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Expert Opinion on Drug Discovery Volume 6, 2011 - Issue 4
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Next generation histone deacetylase inhibitors: the answer to the search for optimized epigenetic therapies?

Florian Thaler European Institute of Oncology, Drug Discovery Unit, Department of Experimental Oncology, Via Celoria 26, 20133 Milan, Italy
&
Saverio Minucci University of Milan, Via Celoria 26, 20133 Milan, Italy; Department of Experimental Oncology at the European Institute of Oncology, IFOM-IEO Campus, Via Celoria 26, 20133 Milan, Italy +39 02 57489855; +39 02 94375138. [email protected]
, MD (Professor of Pathology) (Director of Unit IX) (Professor of Pathology) (Director of Unit IX)
Pages 393-404 | Published online: 23 Feb 2011

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Jenny Y Y Ooi, Natasha K Tuano, Haloom Rafehi, Xiao-Ming Gao, Mark Ziemann, Xiao-Jun Du & Assam El-Osta. (2015) HDAC inhibition attenuates cardiac hypertrophy by acetylation and deacetylation of target genes . Epigenetics 10:5, pages 418-430.
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MarianaS. Gerova & OgnyanI. Petrov. (2014) A Convenient Synthesis of the New Histone Deacetylase Inhibitor Scriptaid. Organic Preparations and Procedures International 46:1, pages 76-79.
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Geneviève P Delcuve, Dilshad H Khan & James R Davie. (2013) Targeting class I histone deacetylases in cancer therapy. Expert Opinion on Therapeutic Targets 17:1, pages 29-41.
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Articles from other publishers (29)

Uttam Ghosh, Moumita Basu, Sudip Pal, Sanjeev Meena, Dipak Datta, Ravi Sankar Ampapathi, Tapas K Kundu, Gajendra Singh & Tushar Kanti Chakraborty. (2021) Design, Synthesis and Conformational Studies of Cyclic Tetrapeptides having βγ Fused Turns as HDAC Inhibitors. ChemistrySelect 6:31, pages 7887-7893.
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Kunal Nepali & Jing-Ping Liou. (2021) Recent developments in epigenetic cancer therapeutics: clinical advancement and emerging trends. Journal of Biomedical Science 28:1.
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Kunal Nepali, Ting-Yu Chang, Mei-Jung Lai, Kai-Cheng Hsu, Yun Yen, Tony Eight Lin, Sung-Bau Lee & Jing-Ping Liou. (2020) Purine/purine isoster based scaffolds as new derivatives of benzamide class of HDAC inhibitors. European Journal of Medicinal Chemistry 196, pages 112291.
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Sara S. Oltra, Juan Miguel Cejalvo, Eduardo Tormo, Marta Albanell, Ana Ferrer, Marta Nacher, Begoña Bermejo, Cristina Hernando, Isabel Chirivella, Elisa Alonso, Octavio Burgués, Maria Peña-Chilet, Pilar Eroles, Ana Lluch, Gloria Ribas & María Teresa Martinez. (2020) HDAC5 Inhibitors as a Potential Treatment in Breast Cancer Affecting Very Young Women. Cancers 12:2, pages 412.
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Xinyao Li, Yongling Guo, Xingyi Kuang, Lu Zhao, Hongsong Li, Bingqing Cheng, Weili Wang, Zhaoyuan Zhang, Ping Liu & Jishi Wang. (2019) Histone deacetylase inhibitor LMK-235-mediated HO-1 expression induces apoptosis in multiple myeloma cells via the JNK/AP-1 signaling pathway. Life Sciences 223, pages 146-157.
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Aline Kaletsch, Maria Pinkerneil, Michèle J. Hoffmann, Ananda A. Jaguva Vasudevan, Chenyin Wang, Finn K. Hansen, Constanze Wiek, Helmut Hanenberg, Christoph Gertzen, Holger Gohlke, Matthias U. Kassack, Thomas Kurz, Wolfgang A. Schulz & Günter Niegisch. (2018) Effects of novel HDAC inhibitors on urothelial carcinoma cells. Clinical Epigenetics 10:1.
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Siddharth Narayanan, Gopalakrishnan Loganathan, SriPrakash Mokshagundam, Michael G. Hughes, Stuart K. Williams & Appakalai N. Balamurugan. (2018) Endothelial cell regulation through epigenetic mechanisms: Depicting parallels and its clinical application within an intra-islet microenvironment. Diabetes Research and Clinical Practice 143, pages 120-133.
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Qi-Yin Chen, Pravin R. Chaturvedi & Hendrik Luesch. (2018) Process Development and Scale-up Total Synthesis of Largazole, a Potent Class I Histone Deacetylase Inhibitor. Organic Process Research & Development 22:2, pages 190-199.
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Kai-Cheng Hsu, Chang-Yi Liu, Tony Eight Lin, Jui-Hua Hsieh, Tzu-Ying Sung, Hui-Ju Tseng, Jinn-Moon Yang & Wei-Jan Huang. (2017) Novel Class IIa-Selective Histone Deacetylase Inhibitors Discovered Using an in Silico Virtual Screening Approach. Scientific Reports 7:1.
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Dimitry A. Chistiakov, Alexander N. Orekhov & Yuri V. Bobryshev. (2017) Treatment of cardiovascular pathology with epigenetically active agents: Focus on natural and synthetic inhibitors of DNA methylation and histone deacetylation. International Journal of Cardiology 227, pages 66-82.
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Florian Thaler, Loris Moretti, Raffaella Amici, Agnese Abate, Andrea Colombo, Giacomo Carenzi, Maria Carmela Fulco, Roberto Boggio, Giulio Dondio, Stefania Gagliardi, Saverio Minucci, Luca Sartori, Mario Varasi & Ciro Mercurio. (2016) Synthesis, biological characterization and molecular modeling insights of spirochromanes as potent HDAC inhibitors. European Journal of Medicinal Chemistry 108, pages 53-67.
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Dorleta Otaegui, Carme Masdeu, Eneko Aldaba, Yosu Vara, Aizpea Zubia, Eider San Sebastian, Maria Alcalá, Sergio Villafruela, Fernando P. Cossío & Alicia Rodriguez-Gascón. (2015) Development and validation of a LC-MS assay for the quantification of ikh12 a novel anti-tumor candidate in rat plasma and tissues and its application in a pharmacokinetic study. Biomedical Chromatography 29:8, pages 1249-1258.
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Sylvain Fraineau, Carmen G. Palii, David S. Allan & Marjorie Brand. (2015) Epigenetic regulation of endothelial-cell-mediated vascular repair. FEBS Journal 282:9, pages 1605-1629.
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Thomas B. Nicholson, Nicolas Veland & Taiping Chen. 2015. Epigenetic Cancer Therapy. Epigenetic Cancer Therapy 31 66 .
Haloom Rafehi, Aneta Balcerczyk, Sebastian Lunke, Antony Kaspi, Mark Ziemann, Harikrishnan KN, Jun Okabe, Ishant Khurana, Jenny Ooi, Abdul Waheed Khan, Xiao-Jun Du, Lisa Chang, Izhak Haviv, Samuel T. Keating, Tom C. Karagiannis & Assam El-Osta. (2014) Vascular histone deacetylation by pharmacological HDAC inhibition. Genome Research 24:8, pages 1271-1284.
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Florian Thaler & Ciro Mercurio. (2014) Towards Selective Inhibition of Histone Deacetylase Isoforms: What Has Been Achieved, Where We Are and What Will Be Next. ChemMedChem 9:3, pages 523-536.
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Micaela Montanari, Marcella Macaluso & Antonio Giordano. 2014. Springer Handbook of Bio-/Neuroinformatics. Springer Handbook of Bio-/Neuroinformatics 477 489 .
Mariateresa PuglieseNicoletta FortunatiAntonina GermanoSofia AsioliFrancesca MaranoNicola PalestiniRoberto FrairiaGiuseppe BoccuzziMaria Graziella Catalano. (2013) Histone Deacetylase Inhibition Affects Sodium Iodide Symporter Expression and Induces 131 I Cytotoxicity in Anaplastic Thyroid Cancer Cells . Thyroid 23:7, pages 838-846.
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Florian Thaler, Mario Varasi, Agnese Abate, Giacomo Carenzi, Andrea Colombo, Chiara Bigogno, Roberto Boggio, Roberto Dal Zuffo, Daniela Rapetti, Anna Resconi, Nickolas Regalia, Stefania Vultaggio, Giulio Dondio, Stefania Gagliardi, Saverio Minucci & Ciro Mercurio. (2013) Synthesis and biological characterization of spiro[2H-(1,3)-benzoxazine-2,4′-piperidine] based histone deacetylase inhibitors. European Journal of Medicinal Chemistry 64, pages 273-284.
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Mariam Traoré, Flore Mietton, Danièle Maubon, Marine Peuchmaur, Flaviane Francisco Hilário, Rossimiriam Pereira de Freitas, Alexandre Bougdour, Aurélie Curt, Marjorie Maynadier, Henri Vial, Hervé Pelloux, Mohamed-Ali Hakimi & Yung-Sing Wong. (2013) Flexible Synthesis and Evaluation of Diverse Anti-Apicomplexa Cyclic Peptides. The Journal of Organic Chemistry 78:8, pages 3655-3675.
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Rob De Vreese, Tom Verhaeghe, Tom Desmet & Matthias D'hooghe. (2013) Potent and selective HDAC6 inhibitory activity of N-(4-hydroxycarbamoylbenzyl)-1,2,4,9-tetrahydro-3-thia-9-azafluorenes as novel sulfur analogues of Tubastatin A. Chemical Communications 49:36, pages 3775.
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Lilibeth A. Salvador & Hendrik Luesch. 2013. Natural Products and Cancer Drug Discovery. Natural Products and Cancer Drug Discovery 59 95 .
Kasper P. Kepp. (2012) Bioinorganic Chemistry of Alzheimer’s Disease. Chemical Reviews 112:10, pages 5193-5239.
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Chun-wa Chung & David F. Tough. (2012) Bromodomains: a new target class for small molecule drug discovery. Drug Discovery Today: Therapeutic Strategies 9:2-3, pages e111-e120.
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Florian Thaler, Mario Varasi, Giacomo Carenzi, Andrea Colombo, Agnese Abate, Chiara Bigogno, Roberto Boggio, Simone Carrara, Tiziana Cataudella, Roberto Dal Zuffo, Veronica Reali, Stefania Vultaggio, Giulio Dondio, Stefania Gagliardi, Saverio Minucci & Ciro Mercurio. (2012) Spiro[chromane-2,4′-piperidine]-Based Histone Deacetylase Inhibitors with Improved in vivo Activity. ChemMedChem 7:4, pages 709-721.
Crossref
Florian Thaler. (2012) Current trends in the development of histone deacetylase inhibitors: a review of recent patent applications. Pharmaceutical Patent Analyst 1:1, pages 75-90.
Crossref
F Cherblanc, N Chapman-Rothe, R BrownMJ Fuchter. (2012) Current limitations and future opportunities for epigenetic therapies. Future Medicinal Chemistry 4:4, pages 425-446.
Crossref
Jiyong Hong & Hendrik Luesch. (2012) Largazole: From discovery to broad-spectrum therapy. Natural Product Reports 29:4, pages 449.
Crossref
Chun-wa Chung. 2012. Progress in Medicinal Chemistry Volume 51. Progress in Medicinal Chemistry Volume 51 1 55 .

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