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dc.contributor.authorBowman, Christine E
dc.contributor.authorda Silva, Rafael G
dc.contributor.authorPham, Amber
dc.contributor.authorYoung, Stephen W.
dc.date.accessioned2020-07-22T23:36:57Z
dc.date.available2020-07-22T23:36:57Z
dc.date.issued2019-08-06
dc.identifier260661707
dc.identifier037843f7-79e2-402d-9367-c887942832fe
dc.identifier85071065546
dc.identifier000480371300003
dc.identifier.citationBowman , 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.9b00448en
dc.identifier.issn0006-2960
dc.identifier.otherORCID: /0000-0002-1308-8190/work/60888245
dc.identifier.urihttps://hdl.handle.net/10023/20314
dc.descriptionThe research described in this manuscript was fully funded by Arcus Biosciences, Inc. a publicly traded biotechnology company.en
dc.description.abstractWe 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.extent4
dc.format.extent516464
dc.language.isoeng
dc.relation.ispartofBiochemistryen
dc.subjectQH301 Biologyen
dc.subjectQD Chemistryen
dc.subjectNDASen
dc.subject.lccQH301en
dc.subject.lccQDen
dc.titleAn exceptionally potent inhibitor of human CD73en
dc.typeJournal articleen
dc.contributor.institutionUniversity of St Andrews. Biomedical Sciences Research Complexen
dc.contributor.institutionUniversity of St Andrews. School of Biologyen
dc.identifier.doi10.1021/acs.biochem.9b00448
dc.description.statusPeer revieweden
dc.date.embargoedUntil2020-07-23


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