PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 25573101-3 2015 We have previously reported that SK053, a peptidomimetic compound targeting the thioredoxin-thioredoxin reductase system, induces oxidative stress and demonstrates antitumor activity in mice. 2,6-bis-trifluoromethylbenzoic acid 2-(1-(ethoxycarbonylmethylcarbamoyl)-3-methylbutylcarbamoyl)allyl ester 33-38 thioredoxin 1 Mus musculus 80-91 25573101-3 2015 We have previously reported that SK053, a peptidomimetic compound targeting the thioredoxin-thioredoxin reductase system, induces oxidative stress and demonstrates antitumor activity in mice. 2,6-bis-trifluoromethylbenzoic acid 2-(1-(ethoxycarbonylmethylcarbamoyl)-3-methylbutylcarbamoyl)allyl ester 33-38 thioredoxin 1 Mus musculus 92-103 25573101-6 2015 Incubation of tumor cells with SK053 induces increase in BiP, CHOP, and spliced XBP-1 levels, which precede induction of apoptosis. 2,6-bis-trifluoromethylbenzoic acid 2-(1-(ethoxycarbonylmethylcarbamoyl)-3-methylbutylcarbamoyl)allyl ester 31-36 heat shock protein 5 Mus musculus 57-60 25573101-6 2015 Incubation of tumor cells with SK053 induces increase in BiP, CHOP, and spliced XBP-1 levels, which precede induction of apoptosis. 2,6-bis-trifluoromethylbenzoic acid 2-(1-(ethoxycarbonylmethylcarbamoyl)-3-methylbutylcarbamoyl)allyl ester 31-36 DNA-damage inducible transcript 3 Mus musculus 62-66 25573101-6 2015 Incubation of tumor cells with SK053 induces increase in BiP, CHOP, and spliced XBP-1 levels, which precede induction of apoptosis. 2,6-bis-trifluoromethylbenzoic acid 2-(1-(ethoxycarbonylmethylcarbamoyl)-3-methylbutylcarbamoyl)allyl ester 31-36 X-box binding protein 1 Mus musculus 80-85 25573101-7 2015 CHOP-deficient (CHOP(-/-)) mouse embryonic fibroblasts are more resistant to SK053-induced apoptosis as compared with normal fibroblasts indicating that the apoptosis of tumor cells depends on the expression of this transcription factor. 2,6-bis-trifluoromethylbenzoic acid 2-(1-(ethoxycarbonylmethylcarbamoyl)-3-methylbutylcarbamoyl)allyl ester 77-82 DNA-damage inducible transcript 3 Mus musculus 0-4 25573101-9 2015 Altogether, our results indicate that SK053 induces ER stress-associated apoptosis and reveal a link between thioredoxin inhibition and induction of UPR in tumor cells. 2,6-bis-trifluoromethylbenzoic acid 2-(1-(ethoxycarbonylmethylcarbamoyl)-3-methylbutylcarbamoyl)allyl ester 38-43 thioredoxin 1 Mus musculus 109-120 26636537-10 2016 We observed that treatment of lymphoma cells with SK053 triggers formation of covalent PRDX dimers, accumulation of intracellular reactive oxygen species, phosphorylation of ERK1/2 and AKT and leads to cell cycle arrest and apoptosis. 2,6-bis-trifluoromethylbenzoic acid 2-(1-(ethoxycarbonylmethylcarbamoyl)-3-methylbutylcarbamoyl)allyl ester 50-55 peroxiredoxin 1 Homo sapiens 87-91 26636537-10 2016 We observed that treatment of lymphoma cells with SK053 triggers formation of covalent PRDX dimers, accumulation of intracellular reactive oxygen species, phosphorylation of ERK1/2 and AKT and leads to cell cycle arrest and apoptosis. 2,6-bis-trifluoromethylbenzoic acid 2-(1-(ethoxycarbonylmethylcarbamoyl)-3-methylbutylcarbamoyl)allyl ester 50-55 mitogen-activated protein kinase 3 Homo sapiens 174-180 26636537-10 2016 We observed that treatment of lymphoma cells with SK053 triggers formation of covalent PRDX dimers, accumulation of intracellular reactive oxygen species, phosphorylation of ERK1/2 and AKT and leads to cell cycle arrest and apoptosis. 2,6-bis-trifluoromethylbenzoic acid 2-(1-(ethoxycarbonylmethylcarbamoyl)-3-methylbutylcarbamoyl)allyl ester 50-55 AKT serine/threonine kinase 1 Homo sapiens 185-188 26636537-11 2016 Based on site-directed mutagenesis and modeling studies, we propose a mechanism of SK053-mediated PRDX crosslinking, involving double thioalkylation of active site cysteine residues. 2,6-bis-trifluoromethylbenzoic acid 2-(1-(ethoxycarbonylmethylcarbamoyl)-3-methylbutylcarbamoyl)allyl ester 83-88 peroxiredoxin 1 Homo sapiens 98-102 22128876-5 2012 As a result, a new compound 19a (SK053), which inhibits the activity of the Trx-TrxR system and exhibits antitumor activity, was obtained. 2,6-bis-trifluoromethylbenzoic acid 2-(1-(ethoxycarbonylmethylcarbamoyl)-3-methylbutylcarbamoyl)allyl ester 33-38 SLAM family member 7 Homo sapiens 28-31 30002127-3 2018 Here we show that SK053, a thioredoxin inhibitor, induces differentiation and cell death of acute myeloid leukemia cells. 2,6-bis-trifluoromethylbenzoic acid 2-(1-(ethoxycarbonylmethylcarbamoyl)-3-methylbutylcarbamoyl)allyl ester 18-23 thioredoxin Homo sapiens 27-38 30002127-5 2018 Mass spectrometry of proteins precipitated from acute myeloid leukemia cells incubated with biotinylated SK053 used as a bait revealed protein disulfide isomerase as a potential binding partner for the compound. 2,6-bis-trifluoromethylbenzoic acid 2-(1-(ethoxycarbonylmethylcarbamoyl)-3-methylbutylcarbamoyl)allyl ester 105-110 prolyl 4-hydroxylase subunit beta Homo sapiens 135-162 30002127-6 2018 Biochemical, enzymatic and functional assays using fluorescence lifetime imaging confirmed that SK053 binds to and inhibits the activity of protein disulfide isomerase. 2,6-bis-trifluoromethylbenzoic acid 2-(1-(ethoxycarbonylmethylcarbamoyl)-3-methylbutylcarbamoyl)allyl ester 96-101 prolyl 4-hydroxylase subunit beta Homo sapiens 140-167 30002127-8 2018 Molecular dynamics simulation followed by the covalent docking indicated that SK053 binds to the fourth thioredoxin-like domain of protein disulfide isomerase. 2,6-bis-trifluoromethylbenzoic acid 2-(1-(ethoxycarbonylmethylcarbamoyl)-3-methylbutylcarbamoyl)allyl ester 78-83 thioredoxin Homo sapiens 104-115 30002127-8 2018 Molecular dynamics simulation followed by the covalent docking indicated that SK053 binds to the fourth thioredoxin-like domain of protein disulfide isomerase. 2,6-bis-trifluoromethylbenzoic acid 2-(1-(ethoxycarbonylmethylcarbamoyl)-3-methylbutylcarbamoyl)allyl ester 78-83 prolyl 4-hydroxylase subunit beta Homo sapiens 131-158 30002127-10 2018 SK053 increased the levels of CCAAT enhancer-binding protein alpha and upregulated mRNA levels for differentiation-associated genes. 2,6-bis-trifluoromethylbenzoic acid 2-(1-(ethoxycarbonylmethylcarbamoyl)-3-methylbutylcarbamoyl)allyl ester 0-5 CCAAT enhancer binding protein alpha Homo sapiens 30-66 30002127-11 2018 Finally, SK053 decreased the survival of blasts and increased the percentage of cells expressing the maturation-associated CD11b marker in primary cells isolated from bone marrow or peripheral blood of patients with acute myeloid leukemia. 2,6-bis-trifluoromethylbenzoic acid 2-(1-(ethoxycarbonylmethylcarbamoyl)-3-methylbutylcarbamoyl)allyl ester 9-14 integrin subunit alpha M Homo sapiens 123-128