Table 2.
UPR Targeting Drugs and their site of action.
| Inositol-Requiring Enzyme 1 (IRE1) | |
| RNase domain inhibition | Toyocamycin [93], MKC3946 [94], 4μ8c [95], 3-Methoxy-6-bromosalicyl-aldehyde [96], STF083010 [97], Doxorubicin [81], MKC8866 [24,30], B-H09 [98], 2-hydroxy-1-naphthaldehyde [99] |
| Q-site | Quercetin [100] |
| Kinase domain inhibition | APY29 [26], Sunitinib [101], Compound 3 [102], KIRA6 [26], KIRA8 [103], UPRM8 [104], GSK2850163 [105], FIRE [106] |
| Not determined | Resveratrol [107], 3,6-DMAD [108] |
| PKR-like ER Kinase (PERK) | |
| Kinase inhibition | GSK2606414 [109], GSK2656157 [110], AMG PERK 44 [84] |
| Kinase activation | Compounds A, B, C [111], DHBDC [112] |
| Inhibit downstream effect of EIF2A | ISRIB [113] |
| Promotes maintenance of EIF2A phosphorylation | Salubrinal [114], Guanlabenz [115] |
| Activating transcription factor 6 (ATF6) | |
| Inhibit nuclear translocation | CEAPIN Class 1 [87] |
| Inhibit transcriptional activity | CEAPIN Class 2 [87], |
| PDI inhibitor | PACMA 31 [116], RB11-ca [117], P1 [118], 16F16 [119] |
| Prevent AFT6 cleavage (Serine protease inhibitor) | AEBSF [120] |
| Not determined | Melatonin [121], Compounds 147, 263 [122] |
| Glucose-regulated protein 78 kDa (GRP78) | |
| Reduce GRP78 levels | OSU-03012 (AR-12) [123], Deoxyverrucosidin [124] Plumbagin [92], HA15 [88], DHA [125], |
| Inhibit GRP78 activity | PAT-SM6 [90] |
| Block GRP78 transcriptional induction | Arctigenin [126] |