Publication: Structure-based identification of OATP1B1/3 inhibitors
Structure-based identification of OATP1B1/3 inhibitors
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De Bruyn, T., van Westen, G. J. P., Ijzerman, A. P., Stieger, B., de Witte, P., Augustijns, P. F., & Annaert, P. P. (2013). Structure-based identification of OATP1B1/3 inhibitors. Molecular Pharmacology, 83(6), 1257–1267. https://doi.org/10.1124/mol.112.084152
Abstract
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Several recent studies show that inhibition of the hepatic transport proteins organic anion-transporting polypeptide 1B1 (OATP1B1) and 1B3 (OATP1B3) can result in clinically relevant drug-drug interactions (DDI). To avoid late-stage development drug failures due to OATP1B-mediated DDI, predictive in vitro and in silico methods should be implemented at an early stage of the drug candidate evaluation process. In the present study, we first developed a high-throughput in vitro transporter inhibition assay for the OATP1B subfamily. A tota
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- De Bruyn, Tom
- van Westen, Gerard J P
- Ijzerman, Adriaan P
- Stieger, Bruno
- de Witte, Peter
- Augustijns, Patrick F
- Annaert, Pieter P
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De Bruyn, T., van Westen, G. J. P., Ijzerman, A. P., Stieger, B., de Witte, P., Augustijns, P. F., & Annaert, P. P. (2013). Structure-based identification of OATP1B1/3 inhibitors. Molecular Pharmacology, 83(6), 1257–1267. https://doi.org/10.1124/mol.112.084152
