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

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

Research output: Contribution to journal › Article › peer-review

7 Scopus citations

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.

Original language	English (US)
Pages (from-to)	11268-11271
Number of pages	4
Journal	Chemical Communications
Volume	54
Issue number	80
DOIs	https://doi.org/10.1039/c8cc05982a
State	Published - 2018

ASJC Scopus subject areas

Catalysis
Electronic, Optical and Magnetic Materials
Ceramics and Composites
General Chemistry
Surfaces, Coatings and Films
Metals and Alloys
Materials Chemistry

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10.1039/c8cc05982a

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

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.",

author = "Wei Fan and Wenting Zhang and Sameer Alshehri and Garrison, {Jered C.}",

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year = "2018",

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AU - Fan, Wei

AU - Zhang, Wenting

AU - Alshehri, Sameer

AU - Garrison, Jered C.

N1 - Publisher Copyright: © The Royal Society of Chemistry.

PY - 2018

Y1 - 2018

N2 - 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.

AB - 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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DO - 10.1039/c8cc05982a

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JO - Chemical Communications

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

Abstract

ASJC Scopus subject areas

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