Recent advances in drug development targeting bile acids transporters and related disease
10.16438/j.0513-4870.2022-0889
- VernacularTitle:胆汁酸转运体与相关疾病及药物研发进展
- Author:
Xiao-yan DUAN
;
Jin-ping HU
- Publication Type:Research Article
- Keywords:
bile acid;
enterohepatic circulation;
sodium taurocholate cotransporting polypeptide;
bile salt export pump;
apical sodium-dependent bile acid transporter;
organic solute transporter α/β
- From:
Acta Pharmaceutica Sinica
2022;57(12):3576-3586
- CountryChina
- Language:Chinese
-
Abstract:
Bile acids (BAs) are a major component of bile salt, which plays a vital role in the metabolism of lipids in humans. Ninety-five percent of bile acids are recycled by the enterohepatic circulation (EHC), and therefore EHC is essential for bile acid homeostasis. There are four transporters that mediate the transmembrane transport of bile acids, each of which plays an important role in the enterohepatic circulation. Gene defects in bile acid transporters can lead to disorders of the enterohepatic circulation, ultimately leading to clinical phenotypes such as metabolic diseases and even death. Bile transporter expression is altered in patients with various metabolic disease states, suggesting that disruption of bile acid transporters may be a pivotal pathological mechanism for the development of metabolism diseases. Thus, many drugs targeting bile acid transporters are being developed. We provide a concise overview of the progress of bile acid transporters research, discuss the relationship between different bile acid transporters and disease development, and summarize the current progress in drug development targeting bile acid transporters.