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Pyrimidine-2,4,6-Triones: A New Effective and Selective Class of Matrix Metalloproteinase Inhibitors
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Frank Grams
Published/Copyright:
June 1, 2005
Abstract
Matrix metalloproteinases (MMPs) are a family of zinc endopeptidases that have been implicated in various disease processes. Different classes of MMP inhibitors, including hydroxamic acids, phosphinic acids and thiols, have been previously described. Most of these mimic peptides and most likely bind in a similar way to the corresponding peptide substrates. Here we desccribe pyrimidinetriones as a completely new class of metalloprotease inhibitors. While the pyrimidinetrione template is used as the zincchelating moiety, the substituents have been optimized to yield inhibitors comparable in their inhibition efficiency of matrix metalloproteinases to hydroxamic acid derivatives such as batimastat. However, they are much more specific for a small subgroup of MMPs, namely the gelatinases (MMP-2 and MMP-9).
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Published Online: 2005-06-01
Published in Print: 2001-08-28
Copyright © 2001 by Walter de Gruyter GmbH & Co. KG
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Articles in the same Issue
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- Paper of the Year 2000: Award to Eva Estébanez-Perpiñá and Pablo Fuentes-Prior
- GABAC Receptors: A Molecular View
- Recent Advances in Plant MAP Kinase Signalling
- The Chemical Biology of Ras Lipidation
- This Is the End: Processing, Editing and Repair at the tRNA 3-Terminus
- Binding of IRE-BP to Its Cognate RNA Sequence: SFM Studies on a Universal RNA Backbone for the Analysis of RNA-Protein Interaction
- PAF67, a Novel Protein That Is Associated with the Initiation-Competent Form of RNA Polymerase I
- Characterization of RNase P Holoenzymes from Methanococcus jannaschii and Methanothermobacter thermoautotrophicus
- Identification of Functional Regions of Guanylate Cyclase-Activating Protein 1 (GCAP1) Using GCAP1/GCIP Chimeras
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