The discovery of novel tartrate-based TNF-[alpha] converting enzyme (TACE) inhibitors
Journal Article
·
· Bioorg. Med. Chem. Lett.
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.
- Research Organization:
- Advanced Photon Source (APS), Argonne National Laboratory (ANL), Argonne, IL (US)
- Sponsoring Organization:
- USDOE
- OSTI ID:
- 1002634
- Journal Information:
- Bioorg. Med. Chem. Lett., Journal Name: Bioorg. Med. Chem. Lett. Journal Issue: (3) ; 02, 2010 Vol. 20; ISSN 0960-894X
- Country of Publication:
- United States
- Language:
- ENGLISH
Similar Records
Discovery and SAR of hydantoin TACE inhibitors
Discovery of novel hydroxamates as highly potent tumor necrosis factor-[alpha] converting enzyme inhibitors. Part II: Optimization of the S3′ pocket
Characterization of a tumor necrosis factor. alpha. (TNF-. alpha. ) inhibitor: Evidence of immunological cross-reactivity with the TNF receptor
Journal Article
·
Fri Sep 03 00:00:00 EDT 2010
· Bioorg. Med. Chem. Lett.
·
OSTI ID:1002639
Discovery of novel hydroxamates as highly potent tumor necrosis factor-[alpha] converting enzyme inhibitors. Part II: Optimization of the S3′ pocket
Journal Article
·
Fri Oct 01 00:00:00 EDT 2010
· Bioorg. Med. Chem. Lett.
·
OSTI ID:1007158
Characterization of a tumor necrosis factor. alpha. (TNF-. alpha. ) inhibitor: Evidence of immunological cross-reactivity with the TNF receptor
Journal Article
·
Sun Jul 01 00:00:00 EDT 1990
· Proceedings of the National Academy of Sciences of the United States of America; (USA)
·
OSTI ID:6214363