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. 2021 Feb 9;15:621501. doi: 10.3389/fnins.2021.621501

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.