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Histone Deactylase Inhibitors as Novel Target for Cancer, Diabetes, and Inflammation
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  • Journal title : Journal of the Chosun Natural Science
  • Volume 6, Issue 1,  2013, pp.57-63
  • Publisher : The Research Institute of Chosun Natural Science
  • DOI : 10.13160/ricns.2013.6.1.057
 Title & Authors
Histone Deactylase Inhibitors as Novel Target for Cancer, Diabetes, and Inflammation
Singh, Parul; Madhavan, Thirumurthy;
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 Abstract
Histone deacetylase (HDACs) is an enzyme family that deacetylates histones and non-histones protein. Availability of crystal structure of HDAC8 has been a boosting factor to generate target based inhibitors. Hydroxamic class is the most studied one to generate potent inhibitors. HDAC class I and class II enzymes are emerging as a therapeutic target for cancer, diabetes, inflammation and other diseases. DNA methylation and histone modification are epigenetic mechanism, is important for the regulation of cellular functions. HDACs enzymes play essential role in gene transcription to regulate cell proliferation, migration and death. The aim of this article is to provide a comprehensive overview about structure and function of HDACs enzymes, histone deacetylase inhibitors (HDACi) and HDACs enzymes as a therapeutic target for cancer, inflammation and diabetes.
 Keywords
HDACs;Enzymes;Inhibitors;Cancer;
 Language
English
 Cited by
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 References
1.
A. J. M. De Ruijter, A. H. Van Gennip, H. N. Caron, S. Kemp, and A. B. P. Van Kuilenburg, "Histone deacetylases (HDACs): characterization of the classical HDAC family", Biochem. J., Vol. 370, pp. 737-749, 2003. crossref(new window)

2.
K. Ito, P. J. Barnes, and I. M. Adcock, "Glucocorticoid receptor recruitment of histone deacetylase 2 inhibits interleukin-1beta-induced histone H4 acetylation on lysines 8 and 12", Mol. Cell. Biol., Vol. 20, pp. 6891-6903, 2000. crossref(new window)

3.
D. J. Witter, S. Belvedere, L. Chen, J. Paul Secrist, R. T. Mosleyd, and T. A. Millera, "Benzo[b]thiophenebased histone deacetylase inhibitors", Bioorg. Med. Chem. Lett., Vol. 17, pp 4562-4567, 2007. crossref(new window)

4.
T. Sundarapandian, J. Shalini, S. Sugunadevi, and L. K. Woo, "Docking-enabled pharmacophore model for histone deacetylase 8 inhibitors and its application in anti-cancer drug discovery", J. Mol. Graph. Model., Vol. 29, pp. 382-395, 2010. crossref(new window)

5.
S. Thangapandian, S. John, S. Sakkiah, and K. W. Lee, "Ligand and structure based pharmacophore modeling to facilitate novel histone deacetylase 8 inhibitor design", Eur. J. Med. Chem., Vol. 45, pp. 4409-4417, 2010. crossref(new window)

6.
D. J. Witter, S. Belvedere, L. Chen, J. P. Secrist, R. T. Mosleyd, and T. A. Miller, "Benzo[b]thiophenebased histone deacetylase inhibitors", Bioorg. Med. Chem. Lett., Vol. 17, pp. 4562-4567, 2007. crossref(new window)

7.
S. Vadivelan, B.N. Sinha, G. Rambabu, K. Boppana, and S.A.R.P. Jagarlapudi, "Pharmacophore model ing and virtual screening studies to design some potential histone deacetylase inhibitors as new leads", J. Mol. Graph. Model., Vol. 26, pp. 935-946, 2008. crossref(new window)

8.
Y. Chen, H. Li, W. Tang, C. Zhu, Y. Jiang, J. Zou, Q. Yu and Q. You, "3D-QSAR studies of HDACs inhibitors using pharmacophore-based alignment", Eur. J. Med. Chem., Vol.44, pp. 2868-2876, 2009. crossref(new window)

9.
R. Heinke, L. Carlino, S. Kannan, M. Jung, and W. Sippl, "Computer-and structure-based lead design for epigenetic targets", Bioorg. Med. Chem., Vol. 19, pp. 3605-3615, 2011. crossref(new window)

10.
D. P. Christensen, M. Dahllof, M. Lundh, D. N. Rasmussen, M. D. Nielsen, N. Billestrup, L. G. Grunnet, and T. M. Poulsen, "Histone deacetylase (HDAC) inhibition as a novel treatment for diabetes mellitus", doi: 10.2119/molmed.2011.00021 crossref(new window)

11.
S. Balasubramanian, J. Ramos, W. Luo, M. Sirisawad, E. Verner, and J. J. Buggy, "A novel histone deacetylase 8 (HDAC8)-specific inhibitor PCI-34051 induces apoptosis in T-cell lymphomas Leukemia 22", doi: 10.1038/leu.2008.9 crossref(new window)

12.
H. S. Suh, S. Choi, P. Khattar, N. Choi, and S. C. Lee, "Histone deacetylase inhibitors suppress the expression of inflammatory and innate immune response genes in human microglia and astrocytes", J. Neuroimmune Pharmacol., Vol. 5, pp. 521-32, 2010. crossref(new window)

13.
F. Miao, I. G. Gonzalo, L. Lanting, and R. Natarajan, "In vivo chromatin remodeling events leading to inflammatory gene transcription under diabetic conditions", J. Biol. Chem., Vol. 279, pp. 18091-18097, 2004. crossref(new window)

14.
N. Shanmugam, M. A. Reddy, M. Guha, and R. Natarajan, "High glucose-induced expression of proinflammatory cytokine and chemokine genes in monocytic cells", Diabetes, Vol. 52, pp. 1256-64, 2003. crossref(new window)

15.
M. A. Halili, M. R. Andrews, L. I. Labzin, K. Schroder, G. Matthias, C. Cao, E. Lovelace, R. C. Reid, G. T. Le, D. A. Hume, K. M. Irvine, P. Matthias, D. P. Fairlie, and M. J. Sweet, "Differential effects of selective HDAC inhibitors on macrophage inflammatory responses to the Toll-like receptor 4 agonist LPS", J. Leukoc. Biol., Vol. 87, pp. 1103-14, 2010. crossref(new window)

16.
F. Leoni, G. Fossati, E. C. Lewis, J. K. Lee, G. Porro, P. Pagani, D. Modena, M. L. Moras, P. Pozzi, L. L. Reznikov, B. Siegmund, G. Fantuzzi, C. A. Dinarello, and Paolo Mascagni, "The histone deacetylase inhibitor ITF2357 reduces production of proinflammatory cytokines in vitro and systemic inflammation in vivo", Mol. Med., Vol. 11, pp. 1-15, 2005.

17.
M. A. Halili, M. R. Andrews, M. J. Sweet, and D. P. Fairlie, "Histone deacetylase inhibitors in inflammatory disease", Curr. Top. Med. Chem., Vol. 9, pp. 309-319, 2009. crossref(new window)

18.
I. V. Gregoretti, Y. M. Lee, and H. V. Goodson, "Molecular evolution of the histone deacetylase family: functional implications of phylogenetic analysis", J. Mol. Biol., Vol. 338, pp. 17-31, 2004. crossref(new window)

19.
C. Choudhary, C. Kumar, F. Gnad , M. L. Nielsen, M. Rehman, T. C. Walther, J. V. Olsen, and M. Mann, "Lysine acetylation targets protein complexes and co-regulates major cellular functions", Science, Vol. 325, pp. 834-840, 2009. crossref(new window)

20.
A. Vannini, C. Volpari, P. Gallinari, P. Jones, M. Mattu, A. Carfi, R. D. Francesco, C. Steinkuhler, and S. D. Marco, "Substrate binding to histone deacetylases as shown by the crystal structure of the HDAC8-substrate complex", EMBO reports, Vol. 8, pp. 9, 2007.

21.
S. Timmermann, H. Lehrmann, A. Polesskaya, and A. Harel-Bellan, "Histone acetylation and disease", Cell. Mol. Life Sci., Vol. 58, pp. 728-736, 2001. crossref(new window)

22.
E. D. Gennaro, F. Bruzzese1, M. Caraglia, A. Abruzzese, and A. Budillon, "Acetylation of proteins as novel target for antitumor therapy", Amino Acids, Vol. 26, pp. 435-441, 2004.

23.
M. Haberland, M. H. Mokalled, R. L. Montgomery, and E. N. Olson, "Epigenetic control of skull morphogenesis by histone deacetylase 8", Gene. Dev., Vol. 23, pp 1625-1630, 2009. crossref(new window)

24.
M. Dokmanovic and P. A. Marks, "Prospects: histone deacetylase inhibitors", J. Cell. Biochem., Vol. 96, pp. 293-304, 2005. crossref(new window)

25.
B. E. Morrison, N. Majdzadeh, and S. R. D. Mello, "Histone deacetylases: Focus on the nervous system", Cell. Mol. Life Sci., Vol. 64, pp. 2258-2269, 2007. crossref(new window)

26.
T. A. McKinsey, "Isoform-selective HDAC inhibitors: Closing in on translational medicine for the heart", J. Mol. Cell. Cardiol., Vol. 51, pp. 491-496, 2011. crossref(new window)

27.
D. M. Fass, S. A. Reis, B. Ghosh, K. M. Hennig, N. F. Joseph d, W. N. Zhao, T. J.F. Nieland, J. S. Guan, C. E. G. Kuhnle, W. Tang, D. D. Barker, R. Mazitschek, S. L. Schreiber, L. H. Tsai, and S. J. H. Crebinostat, "A novel cognitive enhancer that inhibits histone deacetylase activity and modulates chromatin-mediated neuroplasticity", Neuropharmacology, Vol. 64, pp. 81-96, 2013. crossref(new window)

28.
X. Wanga, X. Weia, Q. Pangb, and F. Yia, "Histone deacetylases and their inhibitors: molecular mechanisms and therapeutic implications in diabetes mellitus", Acta Pharmaceutica Sinica B, Vol. 2, pp. 387-395, 2012. crossref(new window)

29.
T. Suzuki, A. Matsuura, A. Kouketsu, H. Nakagawa, and N. Miyata, "Identification of a potent nonhydroxamate histone deacetylase inhibitor by mechanism-based drug design", Bioorg. Med. Chem. Lett., Vol. 15, pp. 331-335, 2005. crossref(new window)

30.
M. R. Shakespear, M. A. Halili, K. M. Irvine, D. P. Fairlie, and Matthew J. Sweet, "Histone deacetylases as regulators of inflammation and immunity", Trends Immunol., Vol. 32, pp. 335-343, 2011. crossref(new window)

31.
O. Witt and R. Lindemann "HDAC inhibitors: Magic bullets, dirty drugs or just another targeted therapy", Cancer Lett., Vol. 280, pp. 123-124, 2009. crossref(new window)

32.
T. Suzuki, A. Kouketsu, A. Matsuura, A. Kohara, S. I. Ninomiya, K. Kohdaa, and Naoki Miyataa, "Thiol-based SAHA analogues as potent histone deacetylase Inhibitors", Bioorg. Med. Chem. Lett., Vol. 14, pp. 3313-3317, 2004. crossref(new window)

33.
S. E. Choi, S. V.W. Weerasinghe, and M. K. H. Pflum, "The structural requirements of histone deacetylase inhibitors: suberoylanilide hydroxamic acid analogs modified at the C3 position display isoform selectivity", Bioorg. Med. Chem. Lett., Vol. 21, pp. 6139-6142, 2011. crossref(new window)

34.
D. Ling, G. M. Marshall, P. Y. Liu, N. Xu, C. A. Nelson, S. E. Iismaa, and T. Liu, "Enhancing the anticancer effect of the histone deacetylase inhibitor by activating transglutaminase", Eur. J. Cancer, Vol. 48, pp. 3278-3287, 2012. crossref(new window)

35.
H. Wang, Z. Y. Lim, Y. Zhou, M. Ng, T. Lu, K. Lee, K. Sangthongpitag, K. C. Goh, X. Wangb, X. Wub, H. H. Khng, S. K. Goh, W. C. Ong, Z. Bonday, and E. T. Sun, "A acylurea connected straight chain hydroxamates as novel histone deacetylase inhibitors: synthesis, SAR, and in vivo antitumor activity", Bioorg. Med. Chem. Lett., Vol. 20, pp. 3314-3321, 2010. crossref(new window)

36.
A. Wahhab, D. Smil, A. Ajamian, M. Allan, Y. Chantigny, E. Therrien, N. Nguyen, S. Manku, S. Leit, J. Rahil, A. J. Petschner, A. H. Lu, A. Nicolescu, S. Lefebvre, S. Montcalm, M. Fournel, T. P. Yan, Z. Li, J. M. Besterman, and R. Deziel, "Sulfamides as novel histone deacetylase inhibitors", Bioorg. Med. Chem. Lett., Vol. 19, pp. 336-340, 2009. crossref(new window)

37.
S. Manku, M. Allan, N. Nguyen, A. Ajamian, J. Rodrigue, E. Therrien, J. Wang, T. Guo, J. Rahil, A. J. Petschner, A. Nicolescu, S. Lefebvre, Z. Li, M. Fournel, J. M. Besterman, R. Deziel, and A. Wahhab, "Synthesis and evaluation of lysine derived sulfamides as histone deacetylase inhibitors", Bioorg. Med. Chem. Lett., Vol. 19, pp. 1866-1870, 2009. crossref(new window)

38.
B. Chen, P. A. Petukhov, M. Jung, A. Velena, E. Eliseeva, A. Dritschilob, and A. P. Kozikowski, "Chemistry and biology of mercaptoacetamides as novel histone deacetylase inhibitors", Bioorg. Med. Chem. Lett., Vol. 15, pp. 1389-1392, 2005. crossref(new window)

39.
O. Moradei, S. Leit, N. Zhou, S. Frechette, I. Paquin, S. Raeppel, F. Gaudette, G. Bouchain, S. H. Woo, A. Vaisburg, M. Fournel, A. Kalita, A. Lu, M. C. T. Bourget, P. T. Yan, J. Liu, Z. Li, J. Rahil, A. R. MacLeod, J. M. Bestermanb, and Daniel Delormea, "Substituted N-(2-aminophenyl)-benzamides, (E)-N-(2-aminophenyl)-acrylamides and their analogues: Novel classes of histone deacetylase inhibitors", Bioorg. Med. Chem. Lett., Vol. 16, pp. 4048-4052, 2006. crossref(new window)

40.
I. Paquin, S. Raeppel, S. Leit, F. Gaudette, N. Zhou, O. Moradei, O. Saavedra, N. Bernstein, F. Raeppel, G. Bouchain, S. Frechette, S. H. Woo, A. Vaisburg, M. Fournel, A. Kalita, M. F. Robert, A. Lu, M. C. T. Bourget, P. T. Yan, J. Liu, J. Rahil, A. R. MacLeod, J. M. Besterman, Z. Lib, and Daniel Delorme, "Design and synthesis of 4-[(s-triazin-2-ylamino)methyl]-N-(2-aminophenyl)-benzamides and their analogues as a novel class of histone deacetylase inhibitors", Bioorg. Med. Chem. Lett., Vol. 18, pp. 1067-1071, 2008. crossref(new window)