non-nucleotide STING agonist
novel mechanism for STING activation
from micromolar HTS hit
Nature
University of Texas Southwestern Medical Center, Dallas, TX
Context. ”Compound 53” (University of Texas Southwestern Medical Center) is a stimulator of interferon (IFN) genes (STING) agonist. STING agonists have been heavily pursued in cancer immunology as increasing data suggests that the efficacy of immunotherapy can be enhanced by proteins such as STING that can induce a strong innate immune response through regulation of type I interferon signaling. We have previously highlighted several STING agonists, including Merk’s MK-1454 (ulevostinag), which is currently the most advanced STING agonist and in Ph. II studies, Aduro’s ADU-S100 which was terminated at Ph. II studies due to poor efficacy, and Eisai’s E7766. “Compound 53” targets a unique pocket in the protein that allows for a potentiated effect since endogenous cGAMP is also able…