Dataset for "Targeted, receptor-mediated delivery of a masked ᴅ-amino acid cell penetrating peptide for cell-specific phototoxicity"

List, Moritz; Jülke, Eva-Maria; Beck-Sickinger, Annette G.

Dataset for "Targeted, receptor-mediated delivery of a masked ᴅ-amino acid cell penetrating peptide for cell-specific phototoxicity"

Description of the data datacite.resourceType	This dataset includes raw assay data, unmodified chromatograms, and unprocessed microscopy images of the research article "Targeted, receptor-mediated delivery of a masked ᴅ-amino acid cell penetrating peptide for cell-specific phototoxicity".
Type of the data datacite.resourceTypeGeneral	Collection
Total size of the dataset datacite.size	260284948
Author dc.contributor.author	List, Moritz
Author dc.contributor.author	Jülke, Eva-Maria
Author dc.contributor.author	Beck-Sickinger, Annette G.
Upload date dc.date.accessioned	2025-11-06T08:43:04Z
Publication date dc.date.available	2025-11-06T08:43:04Z
Data of data creation dc.date.created	2025
Publication date dc.date.issued	2025-11-06
Abstract of the dataset dc.description.abstract	Photodynamic therapy is an innovative treatment option for cancer, but current approaches are limited by poor tumor selectivity and low uptake. Here, we introduce a novel concept for a targeted phototoxic peptide, in which a lysosomally activatable payload is delivered selectively by receptor-mediated endocytosis. For the payload, 6-carboxytetramethylrhodamine (TMR) was attached to an activatable cell penetrating peptide. The regular activity of the CPP was blocked by electrostatic interactions with a poly-glutamate sequence but could be restored through cleavage by the lysosomal protease cathepsin B both in vitro and in cells. The unmasked CPP can then bind to the negatively charged lysosomal membrane, and upon irradiation, TMR generates reactive oxygen species (ROS) that disrupt the integrity of the membrane. This leads to a release of lysosomal contents into the cytosol which subsequently induces cell death. To achieve targeted delivery, the activatable payload was conjugated to chemerin-9, a high-affinity ligand for the chemokine-like receptor 1 (CMKLR1), a G protein-coupled receptor overexpressed in various cancers. Through this receptor-targeted approach, the peptide accumulates in CMKLR1-expressing cells while the lysosomal activation completely prevented off-target toxicity. Notably, this strategy enables even a weak photosensitizer like TMR to achieve potent cytotoxicity through lysosomal targeting. This approach represents an advancement in improving the selectivity and efficacy of photodynamic therapy and holds promise for the development of novel cancer therapies. Furthermore, the concept opens possibilities for specific intracellular delivery of peptides or proteins.
Public reference to this page dc.identifier.uri	https://opara.zih.tu-dresden.de/handle/123456789/1795
Public reference to this page dc.identifier.uri	https://doi.org/10.25532/OPARA-999
Publisher dc.publisher	Universität Leipzig
Licence dc.rights	Attribution 4.0 International	en
URI of the licence text dc.rights.uri	http://creativecommons.org/licenses/by/4.0/
Specification of the discipline(s) dc.subject.classification	2
Title of the dataset dc.title	Dataset for "Targeted, receptor-mediated delivery of a masked ᴅ-amino acid cell penetrating peptide for cell-specific phototoxicity"

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