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Angew Chem Int Ed Engl. 2022 Jan 26;61(5):e202113020. doi: 10.1002/anie.202113020. Epub 2021 Dec 16.

A Bivalent Activatable Fluorescent Probe for Screening and Intravital Imaging of Chemotherapy-Induced Cancer Cell Death.

Angewandte Chemie (International ed. in English)

Nicole D Barth, Lorena Mendive-Tapia, Ramon Subiros-Funosas, Ouldouz Ghashghaei, Rodolfo Lavilla, Laura Maiorino, Xue-Yan He, Ian Dransfield, Mikala Egeblad, Marc Vendrell

Affiliations

  1. Centre for Inflammation Research, The University of Edinburgh, UK.
  2. Laboratory of Medicinal Chemistry, Faculty of Pharmacy and Institute of Biomedicine (IBUB), University of Barcelona, Spain.
  3. Cold Spring Harbor Laboratory, Cold Spring Harbor, NY, 11724, USA.

PMID: 34762762 DOI: 10.1002/anie.202113020

Abstract

The detection and quantification of apoptotic cells is a key process in cancer research, particularly during the screening of anticancer therapeutics and in mechanistic studies using preclinical models. Intravital optical imaging enables high-resolution visualisation of cellular events in live organisms; however, there are few fluorescent probes that can reliably provide functional readouts in situ without interference from tissue autofluorescence. We report the design and optimisation of the fluorogenic probe Apotracker Red for real-time detection of cancer cell death. The strong fluorogenic behaviour, high selectivity, and excellent stability of Apotracker Red make it a reliable optical reporter for the characterisation of the effects of anticancer drugs in cells in vitro and for direct imaging of chemotherapy-induced apoptosis in vivo in mouse models of breast cancer.

© 2021 The Authors. Angewandte Chemie International Edition published by Wiley-VCH GmbH.

Keywords: apoptosis; breast cancer; chemotherapy; fluorogenic probes; peptides

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