Histone deacetylase inhibitors

Marzena Baran, Paulina Anna Miziak, Katarzyna Bonio

DOI: http://dx.doi.org/10.12775/JEHS.2020.10.08.043

Abstract


The human genome is contained in chromatin, which is a complex macromolecular complex. It is made of DNA, histones and non-histone proteins. The structure of chromatin and the process of its rearrangement regulate the process of transcription, and hence gene expression.  Deacetylase (HDAC) is a group of enzymes that catalyzes the cleavage of acetyl groups from lysine residues in histone and nonhistone proteins. This reaction is catalyzed by zinc or NAD + ions [3]. Histone deacetylases are present in the cytoplasm or nucleus of eukaryotes [4, 5]. These enzymes have been divided into 5 classes (I, IIa, IIb, III and IV) due to the similarity in structure and origin. Vorinostat is one of the most studied HDAC inhibitors. It belongs to the second generation polar-planar hydroxamic acid derivatives that inhibit class I and II histone deacetylases. Panobinostat and belinostat are HDAC inhibitors derived from hydroxamic acid that have also entered clinical trials. Valproic acid, from the group of aliphatic acids, belongs to inhibitors of class I and IIα deacetylases and is an established drug anticonvulsants. Histone deacetylase inhibitors may be useful in the treatment of neoplasms because they influence the action of factors related to cell proliferation, may cause cell cycle arrest, and coordinate the action of apoptotic factors and induce apoptosis. There are several deacetylase inhibitors available as drugs and are in different phases of clinical trials. They differ in potency and enzyme specificity. However, it is still unknown which deacetylases are essential for initiating and sustaining metabolic pathways leading to tumor development.


Keywords


inhibitors; histone deacetylase; cancer

Full Text:

PDF

References


. Chen P-J i inni, Epigenetic modifications by histone deacetylases: Biological implications and therapeutic potential in liver fibrosis, Biochimie, 2015 Vol.116, Pages 61-69

. Qiu X i inni, Histone deacetylases inhibitors (HDACis) as novel therapeutic application in various clinical diseases, Progress in Neuro-Psychopharmacology and Biological Psychiatry, 2017, Vol. 72

. Seto E., Yoshida M., Erasers of histone acetylation: the histone deacetylase enzymes,

Cold Spring Harb Perspect Biol., 2014,6(4)

. Seidel C. i inni, , Histone deacetylase 6 in health and disease,

Epigenomics, 2015, 7(1), 103-18

. Wawruszak A i inni., Histone Deacetylase Inhibitors and Phenotypical Transformation of Cancer Cells, Cancers., 2019, 11(2), 148

. Grabarska A, Dmoszyńska-Graniczka M, Nowosadzka E, Stepulak A. Inhibitory deacetylaz histonów - mechanizmy działania na poziomie molekularnym i zastosowania kliniczne [Histone deacetylase inhibitors - molecular mechanisms of actions and clinical applications]. Postepy Hig Med Dosw (Online). 2013 Aug 2;67:722-35. Polish. doi: 10.5604/17322693.1061381. PMID: 24018438.

. Kuendgen A., Knipp S., Fox F., Strupp C., Hildebrandt B., Steidl C., Germing U., Haas R., Gattermann N.: Results of a phase 2 study of valproic acid alone or in combination with all-trans retinoic acid in 75 patients with myelodysplastic syndrome and relapsed or refractory acute myeloid leukemia. Ann. Hematol., 2005; 84, Suppl 1: 61-66

. Eckschlager T, Plch J, Stiborova M, Hrabeta J. Histone Deacetylase Inhibitors as Anticancer Drugs. Int J Mol Sci. 2017 Jul 1;18(7):1414. doi: 10.3390/ijms18071414. PMID: 28671573; PMCID: PMC5535906.


Article Metrics

Metrics Loading ...

Metrics powered by PLOS ALM




Journal of Education, Health and Sport formerly Journal of Health Sciences

Declaration on the original version.

Editors indicates that the main version of the magazine is to issue a "electronic".

The journal has had 5 points in Ministry of Science and Higher Education parametric evaluation. § 8. 2) and § 12. 1. 2) 22.02.2019.

1223 Journal of Education, Health and Sport eISSN 2391-8306 7

ISSN 2391-8306 formerly ISSN: 1429-9623 / 2300-665X

Archives 2011 - 2014

PBN 2011 - 2014

https://pbn.nauka.gov.pl/sedno-webapp/search?search&searchCategory=WORK&filter.inJournal=36616

POL-index 2011 - 2014

https://pbn.nauka.gov.pl/polindex-webapp/browse/journal/journal-32a319c5-a850-4f44-ba70-1418a6087655

BASE 2011 - 2014

https://www.base-search.net/Search/Results?lookfor=Journal+of+Health+Sciences+%28Radom%29&type=all&oaboost=1&ling=1&name=&thes=&refid=dcrespl&newsearch=1

http://elibrary.ru/contents.asp?titleid=37467

http://journal.rsw.edu.pl/index.php/JHS/issue/archive

Indexed in Bases, Bazy indeksacyjne: ERIH Plus, Worldcat, PBN/POL-Index, ICI Journals Master List, Directory of Open Access Journals (DOAJ), ZBD, Ulrich's periodicals, Google Scholar, Polska Bibliografia Lekarska, EuroPub database, NLM Catalog Result - NCBI, BASE, Russian Sciences Index, Arianta.

https://zdb-katalog.de/title.xhtml?idn=1080187162

https://europub.co.uk/journals/22625

US NLM = 101679844

101679844 - NLM Catalog Result - NCBI

https://www.ncbi.nlm.nih.gov/nlmcatalog/101679844

Find a library that holds this journal: http://worldcat.org/issn/23918306

 

PBN Poland

https://pbn.nauka.gov.pl/sedno-webapp/journals/49068

POL-index

https://pbn.nauka.gov.pl/polindex-webapp/browse/journal/journal-c39c8169-88d2-45db-9e7f-d948ce9981c4

BASE

https://www.base-search.net/Search/Results?join=AND&bool0[]=AND&lookfor0[]=2391-8306&type0[]=all&page=11&l=pl&oaboost=1&refid=dcpagepl

Redaction, Publisher and Editorial Office

Publisher and Editorial Office
Department of Physical Culture,
Faculty of Earth Sciences and Spatial Management,
Nicolaus Copernicus University in Toruń, Poland
Address: Str. Lwowska 1, 87-100 Toruń, Poland

  Open Access ISSN 2391-8306 formerly ISSN: 1429-9623 / 2300-665X

The journal has been approved for inclusion in ERIH PLUS.

The ERIH PLUS listing of the journal is available at https://dbh.nsd.uib.no/publiseringskanaler/erihplus/periodical/info?id=485984

Indexed in Index Copernicus Journals Master List.

http://journals.indexcopernicus.com/Journal+of+Education+Health+and+Sport,p24782242,3.html

ICV 2018 = 95.95 ICV 2017 = 91.30 ICV 2016 = 84.69 ICV 2015 = 93.34 ICV 2014 = 89.51 Standardized Value: 8.27 ICV 2013: 7.32 ICV 2012: 6.41 ICV 20115.48

RG Journal Impact: 0.18 *

*This value is calculated using ResearchGate data and is based on average citation counts from work published in this journal. The data used in the calculation may not be exhaustive.

RG Journal impact history

2020Available summer 2021
2018 / 20190.18
20170.07
20160.03

RG Journal impact over time

RG Journal impact
0.180.160.140.120.100.080.060.040.02201620172018
  

Indexed in Polish Scholarly Bibliography (PBN) (PBN Polska Bibliografia Naukowa) (https://pbn.nauka.gov.pl/journals/36616)

is a portal of the Polish Ministry of Science and Higher Education, collecting information on publications of Polish scientists and on Polish and foreign scholarly journals. Polish Scholarly Bibliograhpy is a part of POL-on - System of Information on Higher Education. It is operated by the Interdisciplinary Centre for Mathematical and Computational Modelling, University of Warsaw.

Indexed in Russian Sciences Index Российский индекс научного цитирования (РИНЦ) http://elibrary.ru/contents.asp?titleid=37467

Indexed in Arianta Polish scientific and professional electronic journals Aneta Drabek i Arkadiusz Pulikowski

(http://www1.bg.us.edu.pl/bazy/czasopisma/czasop_full.asp?id=3595)

Partnerzy platformy czasopism