Ren Tengqi, Pang Liwei, Dai Wanlin, Wu Shuodong, Kong Jing
Department of General Surgery, Shengjing Hospital of China Medical University, Shenyang, Liaoning, China.
Innovation Institute of China Medical University, Shenyang, Liaoning, China.
Clin Res Hepatol Gastroenterol. 2021 Nov;45(6):101641. doi: 10.1016/j.clinre.2021.101641. Epub 2021 Feb 10.
The bile salt export pump (BSEP/ABCB11) is located on the apical membrane and mediates the secretion of bile salts from hepatocytes into the bile. BSEP-mediated bile salt efflux is the rate-limiting step of bile salt secretion and the main driving force of bile flow. BSEP drives and maintains the enterohepatic circulation of bile salts. In recent years, research efforts have been focused on understanding the physiological and pathological functions and regulatory mechanisms of BSEP. These studies elucidated the roles of farnesoid X receptor (FXR), AMP-activated protein kinase (AMPK), liver receptor homolog-1(LRH-1) and nuclear factor erythroid 2-related factor 2 (Nrf-2) in BSEP expression and discovered some regulatory factors which participate in its post-transcriptional regulation. A series of liver diseases have also been shown to be related to BSEP expression and dysfunction, such as cholestasis, drug-induced liver injury, and gallstones. Here, we systematically review and summarize recent literature on BSEP structure, physiological functions, regulatory mechanisms, and related diseases.
胆盐输出泵（BSEP/ABCB11）位于肝细胞膜顶端，介导胆盐从肝细胞分泌入胆汁。BSEP介导的胆盐外排是胆盐分泌的限速步骤，也是胆汁流动的主要驱动力。BSEP驱动并维持胆盐的肠肝循环。近年来，研究工作聚焦于了解BSEP的生理和病理功能及调控机制。这些研究阐明了法尼醇X受体（FXR）、AMP激活的蛋白激酶（AMPK）、肝脏受体同源物1（LRH-1）和核因子红细胞2相关因子2（Nrf-2）在BSEP表达中的作用，并发现了一些参与其转录后调控的调节因子。一系列肝脏疾病也被证明与BSEP表达及功能障碍有关，如胆汁淤积、药物性肝损伤和胆结石。在此，我们系统地回顾和总结了关于BSEP结构、生理功能、调控机制及相关疾病的近期文献。
