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Identification of Novel Inhibitors against Coactivator Associated Arginine Methyltransferase 1 Based on Virtual Screening and Biological Assays
Joint Authors
Ye, Fei
Zhang, Weiyao
Lu, Wenchao
Xie, Yiqian
Jiang, Hao
Jin, Jia
Luo, Cheng
Source
Issue
Vol. 2016, Issue 2016 (31 Dec. 2016), pp.1-8, 8 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2016-10-27
Country of Publication
Egypt
No. of Pages
8
Main Subjects
Abstract EN
Overexpression of coactivator associated arginine methyltransferase 1 (CARM1), a protein arginine N-methyltransferase (PRMT) family enzyme, is associated with various diseases including cancers.
Consequently, the development of small-molecule inhibitors targeting PRMTs has significant value for both research and therapeutic purposes.
In this study, together with structure-based virtual screening with biochemical assays, two compounds DC_C11 and DC_C66 were identified as novel inhibitors of CARM1.
Cellular studies revealed that the two inhibitors are cell membrane permeable and effectively blocked proliferation of cancer cells including HELA, K562, and MCF7.
We further predicted the binding mode of these inhibitors through molecular docking analysis, which indicated that the inhibitors competitively occupied the binding site of the substrate and destroyed the protein-protein interactions between CARM1 and its substrates.
Overall, this study has shed light on the development of small-molecule CARM1 inhibitors with novel scaffolds.
American Psychological Association (APA)
Ye, Fei& Zhang, Weiyao& Lu, Wenchao& Xie, Yiqian& Jiang, Hao& Jin, Jia…[et al.]. 2016. Identification of Novel Inhibitors against Coactivator Associated Arginine Methyltransferase 1 Based on Virtual Screening and Biological Assays. BioMed Research International،Vol. 2016, no. 2016, pp.1-8.
https://search.emarefa.net/detail/BIM-1098686
Modern Language Association (MLA)
Ye, Fei…[et al.]. Identification of Novel Inhibitors against Coactivator Associated Arginine Methyltransferase 1 Based on Virtual Screening and Biological Assays. BioMed Research International No. 2016 (2016), pp.1-8.
https://search.emarefa.net/detail/BIM-1098686
American Medical Association (AMA)
Ye, Fei& Zhang, Weiyao& Lu, Wenchao& Xie, Yiqian& Jiang, Hao& Jin, Jia…[et al.]. Identification of Novel Inhibitors against Coactivator Associated Arginine Methyltransferase 1 Based on Virtual Screening and Biological Assays. BioMed Research International. 2016. Vol. 2016, no. 2016, pp.1-8.
https://search.emarefa.net/detail/BIM-1098686
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-1098686