An exceptionally potent inhibitor of human CD73
MetadataShow full item record
Altmetrics Handle Statistics
Altmetrics DOI Statistics
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.
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
Copyright © 2019 American Chemical Society. This work has been made available online in accordance with the publisher’s policies. This is the author created, accepted version manuscript following peer review and may differ slightly from the final published version. The final published version of this work is available at https://doi.org/10.1021/acs.biochem.9b00448
DescriptionThe research described in this manuscript was fully funded by Arcus Biosciences, Inc. a publicly traded biotechnology company.
Items in the St Andrews Research Repository are protected by copyright, with all rights reserved, unless otherwise indicated.