ArticleBioconjugate chemistry2013
Synthesis and characterization of Pt(IV) fluorescein conjugates to investigate Pt(IV) intracellular transformations.
Article in Bioconjugate chemistry, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed, 71 citations in OpenAlex.
- Pt(IV) Complexes as Anticancer Drugs and Their Relationship with Oxidative Stress.Biomedicines · 2025Review
- Recent Advances on Pt-Based Compounds for Theranostic Applications.Molecules (Basel, Switzerland) · 2024Review
- Pt(IV) Complexes in the Search for Novel Platinum Prodrugs with Promising Activity.Topics in current chemistry (Cham) · 2024Review
- Article
- Regium-π Bonds Involving Nucleobases: Theoretical Study and Biological Implications.Inorganic chemistry · 2023Article
- Cell-permeable lanthanide-platinum(IV) anti-cancer prodrugs.Dalton transactions (Cambridge, England : 2003) · 2021Article
- Gd(iii)-Pt(iv) theranostic contrast agents for tandem MR imaging and chemotherapy.Chemical science · 2020Article
- Platinum(IV)-Ferrocene Conjugates and Their Cyclodextrin Host-Guest Complexes.Inorganic chemistry · 2019Article
- Controlled in-cell activation of RNA therapeutics using bond-cleaving bio-orthogonal chemistry.Chemical science · 2017Article
- Measurement of drug-target engagement in live cells by two-photon fluorescence anisotropy imaging.Nature protocols · 2017Article
- Conjugation of cisplatin analogues and cyclooxygenase inhibitors to overcome cisplatin resistance.ChemMedChem · 2015Article
- Redox-triggered self-assembly of gadolinium-based MRI probes for sensing reducing environment.Bioconjugate chemistry · 2014Article
- Pt(IV) prodrugs designed to bind non-covalently to human serum albumin for drug delivery.Journal of the American Chemical Society · 2014Article
- Copper-free click-chemistry platform to functionalize cisplatin prodrugs.Chemistry (Weinheim an der Bergstrasse, Germany) · 2014Article
- Conjugates of cisplatin and cyclooxygenase inhibitors as potent antitumor agents overcoming cisplatin resistance.ChemMedChem · 2014Article
- Facile Synthesis of a Pt(IV) Prodrug of Cisplatin and Its IntrinsicallyIndian journal of nuclear medicine : IJNM : the official journal of the Society of Nuclear Medicine, IndiaArticle
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
Pt(IV) anticancer compounds typically operate as prodrugs that are reduced in the hypoxic environment of cancer cells, losing two axial ligands in the process to generate active Pt(II) species. Here we report the synthesis of two fluorescent Pt(IV) prodrugs of cisplatin in order to image and evaluate the Pt(IV) reduction process in simulated and real biological environments. Treatment of the complexes dissolved in PBS buffer with reducing agents typically encountered in cells, glutathione or ascorbate, afforded a 3- to 5-fold fluorescence turn-on owing to reduction and loss of their fluorescein-based axial ligands, which are quenched when bound to platinum. Both Pt(IV) conjugates displayed moderate cytotoxicity against human cancer cell lines, with IC50 values higher than that of cisplatin. Immunoblotting and DNA flow cytometry analyses of one of the complexes, Pt(IV)FL2, revealed that it damages DNA, causes cell cycle arrest in S or G2/M depending on exposure time, and ultimately triggers apoptotic cell death. Fluorescence microscopic studies prove that Pt(IV)FL2 enters cells intact and undergoes reduction intracellularly. The results are best interpreted in terms of a model in which the axial fluorescein ligands are expelled through lysosomes, with the platinum(II) moiety generated in the process binding to genomic DNA, which results in cell death.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.