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  Evaluating cellular drug Uptake with fluorescent sensor proteins

Scarabelli, S., Tan, K. T., Griss, R., Hovius, R., D’Alessandro, P. L., Vorherr, T., et al. (2017). Evaluating cellular drug Uptake with fluorescent sensor proteins. Journal of the American Chemical Society, A-G. doi:10.1021/acssensors.7b00331.

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Item Permalink: http://hdl.handle.net/11858/00-001M-0000-002D-C19B-D Version Permalink: http://hdl.handle.net/11858/00-001M-0000-002E-589D-6
Genre: Journal Article

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ACSSensor_e-pup_2017_A.pdf (Any fulltext), 3MB
 
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ACSSensor_e-pup_2017_A_Suppl.pdf (Supplementary material), 822KB
 
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 Creators:
Scarabelli, Silvia, Author
Tan, Kui Thong, Author
Griss, Rudolf, Author
Hovius, Ruud, Author
D’Alessandro, Pier Luca, Author
Vorherr, Thomas, Author
Johnsson, Kai1, Author              
Affiliations:
1Chemical Biology, Max Planck Institute for Medical Research, Max Planck Society, ou_2364732              

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Free keywords: FRET-based sensor protein; HCAII; cellular absorption; cellular clearance; intracellular concentration; p53-HDM2 interaction; peptide therapeutics
 Abstract: We are introducing a new approach to evaluate cellular uptake of drugs and drug candidates into living cells. The approach is based on converting the protein target of a given class of compounds into a fluorescent biosensor. By measuring the binding of different compounds to their cognate biosensor in live cells and comparing these values to those measured in vitro, their cellular uptake and concentrations can be ranked. We demonstrate that our strategy enables the evaluation of the cellular uptake into the cytosol of 2 classes of inhibitors using two different sensor designs; first, sensors comprising the self-labeling protein SNAP conjugated with a chemically modified inhibitor shown for inhibitors of the enzyme human carbonic anhydrase II; and a label-free sensor for inhibitors of protein-protein interactions demonstrated for the protein pair p53-HDM2.

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Language(s): eng - English
 Dates: 2017-05-182017-07-122017-08-02
 Publication Status: Published in print
 Pages: 7
 Publishing info: -
 Table of Contents: -
 Rev. Type: Peer
 Degree: -

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Title: Journal of the American Chemical Society
  Other : J. Am. Chem. Soc.
  Abbreviation : JACS
Source Genre: Journal
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Publ. Info: Washington, DC : American Chemical Society
Pages: - Volume / Issue: - Sequence Number: - Start / End Page: A - G Identifier: ISSN: 0002-7863
CoNE: https://pure.mpg.de/cone/journals/resource/954925376870