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Expert Opinion on Therapeutic Targets Volume 19, 2015 - Issue 6
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Original Research

Overexpression of pyruvate dehydrogenase kinase supports dichloroacetate as a candidate for cutaneous melanoma therapy

Helena PópuloInstitute of Molecular Pathology and Immunology of the University of Porto (IPATIMUP), University of Porto, Porto, Portugal+22 557 0700; +22 557 0799; [email protected];Institute for Research and Innovation in Health (Instituto de Investigação e Inovação em Saúde), University of Porto, Porto, Portugal
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Regina CaldasInstitute of Molecular Pathology and Immunology of the University of Porto (IPATIMUP), University of Porto, Porto, Portugal+22 557 0700; +22 557 0799; [email protected];Institute for Research and Innovation in Health (Instituto de Investigação e Inovação em Saúde), University of Porto, Porto, Portugal;Faculty of Medicine, University of Porto, Porto, Portugal
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José Manuel LopesInstitute of Molecular Pathology and Immunology of the University of Porto (IPATIMUP), University of Porto, Porto, Portugal+22 557 0700; +22 557 0799; [email protected];Institute for Research and Innovation in Health (Instituto de Investigação e Inovação em Saúde), University of Porto, Porto, Portugal;Department of Pathology and Oncology, Faculty of Medicine, University of Porto, Porto, Portugal;Service of Anatomic Pathology Hospital São João, Porto, Portugal
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Joana PardalService of Anatomic Pathology Hospital São João, Porto, Portugal
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Valdemar MáximoInstitute of Molecular Pathology and Immunology of the University of Porto (IPATIMUP), University of Porto, Porto, Portugal+22 557 0700; +22 557 0799; [email protected];Institute for Research and Innovation in Health (Instituto de Investigação e Inovação em Saúde), University of Porto, Porto, Portugal;Department of Pathology and Oncology, Faculty of Medicine, University of Porto, Porto, Portugal
&
Paula SoaresInstitute of Molecular Pathology and Immunology of the University of Porto (IPATIMUP), University of Porto, Porto, Portugal+22 557 0700; +22 557 0799; [email protected];Institute for Research and Innovation in Health (Instituto de Investigação e Inovação em Saúde), University of Porto, Porto, Portugal;Department of Pathology and Oncology, Faculty of Medicine, University of Porto, Porto, Portugal
Pages 733-745 | Published online: 14 May 2015

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Helena Pópulo, Beatriz Domingues, Cristina Sampaio, José Manuel Lopes & Paula Soares. (2021) Combinatorial Therapies to Overcome BRAF/MEK Inhibitors Resistance in Melanoma Cells: An in vitro Study. Journal of Experimental Pharmacology 13, pages 521-535.
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Beatriz Domingues, José Manuel Lopes, Paula Soares & Helena Pópulo. (2018) Melanoma treatment in review. ImmunoTargets and Therapy 7, pages 35-49.
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María José Bravo, Antonio Manuel Burgos-Molina, Marilina García-Aranda, Maximino Redondo & Teresa Téllez. (2023) Unlocking New Avenues in Breast Cancer Treatment: The Synergy of Kinase Inhibitors and Immunotherapy. Cancers 15:23, pages 5499.
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Saugat Mondal, Ayan Chatterjee, Shreya Banerjee, Tara Singha, Antara Sikder, Tarun K. Bhattacharyya, Mahitosh Mandal, Prasanta K. Datta, Tapas K. Maiti & N. D. Pradeep Singh. (2023) Temporal Release of Cell Cycle Regulator α-Lipoic Acid: An NIR-Light (Two-Photon) Activatable Quinoxaline-Based Nano-Prodrug Delivery System. ACS Applied Materials & Interfaces.
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Yingchao Ma, Xishen Zhang, Xiao Han, Zhizhong Hao, Rong Ji, Jianhui Li, Wenna Guo, Yanting Zhang, Fangxia Guan & Shanshan Ma. (2023) PDK1 regulates the progression of esophageal squamous cell carcinoma through metabolic reprogramming. Molecular Carcinogenesis 62:6, pages 866-881.
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Peter W. Stacpoole & Charles E. McCall. (2023) The pyruvate dehydrogenase complex: Life’s essential, vulnerable and druggable energy homeostat. Mitochondrion 70, pages 59-102.
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Rita Mota, Raquel T. Lima, Carlos Flores, Juliana F. Silva, Beatriz Cruz, Bárbara Alves, Marta T. Pinto, Alessandra Adessi, Sara B. Pereira, Roberto De Philippis, Paula Soares & Paula Tamagnini. (2023) Assessing the Antitumor Potential of Variants of the Extracellular Carbohydrate Polymer from Synechocystis ΔsigF Mutant. Polymers 15:6, pages 1382.
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Shilin Wang, Guohong Liu, Yirong Li & Yunbao Pan. (2022) Metabolic Reprogramming Induces Macrophage Polarization in the Tumor Microenvironment. Frontiers in Immunology 13.
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Jiske F. Tiersma, Bernard Evers, Barbara M. Bakker, Mathilde Jalving & Steven de Jong. (2022) Pyruvate Dehydrogenase Kinase Inhibition by Dichloroacetate in Melanoma Cells Unveils Metabolic Vulnerabilities. International Journal of Molecular Sciences 23:7, pages 3745.
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Nives Škorja Milić, Klemen Dolinar, Katarina Miš, Urška Matkovič, Maruša Bizjak, Mojca Pavlin, Matej Podbregar & Sergej Pirkmajer. (2021) Suppression of Pyruvate Dehydrogenase Kinase by Dichloroacetate in Cancer and Skeletal Muscle Cells Is Isoform Specific and Partially Independent of HIF-1α. International Journal of Molecular Sciences 22:16, pages 8610.
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Rodrigo S. do Nascimento, Marcia K. Nagamine, Gabriela F. De Toledo, Lucas M. Chaible, Marcello V. Tedardi, Murilo P. del-Grande, Ivone I.M. da Fonseca & Maria L.Z. Dagli.. (2020) Sodium dichloroacetate attenuates the growth of B16-F10 melanoma in vitro and in vivo: an opportunity for drug repurposing. Anti-Cancer Drugs 32:2, pages 111-116.
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Tomas Koltai, Stephan J. Reshkin & Salvador Harguindey. 2020. An Innovative Approach to Understanding and Treating Cancer: Targeting pH. An Innovative Approach to Understanding and Treating Cancer: Targeting pH 361 416 .
Carlos Flores, Raquel T. Lima, Alessandra Adessi, Aureliana Sousa, Sara B. Pereira, Pedro L. Granja, Roberto De Philippis, Paula Soares & Paula Tamagnini. (2019) Characterization and antitumor activity of the extracellular carbohydrate polymer from the cyanobacterium Synechocystis ΔsigF mutant. International Journal of Biological Macromolecules 136, pages 1219-1227.
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Ellen C. de Heer, Adrienne H. Brouwers, Ronald Boellaard, Wim J. Sluiter, Gilles F. H. Diercks, Geke A. P. Hospers, Elisabeth G. E. de Vries & Mathilde Jalving. (2018) Mapping heterogeneity in glucose uptake in metastatic melanoma using quantitative 18F-FDG PET/CT analysis. EJNMMI Research 8:1.
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Wen Zhang, Xiaohui Hu, Harapriya Chakravarty, Zheng Yang & Kin Yip Tam. (2018) Identification of Novel Pyruvate Dehydrogenase Kinase 1 (PDK1) Inhibitors by Kinase Activity-Based High-Throughput Screening for Anticancer Therapeutics. ACS Combinatorial Science 20:11, pages 660-671.
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W E Damsky & M Bosenberg. (2017) Melanocytic nevi and melanoma: unraveling a complex relationship. Oncogene 36:42, pages 5771-5792.
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Cecilie Abildgaard, Christina Dahl, Ahmad Abdul-Al, Annette Christensen & Per Guldberg. (2017) Inhibition of retinoic acid receptor β signaling confers glycolytic dependence and sensitization to dichloroacetate in melanoma cells. Oncotarget 8:48, pages 84210-84223.
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Saban Kalay, Aysegul Dogan, Ali Turkan & Asuman Demiroglu-Zergeroglu. (2017) Dicholoroacetate exerts anti-cancer activity on human renal cell carcinoma cells. Turkish Journal of Biochemistry 42:5, pages 577-585.
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Swatishree Sradhanjali, Devjyoti Tripathy, Suryasnata Rath, Ruchi Mittal & Mamatha M. Reddy. (2017) Overexpression of pyruvate dehydrogenase kinase 1 in retinoblastoma: A potential therapeutic opportunity for targeting vitreous seeds and hypoxic regions. PLOS ONE 12:5, pages e0177744.
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Mithilesh Kumar Jha, In-Kyu Lee & Kyoungho Suk. (2016) Metabolic reprogramming by the pyruvate dehydrogenase kinase–lactic acid axis: Linking metabolism and diverse neuropathophysiologies. Neuroscience & Biobehavioral Reviews 68, pages 1-19.
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Peter A. Engel. (2016) Is age-related failure of metabolic reprogramming a principal mediator in idiopathic Parkinson’s disease? Implications for treatment and inverse cancer risk. Medical Hypotheses 93, pages 154-160.
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