Photoactivatable and photolabile pharmacophores: lessons learned from capsaicin

Abstract

Light-controlled molecules have become valuable tools for studying biological systems offering an unparalleled control in space and time. Specifically, the remote-controllable (de)activation of small molecules is attractive both to study molecular processes from a fundamental point of view and to develop future precision therapeutics. While pronounced changes through light-induced cleavage of photolabile protecting groups and the accompanying liberation of bioactive small molecules have become a highly successful strategy, approaches that focus solely on the revert process, i.e. the photochemical deactivation of bioactive agents, are sparse. In this work, we studied whether a given bioactive compound could be made photolability by structural design. We thus used the example of capsaicinoids, which control the transient receptor potential cation channel subfamily V member 1 (TRPV1), to generate both suitable light activation and deactivation strategies.

Graphical abstract: Photoactivatable and photolabile pharmacophores: lessons learned from capsaicin

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Article information

Article type
Paper
Submitted
16 May 2025
Accepted
18 Jul 2025
First published
19 Jul 2025
This article is Open Access
Creative Commons BY license

RSC Chem. Biol., 2025, Advance Article

Photoactivatable and photolabile pharmacophores: lessons learned from capsaicin

N. Imse, L. Rojas, C. Gil Herrero, S. Thallmair, J. Rhee and N. A. Simeth, RSC Chem. Biol., 2025, Advance Article , DOI: 10.1039/D5CB00124B

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