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. 2019 Aug 6;58(31):3331-3334.
doi: 10.1021/acs.biochem.9b00448. Epub 2019 Jul 23.

An Exceptionally Potent Inhibitor of Human CD73

Christine E Bowman  1 , Rafael G da Silva  2 , Amber Pham  1 , Stephen W Young  1
Affiliations

An Exceptionally Potent Inhibitor of Human CD73

Christine E Bowman et al. Biochemistry. .

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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