TABLE 3.
STING modulators.
Compound | Affinity | Disease model | Disease outcome | References |
STING activator CDNs | mSTING; Kd∼110 nM, hSTING; ∼4.59 nM | Viral infection+; Cancer+; EAE+ | Protective against viral infections; shows anti-tumour activity in mouse models of various cancers; delays EAE and reduce the overall disease severity | Burdette et al., 2011; Chandra et al., 2014; Lemos et al., 2014; Li et al., 2014 |
STING activator DMXAA | mSTING; Kd∼130 nM | Cancer+ | Shows potent anti-tumour activity in mouse models of lung cancer and mesothelioma | Conlon et al., 2013; Kim et al., 2013 |
STING activator CMA | mSTING; Kd:3.5 μM | SAH– | Exacerbates neuronal damage and neurobehavioral deficits in a mouse model of SAH | Zhang et al., 2015; Peng et al., 2020 |
STING activator GCV | m/hSTING; Kd:N/A | EAE+; Viral infection+ | Attenuates EAE pathology in mice; protective against cytomegalovirus infections | Mathur et al., 2017 |
STING inhibitor GSK2656157 | N/A | TBI+ | Reduces lesion volume and improves neurobehavioral outcome | Sen et al., 2020 |
STING inhibitor C-176 | mSTING; IC50 < 50 nM | AGS+; SAH+ | Ameliorates STING associated-inflammation in AGS mouse model; reduces brain oedema, neuronal damage and neuroinflammatory response in SAH mouse model | Haag et al., 2018; Peng et al., 2020 |
Kd (dissociation constant) indicates the affinity of STING binding to the compound ligand. Half-maximal inhibitory concentration (IC50) is the concentration of an inhibitor where the response (or binding) is reduced by half. (+) denotes beneficial and (–) denotes detrimental effects of STING compound in disease outcome. mSTING, mouse STNG; hSTING, human STING.