Journal
MOLECULAR PHARMACEUTICS
Volume 3, Issue 3, Pages 223-230Publisher
AMER CHEMICAL SOC
DOI: 10.1021/mp060022d
Keywords
bile acids; prodrugs; hASBT; QSAR; SLC10A2; cell culture; transporters
Funding
- NIDDK NIH HHS [DK67530, R01 DK067530-02, R01 DK067530] Funding Source: Medline
- FDA HHS [U01 FD005946] Funding Source: Medline
Ask authors/readers for more resources
A major hurdle impeding the successful clinical development of drug candidates can be poor intestinal permeability. Low intestinal permeability may be enhanced by a prodrug approach targeting membrane transporters in the small intestine. Transporter specificity, affinity, and capacity are three factors in targeted prodrug design. The human apical sodium dependent bile acid transporter (SLC10A2) belongs to the solute carrier family (SLC) of transporters and is an important carrier protein expressed in the small intestine. In spite of its appearing to be an excellent target for prodrug design, few studies have targeted human apical sodium dependent bile acid transporter (hASBT) to improve oral bioavailability. This review discusses bile acids including their chemistry and their absorptive disposition. Additionally, hASBT-mediated prodrug targeting is discussed, including QSAR, in vitro models for hASBT assay, and the current progress in utilizing hASBT as a drug delivery target.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available