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An exceptionally potent inhibitor of human CD73

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Author(s)

Christine E Bowman, Rafael G da Silva, Amber Pham, Stephen W. Young

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Abstract

We recently reported the initiation of a Phase I clinical trial with AB680, a potent human CD73 inhibitor, being developed for the treatment of solid tumors (NCT03677973). We undertook a detailed kinetic analysis of the interaction between human CD73 and AB680 to determine the mode of inhibition. We found AB680 to be a reversible, slow-onset competitive inhibitor of human CD73 with a Ki of 5 pM. Clinical candidates of this potency are uncommon and deserve special consideration during lead optimization.
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Original languageEnglish
Pages (from-to)3331-3334
Number of pages4
JournalBiochemistry
Volume58
Issue number31
Early online date23 Jul 2019
DOIs
Publication statusPublished - 6 Aug 2019

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