Review Article
Endoplasmic Reticulum Stress: Its Role in Disease and Novel Prospects for Therapy
Table 2
Compounds with potency to ameliorate ER stress.
| Compound | Target/effect | References |
| Chemical chaperones (TUDCA, 4-PBA) | (i) Increased protein folding capacity (ii) Increased ERAD efficiency (iii) Minimized caspase activation | [129, 338–343] |
| Inducers of chaperone activity (lithium, valproate, BIX) | (i) Increased expression and activity of chaperones (ii) Supportive of cell-protective ER stress mechanism | [344–350] |
|
Benzodiazepines | (i) Inhibition of ASK1 function and IRE1-ASK1 signaling (ii) Obstructive to pro-apoptotic ER stress mechanism | [88] |
| Inhibitors of eIF2-alpha phosphatase (salubrinal, Guanabenz) | (i) Inhibition of PP1/GADD34 phosphatase activity (ii) Supportive of attenuated global protein synthesis | [351–353] |
| Antioxidants (BHA, TM2002, and baicalein) | (i) Sequestration of free radicals (ii) Reduction of oxidative stress and apoptosis | [354–357] |
| Inducers of antioxidant pathways (carnosic acid, triterpenoids) | (i) Stimulation of NRF2 pathway (ii) Protection from oxidative stress and resulting apoptosis | [358–363] |
| Stress kinase inhibitors (JNK or p38 inhibitors) | (i) Inhibition of pro-apoptotic JNK or p38 pathways (ii) Antagonism to pro-apoptotic CHOP function | [354, 364–367] |
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BHA: butylated hydroxyanisole. BIX: BiP/GRP78 inducer X (1-(3,4-dihydroxyphenyl)-2-thiocyanate-ethanone). 4-PBA: 4-phenyl butyric acid. TUDCA: tauroursodeoxycholic acid.
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