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Small Molecule Pin1 Inhibitor Blocking NF-B Signaling in Prostate Cancer Cells
Wu, Ke-Jia1; Zhong, Hai-Jing1; Yang, Guanjun1; Wu, Chun2; Huang, Jie-Min1; Li, Guodong1; Ma, Dik-Lung2; Leung, Chung-Hang1
2018-02-02
Source PublicationCHEMISTRY-AN ASIAN JOURNAL
ISSN1861-4728
Volume13Issue:3Pages:275-279
Abstract

Prolyl-isomerase 1 (Pin1) is a conserved enzyme that regulates cell processes such as cell cycle progression, transcriptional regulation, and apoptosis. However, overexpression of Pin1 is correlated with a higher probability of prostate tumor recurrence. We utilized a molecular docking technique to identify Pin1 inhibitors from a database of natural product and natural product-like compounds. The action of the hit compounds against Pin1 activity was studied using multiple methods, including a fluorometric enzymatic assay, co-immunoprecipitation, western blotting, cell thermal shiftm, and other techniques. We have identified compound1 as a natural-product-like inhibitor of Pin1 activity via structure-based virtual screening and showed that compound1 could target Pin1 and disrupt the interaction between Pin1 and the p65 subunit of NF-B in cells. Furthermore, compound1 reduced nuclear p65 (Thr254) phosphorylation and attenuated NF-B activity in cells. Finally, compound1 induced apoptosis in prostate cancer cells. Compound1 represents a natural product-like Pin1 inhibitor that acts via targeting the Pin1-NF-B interaction.

KeywordEnzymes Natural Products Pin1 Protein-protein Interactions Virtual Screening
DOI10.1002/asia.201701216
URLView the original
Indexed BySCI
Language英语
WOS Research AreaChemistry
WOS SubjectChemistry, Multidisciplinary
WOS IDWOS:000424106500012
PublisherWILEY-V C H VERLAG GMBH
The Source to ArticleWOS
Fulltext Access
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Cited Times [WOS]:18   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionInstitute of Chinese Medical Sciences
Affiliation1.University of Macau, Inst Chinese Med Sci, State Key Lab Qual Res Chinese Med, Macau, Peoples R China
2.Hong Kong Baptist Univ, Dept Chem, Kowloon Tong, Hong Kong, Peoples R China
First Author AffilicationUniversity of Macau
Recommended Citation
GB/T 7714
Wu, Ke-Jia,Zhong, Hai-Jing,Yang, Guanjun,et al. Small Molecule Pin1 Inhibitor Blocking NF-B Signaling in Prostate Cancer Cells[J]. CHEMISTRY-AN ASIAN JOURNAL,2018,13(3):275-279.
APA Wu, Ke-Jia.,Zhong, Hai-Jing.,Yang, Guanjun.,Wu, Chun.,Huang, Jie-Min.,...&Leung, Chung-Hang.(2018).Small Molecule Pin1 Inhibitor Blocking NF-B Signaling in Prostate Cancer Cells.CHEMISTRY-AN ASIAN JOURNAL,13(3),275-279.
MLA Wu, Ke-Jia,et al."Small Molecule Pin1 Inhibitor Blocking NF-B Signaling in Prostate Cancer Cells".CHEMISTRY-AN ASIAN JOURNAL 13.3(2018):275-279.
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