Discovery of a Novel CD39 Inhibitor by DEL Screening

The ATP-adenosine pathway plays a crucial role in regulating immune responses, including those involved in combating tumors. CD39 is an enzyme that breaks down ATP into adenosine. Adenosine, in turn, can suppress the immune system, potentially hindering the body’s ability to fight cancer. By inhibiting CD39, researchers aim to increase ATP levels in the tumor microenvironment and reduce adenosine levels, thus promoting anti-tumor immunity.

DNA-encoded library (DEL) technology is a commonly employed screening platform in both the pharmaceutical industry and academia.  WuXi AppTec scientists contributed to a publication describing the discovery of a novel CD39 small molecule inhibitor (designated as compound 338) through the use of DEL.  Compound 338 exhibited potent inhibition against CD39 as well as moderate anti-proliferative activity toward tumor cells, demonstrating its potential as an anticancer agent.