Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 60, Issue 10, Pages 4496-4502Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.6b01472
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Funding
- METRC
- Incanthera
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Matrix metalloproteinases (MMPs) are central to cancer development and metastasis. They are highly active in the tumor environment and absent or inactive in normal tissues; therefore they represent viable targets for cancer drug discovery. In this study we evaluated in silico docking to develop MMP-subtype-selective tumor-activated prodrugs. Proof of principle for this therapeutic approach was demonstrated in vitro against an aggressive human glioma model, with involvement of MMPs confirmed using pharmacological inhibition.
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