Literature DB >> 31334635

An Exceptionally Potent Inhibitor of Human CD73.

Christine E Bowman1, Rafael G da Silva2, Amber Pham1, Stephen W Young1.   

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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Year:  2019        PMID： 31334635     DOI： 10.1021/acs.biochem.9b00448

Source DB:  PubMed          Journal:  Biochemistry        ISSN： 0006-2960            Impact factor:   3.162


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