Molecular Recognition of the Catalytic Zinc(II) Ion in MMP-13: Structure-Based Evolution of an Allosteric Inhibitor to Dual Binding Mode Inhibitors with Improved Lipophilic Ligand Efficiencies

Molecular Recognition of the Catalytic Zinc(II) Ion in MMP-13: Structure-Based Evolution of an Allosteric Inhibitor to Dual Binding Mode Inhibitors with Improved Lipophilic Ligand Efficiencies

Matrix metalloproteinases (MMPs) are a class of zinc dependent endopeptidases which play a crucial role in a multitude of severe diseases such as cancer and osteoarthritis. We employed MMP-13 as the target enzyme for the structure-based design and synthesis of inhibitors able to recognize the cataly...

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Bibliographic Details
Main Authors: Thomas Fischer, Rainer Riedl
Format: Article
Language:English
Published: MDPI AG 2016-03-01
Series:International Journal of Molecular Sciences
Subjects:
structure-based drug design
organic synthesis
matrix metalloproteinase inhibitors
molecular recognition
weak zinc binders
lipophilic ligand efficiency
Online Access:http://www.mdpi.com/1422-0067/17/3/314

Internet

http://www.mdpi.com/1422-0067/17/3/314

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