Abstract
Based on tetrapeptide AVPI, we were able to design and synthesize a new simplified scaffold to inhibit the BIR3 domain of the XIAP protein at low micromolar range. The uncomplicated synthesis and the binding activity of the molecule disclosed here represent an attractive alternative to develop new compounds targeting the protein-protein interaction of XIAP/caspase9.
Publication types
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Research Support, N.I.H., Extramural
MeSH terms
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Apoptosis
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Crystallography, X-Ray
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Drug Design
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Humans
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Inhibitor of Apoptosis Proteins*
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Mitochondrial Proteins
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Oligopeptides / chemistry*
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Protein Conformation
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Protein Structure, Tertiary
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Structure-Activity Relationship*
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X-Linked Inhibitor of Apoptosis Protein / administration & dosage*
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X-Linked Inhibitor of Apoptosis Protein / antagonists & inhibitors
Substances
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Inhibitor of Apoptosis Proteins
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Mitochondrial Proteins
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Oligopeptides
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X-Linked Inhibitor of Apoptosis Protein
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XIAP protein, human