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. 2022 Feb 16;12(6):2658–2671. doi: 10.1016/j.apsb.2022.02.009

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© 2022 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences. Production and hosting by Elsevier B.V.

This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).

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Scheme 1 — Schematic illustration of brain-targeting SPP-ARV-825 micelle against glioma. The mPEG-PDLLA, SP-PEG-PDLLA and ARV-825 were used for the preparation of SPP-ARV-825 micelle with self-assembly way. SPP-ARV-825 was administrated intravenously and reached tumor site. Subsequently, released ARV-825 acted on BRD4 and induced BRD4 ubiquitination and degradation, further exerting anti-tumor function by cells proliferation inhibition, apoptosis induction and M2 macrophages polarization suppression.