Peroxynitrite activated drug conjugate systems based on a coumarin scaffold toward the application of theranostics

Two novel drug-conjugates based on a “coumarin linker” have been designed for the synergic release of a therapeutic agent and fluorescent probe for the potential application of theranostics. The drug conjugates; CC-RNS and CI-RNS were designed to be activated by reactive oxygen species or reactive n...

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Päätekijät: Odyniec, M, Han, H, Gardiner, J, Sedgwick, A, He, X, Bull, S, James, T
Aineistotyyppi: Journal article
Kieli:English
Julkaistu: Frontiers Media 2019
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author Odyniec, M
Han, H
Gardiner, J
Sedgwick, A
He, X
Bull, S
James, T
author_facet Odyniec, M
Han, H
Gardiner, J
Sedgwick, A
He, X
Bull, S
James, T
author_sort Odyniec, M
collection OXFORD
description Two novel drug-conjugates based on a “coumarin linker” have been designed for the synergic release of a therapeutic agent and fluorescent probe for the potential application of theranostics. The drug conjugates; CC-RNS and CI-RNS were designed to be activated by reactive oxygen species or reactive nitrogen species (ROS/RNS). The fluorescence OFF-ON response was triggered by the peroxynitrite-mediated transformation of a boronic acid pinacol ester to a phenol moiety with simultaneous release of the therapeutic agents (Confirmed by HRMS). The limit of detection for peroxynitrite using CC-RNS and CI-RNS was 0.29 and 37.2 μM, respectively. Both CC-RNS and CI-RNS demonstrated the ability to visualize peroxynitrite production thus demonstrating the effectiveness of these probes for use as tools to monitor peroxynitrite-mediated drug release in cancer cell lines.
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spelling oxford-uuid:882611d2-c7fb-4abc-928e-ee6fbfaccff42022-03-26T22:15:07ZPeroxynitrite activated drug conjugate systems based on a coumarin scaffold toward the application of theranosticsJournal articlehttp://purl.org/coar/resource_type/c_dcae04bcuuid:882611d2-c7fb-4abc-928e-ee6fbfaccff4EnglishSymplectic Elements at OxfordFrontiers Media2019Odyniec, MHan, HGardiner, JSedgwick, AHe, XBull, SJames, TTwo novel drug-conjugates based on a “coumarin linker” have been designed for the synergic release of a therapeutic agent and fluorescent probe for the potential application of theranostics. The drug conjugates; CC-RNS and CI-RNS were designed to be activated by reactive oxygen species or reactive nitrogen species (ROS/RNS). The fluorescence OFF-ON response was triggered by the peroxynitrite-mediated transformation of a boronic acid pinacol ester to a phenol moiety with simultaneous release of the therapeutic agents (Confirmed by HRMS). The limit of detection for peroxynitrite using CC-RNS and CI-RNS was 0.29 and 37.2 μM, respectively. Both CC-RNS and CI-RNS demonstrated the ability to visualize peroxynitrite production thus demonstrating the effectiveness of these probes for use as tools to monitor peroxynitrite-mediated drug release in cancer cell lines.
spellingShingle Odyniec, M
Han, H
Gardiner, J
Sedgwick, A
He, X
Bull, S
James, T
Peroxynitrite activated drug conjugate systems based on a coumarin scaffold toward the application of theranostics
title Peroxynitrite activated drug conjugate systems based on a coumarin scaffold toward the application of theranostics
title_full Peroxynitrite activated drug conjugate systems based on a coumarin scaffold toward the application of theranostics
title_fullStr Peroxynitrite activated drug conjugate systems based on a coumarin scaffold toward the application of theranostics
title_full_unstemmed Peroxynitrite activated drug conjugate systems based on a coumarin scaffold toward the application of theranostics
title_short Peroxynitrite activated drug conjugate systems based on a coumarin scaffold toward the application of theranostics
title_sort peroxynitrite activated drug conjugate systems based on a coumarin scaffold toward the application of theranostics
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