Sanguinarine targets BRD4 to suppress cell proliferation and migration in clear cell renal cell carcinoma.

Authors

Yibo Wen, Yue Song, Yuan Ma, Jianguo Wen, Jinghua Yang

Published in

Journal of biochemical and molecular toxicology. Pages e23451. Jul 02, 2023. Epub Jul 02, 2023.

Abstract

Sanguinarine is an alkaloid with diverse biological activities, nevertheless, whether it can target epigenetic modifiers remains unknown. In this study, sanguinarine was characterized as a strong BRD4 inhibitor with IC₅₀  = 361.3 nM against BRD4 (BD1) and IC₅₀  = 302.7 nM against BRD4 (BD2) that can inactivate BRD4 reversibly. Additional cellular assays suggested that sanguinarine can bind BRD4 in human clear cell renal cell carcinoma (ccRCC) cell line 786-O and inhibit cell growth with IC₅₀ (24 h) = 0.6752 μM and IC₅₀ (48 h) = 0.5959 μM in a BRD4 dependent manner partially. Meanwhile, sanguinarine can inhibit the migration of 786-O cells in vitro and in vivo, and reverse epithelial-mesenchymal transition. Moreover, it can inhibit 786-O cells proliferation in vivo in a BRD4 dependent manner partially. In sum, our study identified BRD4 as a new target of sanguinarine, and sanguinarine may serve as a potential therapeutic agent against ccRCC.

PMID:
37393519
Bibliographic data and abstract were imported from PubMed on 02 Jul 2023.

Read full publication at:
Please sign in to see all details.

Stats

1-terrible, 9-excellent. How would you rate this publication? Sign in in to submit your rating.

Post a comment

You need to be signed in to post comments. You can sign in here.

Comments

There are no comments yet.