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Discovery of ABT-263, a Bcl-family protein inhibitor: observations on targeting a large protein–protein interaction

21 Aug 2008

Abstract excerpt

BACKGROUND: The discovery of ABT-263, a rationally designed Bcl-2/Bcl-xL inhibitor at present in Phase I clinical trials for cancer, is described. Emphasis is placed on the specific hurdles overcome throughout the discovery process that relate to the nature of the targeted protein-protein interaction (PPI). OBJECTIVE/METHODS: This review draws on observations from the experience of discovering ABT-263 and...

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PMID: 23506184
DOI: 10.1517/17460441.3.9.1123

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