An Fc-Small Molecule Conjugate for Targeted Inhibition of the Adenosine 2A Receptor.

ABSTRACT: The adenosine A_2A receptor (A_2A R) is expressed in immune cells, as well as brain and heart tissue, and has been intensively studied as a therapeutic target for multiple disease indications. Inhibitors of the A_2A R have the potential for stimulating immune response, which could be valuable for cancer immune surveillance and mounting a response against pathogens. One well-established potent and selective small molecule A_2A R antagonist, ZM-241385 (ZM), has a short pharmacokinetic half-life and the potential for systemic toxicity due to A_2A R effects in the brain and the heart. In this study, we designed an analogue of ZM and tethered it to the Fc domain of the immunoglobulin IgG3 by using expressed protein ligation. The resulting protei

SUBMITTER: Hsiao PY 

PROVIDER: S-EPMC5292873 | biostudies-literature | 2016 Oct

REPOSITORIES: biostudies-literature