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Journal of Enzyme Inhibition and Medicinal Chemistry Volume 32, 2017 - Issue 1
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Research Article

A new nitrobenzoxadiazole-based GSTP1-1 inhibitor with a previously unheard of mechanism of action and high stability

Chiara FulciDepartment of Experimental Medicine and Surgery, University of Tor Vergata, Rome, Italy; View further author information
,
Dante RotiliDepartment of Drug Chemistry and Technologies, University of Rome “Sapienza”, Rome, Italy; ORCID Iconhttp://orcid.org/0000-0002-8428-8763View further author information
ORCID Icon,
Anastasia De LucaDepartment of Experimental Medicine and Surgery, University of Tor Vergata, Rome, Italy; View further author information
,
Lorenzo StellaDepartment of Chemical Sciences and Technologies; ORCID Iconhttp://orcid.org/0000-0002-5489-7381View further author information
ORCID Icon,
Blasco Morozzo della RoccaDepartment of Biology, University of Tor Vergata, Rome, Italy; View further author information
,
Mariantonietta ForgioneDepartment of Drug Chemistry and Technologies, University of Rome “Sapienza”, Rome, Italy; View further author information
,
Veronica Di PaoloDepartment of Pharmaceutical and Pharmacological Sciences, University of Padova, Padova, Italy; View further author information
,
Antonello MaiDepartment of Drug Chemistry and Technologies, University of Rome “Sapienza”, Rome, Italy; ;Pasteur Institute, Cenci Bolognetti Foundation, University of Rome “La Sapienza”, Rome, Italy; View further author information
,
Mattia FalconiDepartment of Biology, University of Tor Vergata, Rome, Italy; View further author information
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Luigi QuintieriDepartment of Pharmaceutical and Pharmacological Sciences, University of Padova, Padova, Italy; View further author information
&
Anna M. CaccuriDepartment of Experimental Medicine and Surgery, University of Tor Vergata, Rome, Italy; ;The NAST Centre for Nanoscience & Nanotechnology & Innovative Instrumentation, University of Tor Vergata, Rome, ItalyCorrespondence[email protected]
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Pages 240-247 | Received 28 Jul 2016, Accepted 20 Sep 2016, Published online: 18 Jan 2017

References

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  • Ricci G, De Maria F, Antonini G, et al. 7-Nitro-2,1,3-benzoxadiazole derivatives, a new class of suicide inhibitors for glutathione S-transferases. Mechanism of action of potential anticancer drugs. J Biol Chem 2005;280:26397–405.
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  • De Luca A, Mei G, Rosato N, et al. The fine-tuning of TRAF2–GSTP1-1 interaction: effect of ligand binding and in situ detection of the complex. Cell Death Dis 2014;5:e1015.
  • Pellizzari Tregno F, Sau A, Pezzola S, et al. In vitro and in vivo efficacy of 6-(7-nitro-2,1,3-benzoxadiazol-4-ylthio)hexanol (NBDHEX) on human melanoma. Eur J Cancer 2009;45:2606–17.
  • Tentori L, Dorio AS, Mazzon E, et al. The glutathione transferase inhibitor 6-(7-nitro-2,1,3-benzoxadiazol-4-ylthio)hexanol (NBDHEX) increases temozolomide efficacy against malignant melanoma. Eur J Cancer 2011;47:1219–30.
  • Rotili D, De Luca A, Tarantino D, et al. Synthesis and structure–activity relationship of new cytotoxic agents targeting human glutathione-S-transferases. Eur J Med Chem 2015;89:156–71.
  • Stella L, van de Weert M. Fluorescence quenching and ligand binding: a critical discussion of a popular methodology. J Mol Struct 2011;998:144–50.
  • Ricci G, Caccuri AM, Lo Bello M, et al. Glutathione transferase P1-1: self-preservation of an anti-cancer enzyme. Biochem J 2003;376:71–6.
  • De Luca A, Rotili D, Carpanese D, et al. A novel orally active water-soluble inhibitor of human glutathione transferase exerts a potent and selective antitumor activity against human melanoma xenografts. Oncotarget 2015;6:4126–43.
  • Hegazy UM, Mannervik B, Stenberg G. Functional role of the lock and key motif at the subunit interface of glutathione transferase p1-1. J Biol Chem 2004;279:9586–96.
  • Wu Y, Fan Y, Xue B, et al. Human glutathione S-transferase P1-1 interacts with TRAF2 and regulates TRAF2-ASK1 signals. Oncogene 2006;25:5787–800.

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