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Mechanistic evaluation and transcriptional signature of a glutathione S-transferase omega 1 inhibitor.

Ramkumar K, Samanta S, Kyani A, Yang S, Tamura S, Ziemke E, Stuckey JA, Li S, Chinnaswamy K, Otake H, Debnath B, Yarovenko V, Sebolt-Leopold JS, Ljungman M, Neamati N
Nat Commun 7 13084 (2016)
Related entries: 4yqm, 4yqv

Cited: 23 times
EuropePMC logo PMID: 27703239

Abstract

Glutathione S-transferase omega 1 (GSTO1) is an atypical GST isoform that is overexpressed in several cancers and has been implicated in drug resistance. Currently, no small-molecule drug targeting GSTO1 is under clinical development. Here we show that silencing of GSTO1 with siRNA significantly impairs cancer cell viability, validating GSTO1 as a potential new target in oncology. We report on the development and characterization of a series of chloroacetamide-containing potent GSTO1 inhibitors. Co-crystal structures of GSTO1 with our inhibitors demonstrate covalent binding to the active site cysteine. These potent GSTO1 inhibitors suppress cancer cell growth, enhance the cytotoxic effects of cisplatin and inhibit tumour growth in colon cancer models as single agent. Bru-seq-based transcription profiling unravelled novel roles for GSTO1 in cholesterol metabolism, oxidative and endoplasmic stress responses, cytoskeleton and cell migration. Our findings demonstrate the therapeutic utility of GSTO1 inhibitors as anticancer agents and identify the novel cellular pathways under GSTO1 regulation in colorectal cancer.

Articles - 4yqu mentioned but not cited (2)

  1. Mechanistic evaluation and transcriptional signature of a glutathione S-transferase omega 1 inhibitor. Ramkumar K, Samanta S, Kyani A, Yang S, Tamura S, Ziemke E, Stuckey JA, Li S, Chinnaswamy K, Otake H, Debnath B, Yarovenko V, Sebolt-Leopold JS, Ljungman M, Neamati N. Nat Commun 7 13084 (2016)
  2. Structure-Based Design of N-(5-Phenylthiazol-2-yl)acrylamides as Novel and Potent Glutathione S-Transferase Omega 1 Inhibitors. Dai W, Samanta S, Xue D, Petrunak EM, Stuckey JA, Han Y, Sun D, Wu Y, Neamati N. J Med Chem 62 3068-3087 (2019)


Reviews citing this publication (4)

  1. Glutathione Transferases: Potential Targets to Overcome Chemoresistance in Solid Tumors. Pljesa-Ercegovac M, Savic-Radojevic A, Matic M, Coric V, Djukic T, Radic T, Simic T. Int J Mol Sci 19 E3785 (2018)
  2. Cellular Mechanisms Accounting for the Refractoriness of Colorectal Carcinoma to Pharmacological Treatment. Marin JJG, Macias RIR, Monte MJ, Herraez E, Peleteiro-Vigil A, Blas BS, Sanchon-Sanchez P, Temprano AG, Espinosa-Escudero RA, Lozano E, Briz O, Romero MR. Cancers (Basel) 12 E2605 (2020)
  3. Chemistry and biology of enzymes in protein glutathionylation. Oppong D, Schiff W, Shivamadhu MC, Ahn YH. Curr Opin Chem Biol 75 102326 (2023)
  4. Overexpression of Glutathione S-Transferases in Human Diseases: Drug Targets and Therapeutic Implications. Lv N, Huang C, Huang H, Dong Z, Chen X, Lu C, Zhang Y. Antioxidants (Basel) 12 1970 (2023)

Articles citing this publication (17)

  1. The Hydroxyquinoline Analogue YUM70 Inhibits GRP78 to Induce ER Stress-Mediated Apoptosis in Pancreatic Cancer. Samanta S, Yang S, Debnath B, Xue D, Kuang Y, Ramkumar K, Lee AS, Ljungman M, Neamati N. Cancer Res 81 1883-1895 (2021)
  2. GSTO1-1 plays a pro-inflammatory role in models of inflammation, colitis and obesity. Menon D, Innes A, Oakley AJ, Dahlstrom JE, Jensen LM, Brüstle A, Tummala P, Rooke M, Casarotto MG, Baell JB, Nguyen N, Xie Y, Cuellar M, Strasser J, Dahlin JL, Walters MA, Burgio G, O'Neill LAJ, Board PG. Sci Rep 7 17832 (2017)
  3. Upregulated glutathione transferase omega-1 correlates with progression of urinary bladder carcinoma. Djukic T, Simic T, Pljesa-Ercegovac M, Matic M, Suvakov S, Coric V, Dragicevic D, Savic-Radojevic A. Redox Rep 22 486-492 (2017)
  4. Glutathione S-transferase omega 1 inhibition activates JNK-mediated apoptotic response in breast cancer stem cells. Manupati K, Debnath S, Goswami K, Bhoj PS, Chandak HS, Bahekar SP, Das A. FEBS J 286 2167-2192 (2019)
  5. Proteomics analysis of colon cancer progression. Saleem S, Tariq S, Aleem I, Sadr-Ul Shaheed, Tahseen M, Atiq A, Hassan S, Abu Bakar M, Khattak S, Syed AA, Ahmad AH, Hussain M, Yusuf MA, Sutton C. Clin Proteomics 16 44 (2019)
  6. GSTO1*CC Genotype (rs4925) Predicts Shorter Survival in Clear Cell Renal Cell Carcinoma Male Patients. Radic T, Coric V, Bukumiric Z, Pljesa-Ercegovac M, Djukic T, Avramovic N, Matic M, Mihailovic S, Dragicevic D, Dzamic Z, Simic T, Savic-Radojevic A. Cancers (Basel) 11 E2038 (2019)
  7. Activity-based protein profiling reveals GSTO1 as the covalent target of piperlongumine and a promising target for combination therapy for cancer. Li L, Zhao Y, Cao R, Li L, Cai G, Li J, Qi X, Chen S, Zhang Z. Chem Commun (Camb) 55 4407-4410 (2019)
  8. Characterization of a small molecule inhibitor of disulfide reductases that induces oxidative stress and lethality in lung cancer cells. Johnson FD, Ferrarone J, Liu A, Brandstädter C, Munuganti R, Farnsworth DA, Lu D, Luu J, Sihota T, Jansen S, Nagelberg A, Shi R, Forcina GC, Zhang X, Cheng GSW, Spencer Miko SE, de Rappard-Yuswack G, Sorensen PH, Dixon SJ, Guha U, Becker K, Djaballah H, Somwar R, Varmus H, Morin GB, Lockwood WW. Cell Rep 38 110343 (2022)
  9. Curcumin improves D-galactose and normal-aging associated memory impairment in mice: In vivo and in silico-based studies. Rahman MA, Shuvo AA, Bepari AK, Hasan Apu M, Shill MC, Hossain M, Uddin M, Islam MR, Bakshi MK, Hasan J, Rahman A, Rahman GMS, Reza HM. PLoS One 17 e0270123 (2022)
  10. Deletion of Glutathione S-Transferase Omega 1 Activates Type I Interferon Genes and Downregulates Tissue Factor. Xu Y, Bankhead A, Tian X, Tang J, Ljungman M, Neamati N. Cancer Res 80 3692-3705 (2020)
  11. Structure-function analyses of candidate small molecule RPN13 inhibitors with antitumor properties. Anchoori RK, Tan M, Tseng SH, Peng S, Soong RS, Algethami A, Foran P, Das S, Wang C, Wang TL, Liang H, Hung CF, Roden RBS. PLoS One 15 e0227727 (2020)
  12. Tunable Cysteine-Targeting Electrophilic Heteroaromatic Warheads Induce Ferroptosis. Karaj E, Sindi SH, Kuganesan N, Perera L, Taylor W, Tillekeratne LMV. J Med Chem 65 11788-11817 (2022)
  13. Integrated phenotypic screening and activity-based protein profiling to reveal potential therapy targets of pancreatic cancer. Liu W, Zhang Z, Zhang ZM, Hao P, Ding K, Li Z. Chem Commun (Camb) 55 1596-1599 (2019)
  14. Polyphotosensitizer-Based Nanoparticles with Michael Addition Acceptors Inhibiting GST Activity and Cisplatin Deactivation for Enhanced Chemotherapy and Photodynamic Immunotherapy. Zhao Q, Liang G, Guo B, Wang W, Yang C, Chen D, Yang F, Xiao H, Xing N. Adv Sci (Weinh) 10 e2300175 (2023)
  15. research-article Inhibition of glutathione S-transferase omega 1-catalyzed protein deglutathionylation suppresses adipocyte differentiation. Iram S, Mashaal A, Go S, Kim J. BMB Rep 56 457-462 (2023)
  16. Integrated Covalent Drug Design Workflow Using Site Identification by Ligand Competitive Saturation. Yu W, Weber DJ, MacKerell AD. J Chem Theory Comput 19 3007-3021 (2023)
  17. The Use of a Brief Synchronization Treatment after Weaning, Combined with Superovulation, Has Moderate Effects on the Gene Expression of Surviving Pig Blastocysts. Gonzalez-Ramiro H, Gil MA, Cuello C, Cambra JM, Gonzalez-Plaza A, Vazquez JM, Vazquez JL, Rodriguez-Martinez H, Lucas-Sanchez A, Parrilla I, Martinez CA, Martinez EA. Animals (Basel) 13 1568 (2023)


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