- The discovery of potent small molecule cyclic urea activators of STING.
The discovery of potent small molecule cyclic urea activators of STING.
European journal of medicinal chemistry (2022-01-09)
Sourav Basu, Sandip Middya, Monali Banerjee, Rajib Ghosh, David C Pryde, Dharmendra B Yadav, Ritesh Shrivastava, Arjun Surya
PMID34998056
ABSTRACT
STING mediates innate immune responses that are triggered by the presence of cytosolic DNA. Activation of STING to boost antigen recognition is a therapeutic modality that is currently being tested in cancer patients using nucleic-acid based macrocyclic STING ligands. We describe here the discovery of 3,4-dihydroquinazolin-2(1H)-one based 6,6-bicyclic heterocyclic agonists of human STING that activate all known human variants of STING with high potency.
MATERIALS