Increasing time on target: utilization of inhibitors of cysteine cathepsins to enhance the tumor retention of receptor-targeted agents

Wei Fan; Wenting Zhang; Sameer Alshehri; Jered C. Garrison

doi:10.1039/C8CC05982A

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Increasing time on target: utilization of inhibitors of cysteine cathepsins to enhance the tumor retention of receptor-targeted agents†

Wei Fan,

‡^ab Wenting Zhang,

‡^ab Sameer Alshehri^ab and Jered C. Garrison

*^abcd

Author affiliations

* Corresponding authors

^a Department of Pharmaceutical Sciences, University of Nebraska Medical Center, 985830 Nebraska Medical Center, Omaha, NE 68198, USA
E-mail: jcgarrison@unmc.edu

^b Center for Drug Delivery and Nanomedicine, University of Nebraska Medical Center, 985830 Nebraska Medical Center, Omaha, NE 68198, USA

^c Department of Biochemistry and Molecular Biology, University of Nebraska Medical Center, 985870 Nebraska Medical Center, Omaha, NE 68198, USA

^d Eppley Cancer Center, University of Nebraska Medical Center, 985950 Nebraska Medical Center, Omaha, NE 68198, USA

Abstract

We report a strategy of utilizing irreversible cysteine cathepsin inhibitor as trapping agent to increase the tumor residence time of receptor-targeted agents. The targeted constructs incorporating these cysteine cathepsin trapping agents were able to form high molecular weight adducts with intracellular cysteine cathepsins, thus achieving superior retention in tumor tissues.

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Article information

DOI: https://doi.org/10.1039/C8CC05982A
Article type: Communication
Submitted: 24 Jul 2018
Accepted: 29 Aug 2018
First published: 30 Aug 2018

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Chem. Commun., 2018,54, 11268-11271

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Increasing time on target: utilization of inhibitors of cysteine cathepsins to enhance the tumor retention of receptor-targeted agents

W. Fan, W. Zhang, S. Alshehri and J. C. Garrison, Chem. Commun., 2018, 54, 11268 DOI: 10.1039/C8CC05982A

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Chemical Communications

Increasing time on target: utilization of inhibitors of cysteine cathepsins to enhance the tumor retention of receptor-targeted agents†

Abstract

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Increasing time on target: utilization of inhibitors of cysteine cathepsins to enhance the tumor retention of receptor-targeted agents

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