Towards Selective Delivery of a Ruthenium(II) Polypyridyl Complex‐Containing Bombesin Conjugate into Cancer Cells

Autor: Maria J. S. A. Silva, Robin Vinck, Youchao Wang, Bruno Saubaméa, Mickaël Tharaud, Elena Dominguez‐Jurado, Johannes Karges, Pedro M. P. Gois, Gilles Gasser
Přispěvatelé: Ecole Nationale Supérieure de Chimie de Paris - Chimie ParisTech-PSL (ENSCP), Université Paris sciences et lettres (PSL), ERC, European Project: 681679, H2020-EU.1.1. - EXCELLENT SCIENCE - European Research Council (ERC),681679,PhotoMedMet(2017)
Jazyk: angličtina
Rok vydání: 2022
Předmět:
Zdroj: ChemBioChem
ChemBioChem, 2022, ⟨10.1002/cbic.202200647⟩
ISSN: 1439-4227
1439-7633
Popis: International audience; There is an increasing number of novel Ru(II) polypyridyl complexes successfully applied as photosensitizers (PSs) for photodynamic therapy (PDT). Despite recent advances on optimized PSs with refined photophysical properties, the lack of tumoral selectivity is often a major hurdle for their clinical development. Herein, classical maleimide and versatile NHS-activated acrylamide strategies were employed to site-selectively conjugate a promising Ru(II) polypyridyl complex to the N-terminal Cys modified Bombesin (BBN) targeting unit. Surprisingly, the decreased cell uptake of these novel Ru-BBN conjugates in cancer cells did not hamper the high phototoxic activity of the Ru-containing bioconjugates and even decrease the toxicity of the constructs in the absence of light irradiation. Overall, while deceiving in terms of selectivity, our new bioconjugates could be still useful for advanced cancer treatment due to their non-toxicity in the dark.
Databáze: OpenAIRE
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