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Design and synthesis of a simplified inhibitor for XIAP-BIR3 domain.

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.

SUBMITTER: Crisostomo FR

PROVIDER: S-EPMC3807767 | biostudies-literature | 2009 Nov

REPOSITORIES: biostudies-literature

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Design and synthesis of a simplified inhibitor for XIAP-BIR3 domain.

Crisóstomo Fernando R Pinacho FR Feng Yongmei Y Zhu Xuejun X Welsh Kate K An Jing J Reed John C JC Huang Ziwei Z

Bioorganic & medicinal chemistry letters 20090917 22

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. ...[more]

PMID: 19819692

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