Abstract
Transmembrane efflux pumps play an increasing role in the success of ART. The occurrence of increasing mRNA levels of the efflux pump proteins P-gp and MRP subtypes has been associated with ART therapeutics like PIs and NNRTIs. Moreover, a relation has been suggested of MRP subtypes and CD4 cell counts. So there is a challenge to find selective MRP inhibitors which may reduce MRP-induced drug resistances as well as discussed effects on CD4 cells. We developed novel nonpeptidic inhibitors of important MRP subtypes related to both MRP-mediated resistances as well as reduced cell counts.
Highlights
Transmembrane efflux pumps play an increasing role in the success of ART
Novel MDR-reversing inhibitors of MRP subtypes related to antiretroviral drug resistance and CD4 cell counts
The occurrence of increasing mRNA levels of the efflux pump proteins P-gp and MRP subtypes has been associated with ART therapeutics like PIs and NNRTIs
Summary
Transmembrane efflux pumps play an increasing role in the success of ART. The occurrence of increasing mRNA levels of the efflux pump proteins P-gp and MRP subtypes has been associated with ART therapeutics like PIs and NNRTIs. a relation has been suggested of MRP subtypes and CD4 cell counts. There is a challenge to find selective MRP inhibitors which may reduce MRPinduced drug resistances as well as discussed effects on CD4 cells. We developed novel nonpeptidic inhibitors of important MRP subtypes related to both MRP-mediated resistances as well as reduced cell counts
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