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Fluorescent Artificial Receptor-Based Membrane Assay (FARMA) for Spatiotemporally Resolved Monitoring of Biomembrane Permeability

preprint
submitted on 27.08.2019, 09:44 and posted on 28.08.2019, 17:47 by Frank Biedermann, Garima Ghale, Ghale, Andreas Hennig, Werner M. Nau

The spatiotemporally resolved monitoring of membrane translocation, e.g., of drugs or toxins, has been a long-standing goal. Herein, we introduce the fluorescent artificial receptor-based membrane assay (FARMA), a facile, label-free method. With FARMA, the permeation of more than hundred organic compounds (drugs, toxins, pesticides, neurotransmitters, peptides, etc.) through vesicular phospholipid bilayer membranes has been monitored in real time (µs-h time scale) and with high sensitivity (nM-µM concentration), affording permeability coefficients across an exceptionally large range from 10–9‑10–3 cm s–1. From a fundamental point of view, FARMA constitutes a powerful tool to assess structure-permeability relationships and to test biophysical models for membrane passage. From an applied perspective, FARMA can be extended to high-throughput screening by adaption of the microplate reader format, to spatial monitoring of membrane permeation by microscopy imaging, and to the compartmentalized monitoring of enzymatic activity.

Funding

BI-1805/2-1

NA-686/11

HE 5967/4-1

History

Email Address of Submitting Author

frank.biedermann@kit.edu

Institution

Karlsruhe Institute of Technology (KIT)

Country

Deutschland

ORCID For Submitting Author

0000-0002-1077-6529

Declaration of Conflict of Interest

no conflict of interests

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