Document Detail

Apical sodium dependent bile acid transporter (ASBT, SLC10A2): a potential prodrug target.
MedLine Citation:
PMID:  16749855     Owner:  NLM     Status:  MEDLINE    
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.
Anand Balakrishnan; James E Polli
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Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural; Review    
Journal Detail:
Title:  Molecular pharmaceutics     Volume:  3     ISSN:  1543-8384     ISO Abbreviation:  Mol. Pharm.     Publication Date:    2006 May-Jun
Date Detail:
Created Date:  2006-06-05     Completed Date:  2006-08-08     Revised Date:  2010-09-14    
Medline Journal Info:
Nlm Unique ID:  101197791     Medline TA:  Mol Pharm     Country:  United States    
Other Details:
Languages:  eng     Pagination:  223-30     Citation Subset:  IM    
Department of Pharmaceutical Sciences, School of Pharmacy, University of Maryland, Baltimore, Maryland 21201, USA.
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MeSH Terms
Administration, Oral
Bile Acids and Salts / chemistry,  metabolism*
Biological Availability
Biological Transport
Cell Line
Drug Delivery Systems*
Enterohepatic Circulation
Organic Anion Transporters, Sodium-Dependent / metabolism*
Prodrugs / metabolism*
Quantitative Structure-Activity Relationship
Symporters / metabolism*
Grant Support
Reg. No./Substance:
0/Bile Acids and Salts; 0/Organic Anion Transporters, Sodium-Dependent; 0/Prodrugs; 0/Symporters; 145420-23-1/sodium-bile acid cotransporter

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