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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.

SUBMITTER: Fan W

PROVIDER: S-EPMC6181586 | biostudies-literature | 2018 Oct

REPOSITORIES: biostudies-literature

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

Fan Wei W Zhang Wenting W Alshehri Sameer S Garrison Jered C JC

Chemical communications (Cambridge, England) 20181001 80

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. ...[more]

PMID: 30182093

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