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Table 1 Examples of UPR-targeted cancer drugs in development

From: Unfolded protein response in cancer: the Physician's perspective

Drug Classification/Mechanism Development Stage Disease Indication Reference
Bortezomib Proteasome inhibitor FDA approved Multiple myeloma, mantle-cell lymphoma San et al. [97]
NPI-0052 (salinosporamide A) Irreversible proteasome inhibitor Phase I clinical trials Multiple Myeloma, Advanced malignancies Chauhan et al. [98]
Carfilzomib (PR-171) Selective proteasome inhibitor Phase I, II, III clinical trials Multiple Myeloma, Waldenstrom's Macroglobulinemia O'Connor et al. [99] Lee et al. [100]
PS-341 Selective proteasome inhibitor Phase II Multiple Myeloma Richardson et al. [101]
CEP-18770 Proteasome inhibitor Phase I, II clinical trials and preclinical studies multiple myeloma, Non- Hodgkin's lymphoma Piva et al. [102]
Tanespimycin (17-AAG, (17-Allylamino-17-demethoxygeldanamycin), KOS-953) HSP90 Inhibitor Phase I, II, III clinical trials Gastrointestinal stromal tumors, breast cancer, gynecological, leukemia, lymphoma, melanoma, prostate, renal, thyroid carcinoma, melanoma Richardson et al. [103, 104] Heath et al. [105] Pacey et al. [106]
Alvespimycin (KOS-1022, 17-DMAG) HSP90 Inhibitor Phase I clinical trials and preclinical studies Acute myeloid leukemia, advanced carcinoma Kummar et al. [107] Lancet et al. [108] Pamanathan et al. [109] Zismanov et al. [110]
Retaspimycin (IPI-504) HSP90 Inhibitor Phase II clinical trials Gastrointestinal stromal tumors, nonsmall cell lung, prostate Hanson et al. [111]
PU-H71 HSP90 Inhibitor Preclinical studies Breast cancer, myeloma, myeloproliferative disorder Usmani et al. [84] Caldas-Lopes et al. [112] Marubayashi et al. [113]
SNX-2112 HSP-90 inhibitor Preclinical studies Gastric cancer Bachleitner-Hofmann, et al. [114]
Eeyarestatin I (EerI) Inhibitor of ER-associated degradation (ERAD) Preclinical studies   Cross et al. [115]
Versipelostatin GRP78 inhibitor Preclinical studies   Matsuo et al. [87]
(-)-epigallocatechin gallate (EGCG) GRP78 inhibitor Preclinical studies Breast carcinoma Luo et al. [116]
Epidermal growth factor (EGF)-SubA GRP78-targeting cytotoxin Preclinical murine animal models Prostate tumor Backer et al. [90]
Irestatins IRE1α inhibitor Preclinical studies Multiple Myeloma, Feldman et al. [117]
Delta(9)-Tetrahydrocannabinol (THC) Cannabinoid, activates ER stress and autophagy Phase I clinical trial Glioblastoma multiforme Guzmán et al. [118]