Searching with Transporter Pharmacophores

Breast cancer resistance protein BCRP (ABCG2) [12, 68, 86, 89] 

Bile salt export pump BSEP (ABCBll) None  

P-glycoprotein (P-gp, Table 8.2) plays an important role in determining drug distribution of many important drug candidates. P-gp substrates generally have reduced oral drug absorption and enhanced renal and biliary excretion. Limiting the exposure of xenobiotics to P-gp at the blood-brain barrier and placenta] barrier may also be important considerations. The rapid identification of P-gp substrates or 

An additional ABC transporter is the breast cancer resistance protein (BCRP, 

It should be noted that the number of transporters addressed using pharmacophore methods in Tables 8.1 and 8.2 is very small while P-gp has been undoubtedly the most widely studied, enabling many pharmacophores (Table 8.1) and QSAR models to be generated [21]. There are examples of several drug transporters that have been studied in vitro with inhibitor and substrate data that as yet have rarely been used to develop pharmacophores (e.g., organic anion transporters [69, 70] (Table 8.1) from mouse, but not human, have been modeled [71]) or not at all as in the case of the bile salt export pump [72] (Table 8.2). The lack of pharmacophore availability may not be limited to the amount of available data, at least in the case of these two transporters. 

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