Structural highlights
Evolutionary Conservation
Check, as determined by ConSurfDB. You may read the explanation of the method and the full data available from ConSurf.
Publication Abstract from PubMed
A series of IAP antagonists based on thiazole or benzothiazole amide isosteres was designed and synthesized. These compounds were tested for binding to the XIAP-BIR3 and ML-IAP BIR using a fluorescence polarization assay. The most potent of these compounds, 19a and 33b, were found to have K(i)'s of 20-30 nM against ML-IAP and 50-60 nM against XIAP-BIR3.
Antagonists of inhibitor of apoptosis proteins based on thiazole amide isosteres.,Cohen F, Koehler MF, Bergeron P, Elliott LO, Flygare JA, Franklin MC, Gazzard L, Keteltas SF, Lau K, Ly CQ, Tsui V, Fairbrother WJ Bioorg Med Chem Lett. 2010 Apr 1;20(7):2229-33. Epub 2010 Feb 8. PMID:20189383[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
References
- ↑ Cohen F, Koehler MF, Bergeron P, Elliott LO, Flygare JA, Franklin MC, Gazzard L, Keteltas SF, Lau K, Ly CQ, Tsui V, Fairbrother WJ. Antagonists of inhibitor of apoptosis proteins based on thiazole amide isosteres. Bioorg Med Chem Lett. 2010 Apr 1;20(7):2229-33. Epub 2010 Feb 8. PMID:20189383 doi:10.1016/j.bmcl.2010.02.021
