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Rationalized Computer-Aided Design of Matrix-Metalloprotease-Selective Prodrugs

Yes / 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.

Identiferoai:union.ndltd.org:BRADFORD/oai:bradscholars.brad.ac.uk:10454/12041
Date04 May 2017
CreatorsJain, M., Harburn, J.J., Gill, Jason H., Loadman, Paul, Falconer, Robert A., Mooney, C.A., Cobb, S.L., Berry, David J.
Source SetsBradford Scholars
LanguageEnglish
Detected LanguageEnglish
TypeArticle, Accepted manuscript
Rights(c) 2017 ACS. This document is the Accepted Manuscript version of a Published Work that appeared in final form in the Journal of Medicinal Chemistry. To access the final edited and published work see http://dx.doi.org/10.1021/acs.jmedchem.6b01472., Unspecified

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