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

preprint
submitted on 27.08.2019 and posted on 28.08.2019 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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