| Structural highlights
3q2g is a 2 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
| | Method: | X-ray diffraction, Resolution 2.3Å |
| Ligands: | , , , , , |
| Resources: | FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT |
Function
ATS1_HUMAN Cleaves aggrecan, a cartilage proteoglycan, and may be involved in its turnover (By similarity). Has angiogenic inhibitor activity. Active metalloprotease, which may be associated with various inflammatory processes as well as development of cancer cachexia. May play a critical role in follicular rupture.[1]
Publication Abstract from PubMed
Two series of N-hydroxyformamide inhibitors of ADAM-TS4 were identified from screening compounds previously synthesised as inhibitors of matrix metalloproteinase-13 (collagenase-3). Understanding of the binding mode of this class of compound using ADAM-TS1 as a structural surrogate has led to the discovery of potent and very selective inhibitors with favourable DMPK properties. Synthesis, structure-activity relationships, and strategies to improve selectivity and lower in vivo metabolic clearance are described.
The design and synthesis of novel N-hydroxyformamide inhibitors of ADAM-TS4 for the treatment of osteoarthritis.,De Savi C, Pape A, Cumming JG, Ting A, Smith PD, Burrows JN, Mills M, Davies C, Lamont S, Milne D, Cook C, Moore P, Sawyer Y, Gerhardt S Bioorg Med Chem Lett. 2011 Mar 1;21(5):1376-81. Epub 2011 Jan 18. PMID:21300546[2]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ Vazquez F, Hastings G, Ortega MA, Lane TF, Oikemus S, Lombardo M, Iruela-Arispe ML. METH-1, a human ortholog of ADAMTS-1, and METH-2 are members of a new family of proteins with angio-inhibitory activity. J Biol Chem. 1999 Aug 13;274(33):23349-57. PMID:10438512
- ↑ De Savi C, Pape A, Cumming JG, Ting A, Smith PD, Burrows JN, Mills M, Davies C, Lamont S, Milne D, Cook C, Moore P, Sawyer Y, Gerhardt S. The design and synthesis of novel N-hydroxyformamide inhibitors of ADAM-TS4 for the treatment of osteoarthritis. Bioorg Med Chem Lett. 2011 Mar 1;21(5):1376-81. Epub 2011 Jan 18. PMID:21300546 doi:10.1016/j.bmcl.2011.01.036
|
