An exceptionally potent inhibitor of human CD73
Date
06/08/2019Metadata
Show full item recordAbstract
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.
Citation
Bowman , C E , da Silva , R G , Pham , A & Young , S W 2019 , ' An exceptionally potent inhibitor of human CD73 ' , Biochemistry , vol. 58 , no. 31 , pp. 3331-3334 . https://doi.org/10.1021/acs.biochem.9b00448
Publication
Biochemistry
Status
Peer reviewed
ISSN
0006-2960Type
Journal article
Description
The research described in this manuscript was fully funded by Arcus Biosciences, Inc. a publicly traded biotechnology company.Collections
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