School of Pharmacy, Key Laboratory of Molecular Pharmacology and Drug Evaluation (Yantai University), Ministry of Education, Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Yantai University, Yantai, China.
National Chengdu Center for Safety Evaluation of Drugs, State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, and Collaborative Innovation Center for Biotherapy, Chengdu, China.
Addict Biol. 2020 Sep;25(5):e12808. doi: 10.1111/adb.12808. Epub 2019 Jul 30.
Cocaine addiction is a chronic relapsing brain disorder characterized by compulsive drug seeking. Preliminary study suggested that bromodomain-containing protein 4 (BRD4), an epigenetic reader protein, participates in cocaine-induced reward and neuroplasticity. However, the exact role of BRD4 in cocaine addiction, particularly cocaine relapse, remains elusive. In this study, we found that BRD4 phosphorylation in the nucleus accumbens (NAc) was closely related to the maintenance of cocaine reinforcement and relapse in different cocaine exposure paradigms. Cocaine significantly increased the binding of phosphorylated BRD4 (pBRD4) at the promoter of Gria2 and Bdnf genes in the NAc. (+)JQ1, a selective BRD4 inhibitor, markedly reduced the reinforcement and reinstatement of cocaine-seeking behaviors, which was accompanied by the decreased expressions of GRIA2 and BDNF. Furthermore, chromatin immunoprecipitation assay showed that (+)JQ1 clearly attenuated cocaine-enhanced binding of pBRD4 at the promotor of Gria2 and Bdnf genes. Blockade of casein kinase II significantly attenuated BRD4 phosphorylation and cocaine relapse-like behaviors, suggesting the important role of pBRD4 in modulating cocaine effect. Together, our findings suggest that BRD4 phosphorylation in the NAc modulates multiple addiction-related behaviors of cocaine and particularly relapse to cocaine-seeking behaviors. Inhibition of BRD4 activity may be a novel target against cocaine addiction and relapse.
可卡因成瘾是一种慢性复发性脑部疾病,其特征是强迫性药物寻求。初步研究表明,溴结构域蛋白 4(BRD4)作为一种表观遗传读蛋白,参与可卡因诱导的奖赏和神经可塑性。然而,BRD4 在可卡因成瘾中的确切作用,特别是可卡因复吸,仍然难以捉摸。在这项研究中,我们发现,伏隔核(NAc)中 BRD4 的磷酸化与不同可卡因暴露范式中可卡因强化和复吸的维持密切相关。可卡因显著增加了 NAc 中 Gria2 和 Bdnf 基因启动子上磷酸化 BRD4(pBRD4)的结合。选择性 BRD4 抑制剂(+)JQ1 明显减少了可卡因寻求行为的强化和再现,同时 GRIA2 和 BDNF 的表达减少。此外,染色质免疫沉淀试验表明,(+)JQ1 明显减弱了可卡因增强的 Gria2 和 Bdnf 基因启动子上 pBRD4 的结合。酪蛋白激酶 II 阻断明显减弱了 BRD4 磷酸化和可卡因复吸样行为,表明 pBRD4 在调节可卡因效应中起重要作用。总之,我们的研究结果表明,NAc 中的 BRD4 磷酸化调节可卡因的多种成瘾相关行为,特别是可卡因寻求行为的复吸。抑制 BRD4 活性可能是治疗可卡因成瘾和复吸的新靶点。