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2c0i
From Proteopedia
| 2c0i, resolution 2.30Å () | |||||||||
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| Sites: | , , and | ||||||||
| Ligands: | , | ||||||||
| Non-Standard Residues: | |||||||||
| Activity: | Transferase, with EC number and 2.7.10.2 2.7.10.1 and 2.7.10.2 | ||||||||
| Related: | 1ad5, 1bu1, 1qcf, 2c0o, 2c0t, 2hck, 3hck, 4hck, 5hck | ||||||||
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| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||||
SRC FAMILY KINASE HCK WITH BOUND INHIBITOR A-420983
We describe the identification, SAR, and pharmacology of the src-family selective lck inhibitor A-770041 that prolongs the survival of major histocompatibility mismatched allografts in models of solid organ transplant rejection for greater than 65 days.
Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection., Burchat A, Borhani DW, Calderwood DJ, Hirst GC, Li B, Stachlewitz RF, Bioorg Med Chem Lett. 2006 Jan 1;16(1):118-22. Epub 2005 Oct 10. PMID:16216497
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
About this Structure
2c0i is a 2 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA.
Reference
- Burchat A, Borhani DW, Calderwood DJ, Hirst GC, Li B, Stachlewitz RF. Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection. Bioorg Med Chem Lett. 2006 Jan 1;16(1):118-22. Epub 2005 Oct 10. PMID:16216497 doi:10.1016/j.bmcl.2005.09.039
- Borhani DW, Calderwood DJ, Friedman MM, Hirst GC, Li B, Leung AK, McRae B, Ratnofsky S, Ritter K, Waegell W. A-420983: a potent, orally active inhibitor of lck with efficacy in a model of transplant rejection. Bioorg Med Chem Lett. 2004 May 17;14(10):2613-6. PMID:15109663 doi:10.1016/j.bmcl.2004.02.101
