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Synonyms: compound 5h [PMID: 16426848] | TMI-05 | TMI005
Compound class: Synthetic organic
Comment: Apratastat (TMI-005) is an orally active dual TACE (ADAM17)/MMP13 inhibitor that was developed for the potential treatment of inflammation . TACE = TNF α-converting enzyme, which is a well validated therapeutic target for the treatment of rheumatoid arthritis. Inhibition of MMP13 (a peptidase that preferentially degrades type II collagen and aggrecan) is relevant since this is predicted to prevent the degradation of cartilage in rheumatoid arthritis [1,4].
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. Konttinen YT, Ainola M, Valleala H, Ma J, Ida H, Mandelin J, Kinne RW, Santavirta S, Sorsa T, López-Otín C et al.. (1999)
Analysis of 16 different matrix metalloproteinases (MMP-1 to MMP-20) in the synovial membrane: different profiles in trauma and rheumatoid arthritis.
Ann. Rheum. Dis., 58 (11): 691-7. [PMID:10531073]
2. Levin JI, Chen JM, Laakso LM, Du M, Schmid J, Xu W, Cummons T, Xu J, Jin G, Barone D et al.. (2006)
Acetylenic TACE inhibitors. Part 3: Thiomorpholine sulfonamide hydroxamates.
Bioorg. Med. Chem. Lett., 16 (6): 1605-9. [PMID:16426848]
3. Thabet MM, Huizinga TW. (2006)
Drug evaluation: apratastat, a novel TACE/MMP inhibitor for rheumatoid arthritis.
Curr Opin Investig Drugs, 7 (11): 1014-9. [PMID:17117591]
4. Yoshihara Y, Nakamura H, Obata K, Yamada H, Hayakawa T, Fujikawa K, Okada Y. (2000)
Matrix metalloproteinases and tissue inhibitors of metalloproteinases in synovial fluids from patients with rheumatoid arthritis or osteoarthritis.
Ann. Rheum. Dis., 59 (6): 455-61. [PMID:10834863]