6-(7-nitro-2,1,3-benzoxadiazol-4-ylthio) hexanol: a promising new anticancer compound
The 7-nitro-2,1,3-nitrobenzoxadiazole (NBD) derivatives are a series of compounds containing the NBD scaffold that are not glutathione (GSH) peptidomimetics, and result in a strong inhibition of glutathione S-transferases (GSTs). Growing evidences highlight their pivotal roles and outstanding antica...
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description | The 7-nitro-2,1,3-nitrobenzoxadiazole (NBD) derivatives are a series of compounds containing the NBD scaffold that are not glutathione (GSH) peptidomimetics, and result in a strong inhibition of glutathione S-transferases (GSTs). Growing evidences highlight their pivotal roles and outstanding anticancer activity in different tumor models. In particular, 6-(7-nitro-2,1,3-benzoxadiazol-4-ylthio) hexanol (NBDHEX) is extensively studied, which is a very efficient inhibitor of GSTP1-1. It triggers apoptosis in several tumor cell lines and this cytotoxic activity is observed at micro and submicromolar concentrations. Importantly, studies have shown that NBDHEX acts as an anticancer drug by inhibiting GSTs catalytic activity, avoiding inconvenience of the inhibitor extrusion from the cell by specific pumps and disrupting the interaction between the GSTP1-1 and key signaling effectors. Additionally, some researchers also have discovered that NBDHEX can act as late-phase autophagy inhibitor, which opens new opportunities to fully exploit its therapeutic potential. In this review, we summarize the advantages, anticancer mechanisms, and analogs of this compound, which will establish the basis on the usage of NBDHEX in clinical applications in future. |
doi_str_mv | 10.1042/bsr20171440 |
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Growing evidences highlight their pivotal roles and outstanding anticancer activity in different tumor models. In particular, 6-(7-nitro-2,1,3-benzoxadiazol-4-ylthio) hexanol (NBDHEX) is extensively studied, which is a very efficient inhibitor of GSTP1-1. It triggers apoptosis in several tumor cell lines and this cytotoxic activity is observed at micro and submicromolar concentrations. Importantly, studies have shown that NBDHEX acts as an anticancer drug by inhibiting GSTs catalytic activity, avoiding inconvenience of the inhibitor extrusion from the cell by specific pumps and disrupting the interaction between the GSTP1-1 and key signaling effectors. Additionally, some researchers also have discovered that NBDHEX can act as late-phase autophagy inhibitor, which opens new opportunities to fully exploit its therapeutic potential. In this review, we summarize the advantages, anticancer mechanisms, and analogs of this compound, which will establish the basis on the usage of NBDHEX in clinical applications in future.</description><identifier>ISSN: 0144-8463</identifier><identifier>EISSN: 1573-4935</identifier><identifier>DOI: 10.1042/bsr20171440</identifier><identifier>PMID: 29358310</identifier><language>eng</language><publisher>England: Portland Press Ltd The Biochemical Society</publisher><subject>Anticancer properties ; Antineoplastic drugs ; Antitumor activity ; Apoptosis ; Autophagy ; Bone cancer ; Catalytic activity ; Cell cycle ; Cytotoxicity ; Drug interactions ; Drug resistance ; Glutathione ; Glutathione transferase ; Hexanol ; Inhibitors ; Kinases ; Leukemia ; Melanoma ; Mesothelioma ; Peptidomimetics ; Phosphorylation ; Proteins ; Review ; Sarcoma ; Signal transduction ; Tumor cell lines ; Tumors</subject><ispartof>Bioscience reports, 2018-02, Vol.38 (1)</ispartof><rights>2018 The Author(s).</rights><rights>2018. This work is published under http://creativecommons.org/licenses/by/4.0/ (the “License”). 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Growing evidences highlight their pivotal roles and outstanding anticancer activity in different tumor models. In particular, 6-(7-nitro-2,1,3-benzoxadiazol-4-ylthio) hexanol (NBDHEX) is extensively studied, which is a very efficient inhibitor of GSTP1-1. It triggers apoptosis in several tumor cell lines and this cytotoxic activity is observed at micro and submicromolar concentrations. Importantly, studies have shown that NBDHEX acts as an anticancer drug by inhibiting GSTs catalytic activity, avoiding inconvenience of the inhibitor extrusion from the cell by specific pumps and disrupting the interaction between the GSTP1-1 and key signaling effectors. Additionally, some researchers also have discovered that NBDHEX can act as late-phase autophagy inhibitor, which opens new opportunities to fully exploit its therapeutic potential. In this review, we summarize the advantages, anticancer mechanisms, and analogs of this compound, which will establish the basis on the usage of NBDHEX in clinical applications in future.</description><subject>Anticancer properties</subject><subject>Antineoplastic drugs</subject><subject>Antitumor activity</subject><subject>Apoptosis</subject><subject>Autophagy</subject><subject>Bone cancer</subject><subject>Catalytic activity</subject><subject>Cell cycle</subject><subject>Cytotoxicity</subject><subject>Drug interactions</subject><subject>Drug resistance</subject><subject>Glutathione</subject><subject>Glutathione transferase</subject><subject>Hexanol</subject><subject>Inhibitors</subject><subject>Kinases</subject><subject>Leukemia</subject><subject>Melanoma</subject><subject>Mesothelioma</subject><subject>Peptidomimetics</subject><subject>Phosphorylation</subject><subject>Proteins</subject><subject>Review</subject><subject>Sarcoma</subject><subject>Signal 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hexanol: a promising new anticancer compound</title><author>Sha, Huan-Huan ; Wang, Zhen ; Dong, Shu-Chen ; Hu, Tian-Mu ; Liu, Si-Wen ; Zhang, Jun-Ying ; Wu, Yang ; Ma, Rong ; Wu, Jian-Zhong ; Chen, Dan ; Feng, Ji-Feng</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c475t-d3ea3f61b4b8ac52fbf947f63f0c0e2df613e359addccff88ff30544143c17943</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2018</creationdate><topic>Anticancer properties</topic><topic>Antineoplastic drugs</topic><topic>Antitumor activity</topic><topic>Apoptosis</topic><topic>Autophagy</topic><topic>Bone cancer</topic><topic>Catalytic activity</topic><topic>Cell cycle</topic><topic>Cytotoxicity</topic><topic>Drug interactions</topic><topic>Drug resistance</topic><topic>Glutathione</topic><topic>Glutathione transferase</topic><topic>Hexanol</topic><topic>Inhibitors</topic><topic>Kinases</topic><topic>Leukemia</topic><topic>Melanoma</topic><topic>Mesothelioma</topic><topic>Peptidomimetics</topic><topic>Phosphorylation</topic><topic>Proteins</topic><topic>Review</topic><topic>Sarcoma</topic><topic>Signal transduction</topic><topic>Tumor cell lines</topic><topic>Tumors</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Sha, Huan-Huan</creatorcontrib><creatorcontrib>Wang, Zhen</creatorcontrib><creatorcontrib>Dong, Shu-Chen</creatorcontrib><creatorcontrib>Hu, Tian-Mu</creatorcontrib><creatorcontrib>Liu, Si-Wen</creatorcontrib><creatorcontrib>Zhang, Jun-Ying</creatorcontrib><creatorcontrib>Wu, Yang</creatorcontrib><creatorcontrib>Ma, Rong</creatorcontrib><creatorcontrib>Wu, Jian-Zhong</creatorcontrib><creatorcontrib>Chen, Dan</creatorcontrib><creatorcontrib>Feng, 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compounds containing the NBD scaffold that are not glutathione (GSH) peptidomimetics, and result in a strong inhibition of glutathione S-transferases (GSTs). Growing evidences highlight their pivotal roles and outstanding anticancer activity in different tumor models. In particular, 6-(7-nitro-2,1,3-benzoxadiazol-4-ylthio) hexanol (NBDHEX) is extensively studied, which is a very efficient inhibitor of GSTP1-1. It triggers apoptosis in several tumor cell lines and this cytotoxic activity is observed at micro and submicromolar concentrations. Importantly, studies have shown that NBDHEX acts as an anticancer drug by inhibiting GSTs catalytic activity, avoiding inconvenience of the inhibitor extrusion from the cell by specific pumps and disrupting the interaction between the GSTP1-1 and key signaling effectors. Additionally, some researchers also have discovered that NBDHEX can act as late-phase autophagy inhibitor, which opens new opportunities to fully exploit its therapeutic potential. In this review, we summarize the advantages, anticancer mechanisms, and analogs of this compound, which will establish the basis on the usage of NBDHEX in clinical applications in future.</abstract><cop>England</cop><pub>Portland Press Ltd The Biochemical Society</pub><pmid>29358310</pmid><doi>10.1042/bsr20171440</doi><oa>free_for_read</oa></addata></record> |
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subjects | Anticancer properties Antineoplastic drugs Antitumor activity Apoptosis Autophagy Bone cancer Catalytic activity Cell cycle Cytotoxicity Drug interactions Drug resistance Glutathione Glutathione transferase Hexanol Inhibitors Kinases Leukemia Melanoma Mesothelioma Peptidomimetics Phosphorylation Proteins Review Sarcoma Signal transduction Tumor cell lines Tumors |
title | 6-(7-nitro-2,1,3-benzoxadiazol-4-ylthio) hexanol: a promising new anticancer compound |
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