An Exceptionally Potent Inhibitor of Human CD73 | Zendy

Christine E. Bowman | Zendy; Rafael G. da Silva | Zendy; Amber Pham | Zendy; Stephen W. Young | Zendy

AI Assistant Blog Pricing

Home ZAIA Blog

Open Access

An Exceptionally Potent Inhibitor of Human CD73

Author(s) -

Christine E. Bowman,

Rafael G. da Silva,

Amber Pham,

Stephen W. Young

Publication year - 2019

Publication title -

biochemistry

Language(s) - English

Resource type - Journals

eISSN - 1520-4995

pISSN - 0006-2960

DOI - 10.1021/acs.biochem.9b00448

Subject(s) - potency , pharmacology , chemistry , clinical trial , medicine , biochemistry , in vitro

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 K i of 5 pM. Clinical candidates of this potency are uncommon and deserve special consideration during lead optimization.

The content you want is available to Zendy users.

Already have an account? Click here to sign in.

Having issues? You can contact us here

Accelerating Research