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The discovery of novel tartrate-based TNF-alpha converting enzyme (TACE) inhibitors.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2010 Feb 01; Vol. 20 (3), pp. 1189-93. Date of Electronic Publication: 2009 Dec 05. - Publication Year :
- 2010
-
Abstract
- A novel series of TNF-alpha convertase (TACE) inhibitors which are non-hydroxamate have been discovered. These compounds are bis-amides of L-tartaric acid (tartrate) and coordinate to the active site zinc in a tridentate manner. They are selective for TACE over other MMP's. We report the first X-ray crystal structure for a tartrate-based TACE inhibitor.<br /> (Copyright (c) 2009 Elsevier Ltd. All rights reserved.)
- Subjects :
- ADAM17 Protein
Binding Sites
Combinatorial Chemistry Techniques
Crystallography, X-Ray
Humans
Protease Inhibitors metabolism
Protease Inhibitors pharmacology
Tartrates metabolism
Tartrates pharmacology
ADAM Proteins antagonists & inhibitors
ADAM Proteins metabolism
Drug Discovery methods
Protease Inhibitors chemistry
Tartrates chemistry
Tumor Necrosis Factor-alpha metabolism
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 20
- Issue :
- 3
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 20022498
- Full Text :
- https://doi.org/10.1016/j.bmcl.2009.12.004