Non-peptidic small molecule inhibitors of XIAP.

Park CM, Sun C, Olejniczak ET, Wilson AE, Meadows RP, Betz SF, Elmore SW, Fesik SW
Bioorg Med Chem Lett. 2005 15 (3): 771-5

PMID: 15664855 · DOI:10.1016/j.bmcl.2004.11.010

Non-peptidic small molecule SMAC mimetics were designed and synthesized that bind to the BIR3 domain of XIAP using structure-based design. Substituted five-membered heterocycles such as thiazoles and imidazoles were identified that serve as replacements for peptide fragments of the lead.

MeSH Terms (11)

Binding Sites Drug Design Heterocyclic Compounds Humans Imidazoles Ligands Magnetic Resonance Spectroscopy Proteins Structure-Activity Relationship Thiazoles X-Linked Inhibitor of Apoptosis Protein

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