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Updated: Jul 14, 2026
In Vitro and In Vivo Evaluation of Photocontrolled Biologically Active Compounds - Potential Drug Candidates for Cancer Photopharmacology
Published on: September 29, 2023
Design and biological evaluation of photo-switchable inhibitors
Melanie Füllbeck1, Elke Michalsky, Ines Stephanie Jaeger
1Berlin Center of Genome Based Bioinformatics, 3D Dataminig Group, Institute of Molecular Biology and Bioinformatics, University Medicine Berlin-Charité (CBF), Arnimallee 22, D-10117 Berlin, Germany. melanie.fuellbeck@charite.de
Abstract:
Photo-switchable compounds are becoming increasingly popular for a series of biological applications based on the reversible photo-control of structure and function of biomolecules. Three applications for the usage of BODTCM and hemithioindigo as photo-reactive compounds are described here. The structure of the villin headpiece was modified by replacing a part of the backbone with hemithioindigo, aiming at induction of the folding process by irradiation with a defined wavelength. The E-isomer of BODTCM was applied as potential inhibitor of the 12/15-lipoxygenase (12/15-LOX), which is implicated in the pathogenesis of inflammatory diseases. A required death domain for the binding of proapoptotic proteins (e.g. Bak) to the hydrophobic groove of antiapoptotic proteins is the BH3 helix. Inserting hemithioindigo into this short peptide, stabilization towards proteolytic degradation is achieved. Such photo-reactive compounds might be developed as potential drugs for a great variety of diseases.
