Rationalized Computer-Aided Design of Matrix-Metalloprotease-Selective Prodrugs
dc.contributor.author | Jain, M. | * |
dc.contributor.author | Harburn, J.J. | * |
dc.contributor.author | Gill, Jason H. | * |
dc.contributor.author | Loadman, Paul | * |
dc.contributor.author | Falconer, Robert A. | * |
dc.contributor.author | Mooney, C.A. | * |
dc.contributor.author | Cobb, S.L. | * |
dc.contributor.author | Berry, David J. | * |
dc.date.accessioned | 2017-05-25T13:42:01Z | |
dc.date.available | 2017-05-25T13:42:01Z | |
dc.date.issued | 2017-05-25 | |
dc.identifier.citation | Jain M, Harburn JJ, Gill JH et al (2017) Rationalized Computer-Aided Design of Matrix- Metalloprotease-Selective Prodrugs. Journal of Medicinal Chemistry. 60(10): 4496-4502. | |
dc.identifier.uri | http://hdl.handle.net/10454/12041 | |
dc.description | Yes | |
dc.description.abstract | 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. | |
dc.language.iso | en | |
dc.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. | |
dc.subject | Computer-Aided Design | |
dc.subject | Prodrugs | |
dc.title | Rationalized Computer-Aided Design of Matrix-Metalloprotease-Selective Prodrugs | |
dc.status.refereed | Yes | |
dc.date.application | 2017-05-04 | |
dc.type | Article | |
dc.type.version | Accepted manuscript | |
dc.identifier.doi | https://doi.org/10.1021/acs.jmedchem.6b01472 | |
dc.rights.license | Unspecified | |
refterms.dateFOA | 2018-05-05T00:00:00Z | |
dc.openaccess.status | openAccess |