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.
Original language | English |
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Pages (from-to) | 3331-3334 |
Number of pages | 4 |
Journal | Biochemistry |
Volume | 58 |
Issue number | 31 |
Early online date | 23 Jul 2019 |
DOIs | |
Publication status | Published - 6 Aug 2019 |
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Rafael Guimaraes da Silva
- School of Biology - Senior Lecturer
- Biomedical Sciences Research Complex
Person: Academic