Quality Research in Chinese Medicine,Institute of Chinese Medical Sciences,University of Macau,Taipa,Macao
Recommended Citation
GB/T 7714
Xu,Jiaqian,Zhang,Zhang,Lin,Ligen,et al. Quantitative Proteomics Reveals Cellular Off-Targets of a DDR1 Inhibitor[J]. ACS Medicinal Chemistry Letters,2020,11(4):535-540.
APA Xu,Jiaqian,Zhang,Zhang,Lin,Ligen,Sun,Hongyan,White,Lorenzo V.,Ding,Ke,&Li,Zhengqiu.(2020).Quantitative Proteomics Reveals Cellular Off-Targets of a DDR1 Inhibitor.ACS Medicinal Chemistry Letters,11(4),535-540.
MLA Xu,Jiaqian,et al."Quantitative Proteomics Reveals Cellular Off-Targets of a DDR1 Inhibitor".ACS Medicinal Chemistry Letters 11.4(2020):535-540.
Files in This Item:
There are no files associated with this item.
Related Services
Recommend this item
Bookmark
Usage statistics
Export to Endnote
Google Scholar
Similar articles in Google Scholar
[Xu,Jiaqian]'s Articles
[Zhang,Zhang]'s Articles
[Lin,Ligen]'s Articles
Baidu academic
Similar articles in Baidu academic
[Xu,Jiaqian]'s Articles
[Zhang,Zhang]'s Articles
[Lin,Ligen]'s Articles
Bing Scholar
Similar articles in Bing Scholar
[Xu,Jiaqian]'s Articles
[Zhang,Zhang]'s Articles
[Lin,Ligen]'s Articles
Terms of Use
No data!
Social Bookmark/Share
All comments (0)
No comment.
 

Items in the repository are protected by copyright, with all rights reserved, unless otherwise indicated.