Prediction of intracellular exposure bridges the gap between target- and cell-based drug discovery

Inadequate target exposure is a major cause of high attrition in drug discovery. Here, we show that a label-free method for quantifying the intracellular bioavailability (F(ic)) of drug molecules predicts drug access to intracellular targets and hence, pharmacological effect. We determined F(ic) in...

Disgrifiad llawn

Wedi'i Gadw mewn:
Manylion Llyfryddiaeth
Cyhoeddwyd yn:Proc Natl Acad Sci U S A
Prif Awduron: Mateus, André, Gordon, Laurie J., Wayne, Gareth J., Almqvist, Helena, Axelsson, Hanna, Seashore-Ludlow, Brinton, Treyer, Andrea, Matsson, Pär, Lundbäck, Thomas, West, Andy, Hann, Michael M., Artursson, Per
Fformat: Artigo
Iaith:Inglês
Cyhoeddwyd: National Academy of Sciences 2017
Pynciau:
PNAS Plus
Mynediad Ar-lein:https://ncbi.nlm.nih.gov/pmc/articles/PMC5544291/
https://ncbi.nlm.nih.gov/pubmed/28701380
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1073/pnas.1701848114
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