西亚试剂：Novel X-linked inhibitor of apoptosis protein inhibitors as

Novel X-linked inhibitor of apoptosis protein inhibitors as probes of apoptosis in biology and medicine

Qi Hu1, Aihua Nie2, Kate Welsh3, Fernando R Pinacho Crisóstomo3, Xuejun Zhu3, Zhengxiang Li1, Jing An3,5, John C Reed3, Liangren Zhang1 and Ziwei Huang3,4,5

We report here a series of new inhibitors of the X-linked inhibitor of apoptosis protein (XIAP protein) based on the SMAC-tetrapeptide AVPI. The structural novelty of these molecules is the presence of the proline mimetic exo-2-azabicyclo[2.2.1]heptane-3-carboxylic acid, leading to analogs with similar activity to the natural ligand peptide. The structure–activity relationship and computational docking studies support the convenience of this unnatural amino acid as a building block to develop new peptides or small molecules targeting the XIAP-BIR3 domain.

Keywords: XIAP-BIR3, AVPI, proline mimetic, exo-2-azabicyclo[2.2.1] heptanes-3-carboxylic acid

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