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Design and synthesis of a simplified inhibitor for XIAP-BIR3 domain |
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| Authors: | Fernando R Pinacho Crisstomo Yongmei Feng Xuejun Zhu Kate Welsh Jing An John C Reed Ziwei Huang |
| Institution: | aThe Burnham Institute for Medical Research, 10901 N. Torrey Pines Rd., La Jolla, CA 92037, USA |
| 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. |
| Keywords: | XIAP-BIR3 domain Molecular simplification Small molecule |
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