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An exceptionally potent inhibitor of human CD73
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dc.contributor.author | Bowman, Christine E | |
dc.contributor.author | da Silva, Rafael G | |
dc.contributor.author | Pham, Amber | |
dc.contributor.author | Young, Stephen W. | |
dc.date.accessioned | 2020-07-22T23:36:57Z | |
dc.date.available | 2020-07-22T23:36:57Z | |
dc.date.issued | 2019-08-06 | |
dc.identifier | 260661707 | |
dc.identifier | 037843f7-79e2-402d-9367-c887942832fe | |
dc.identifier | 85071065546 | |
dc.identifier | 000480371300003 | |
dc.identifier.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 | en |
dc.identifier.issn | 0006-2960 | |
dc.identifier.other | ORCID: /0000-0002-1308-8190/work/60888245 | |
dc.identifier.uri | https://hdl.handle.net/10023/20314 | |
dc.description | The research described in this manuscript was fully funded by Arcus Biosciences, Inc. a publicly traded biotechnology company. | en |
dc.description.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. | |
dc.format.extent | 4 | |
dc.format.extent | 516464 | |
dc.language.iso | eng | |
dc.relation.ispartof | Biochemistry | en |
dc.subject | QH301 Biology | en |
dc.subject | QD Chemistry | en |
dc.subject | NDAS | en |
dc.subject.lcc | QH301 | en |
dc.subject.lcc | QD | en |
dc.title | An exceptionally potent inhibitor of human CD73 | en |
dc.type | Journal article | en |
dc.contributor.institution | University of St Andrews. Biomedical Sciences Research Complex | en |
dc.contributor.institution | University of St Andrews. School of Biology | en |
dc.identifier.doi | 10.1021/acs.biochem.9b00448 | |
dc.description.status | Peer reviewed | en |
dc.date.embargoedUntil | 2020-07-23 |
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