Histone Deacetylases and their Inhibitors in Colorectal Cancer Therapy: Current Evidence and Future Considerations

Nikolaos Garmpis; Christos Damaskos; Anna Garmpi; Afroditi Nonni; Vasiliki E Georgakopoulou; Efstathios Antoniou; Dimitrios Schizas; Panagiotis Sarantis; Alexandros Patsouras; Athanasios Syllaios; Christos Vallilas; Evangelos Koustas; Konstantinos Kontzoglou; Nikolaos Trakas; Dimitrios Dimitroulis

doi:10.2174/0929867328666210915105929

Histone Deacetylases and their Inhibitors in Colorectal Cancer Therapy: Current Evidence and Future Considerations

Curr Med Chem. 2022;29(17):2979-2994. doi: 10.2174/0929867328666210915105929.

Authors

Nikolaos Garmpis^{1

2}, Christos Damaskos^{2

3}, Anna Garmpi⁴, Afroditi Nonni⁵, Vasiliki E Georgakopoulou⁶, Efstathios Antoniou^{1

2}, Dimitrios Schizas⁷, Panagiotis Sarantis⁸, Alexandros Patsouras², Athanasios Syllaios⁷, Christos Vallilas⁸, Evangelos Koustas⁸, Konstantinos Kontzoglou^{1

2}, Nikolaos Trakas⁹, Dimitrios Dimitroulis¹

Affiliations

¹ Second Department of Propedeutic Surgery, Laiko General Hospital, Medical School, National and Kapodistrian University of Athens, Athens, Greece.
² N.S. Christeas Laboratory of Experimental Surgery and Surgical Research, Medical School, National and Kapodistrian University of Athens, Athens, Greece.
³ Renal Transplantation Unit, Laiko General Hospital, Athens, Greece.
⁴ First Department of Propedeutic Internal Medicine, Laiko General Hospital, Medical School, National and Kapodistrian University of Athens, Athens, Greece.
⁵ First Department of Pathology, Medical School, National and Kapodistrian University of Athens, Athens, Greece.
⁶ Department of Pulmonology, Laiko General Hospital, Athens, Greece.
⁷ First Department of Surgery, Laiko General Hospital, Medical School, National and Kapodistrian University of Athens, Athens, Greece.
⁸ Molecular Oncology Unit, Department of Biological Chemistry, Medical School, National and Kapodistrian University of Athens, Athens, Greece.
⁹ Department of Biochemistry, Sismanogleio Hospital, Athens, Greece.

PMID: 34525905
DOI: 10.2174/0929867328666210915105929

Abstract

Colorectal cancer (CRC) comprises a heterogeneous group of gastrointestinal tract tumors. It is a multifactorial disease, and a plethora of distinct factors are involved in its pathogenesis and pathophysiology. The development of CRC is not limited to genetic changes, but epigenetic and environmental factors are also involved. Among the epigenetic factors, histone deacetylases (HDACs), a group of epigenetic enzymes that regulate gene expression, have been reported to be over-expressed in CRC. HDACs and their inhibitors seem to play an important role in the molecular pathophysiology of CRC. The aim of this review was to define the role of HDAC inhibitors as potential anticancer agents against CRC.

Keywords: HDAC; HDACI; Histone; colorectal cancer; deacetylase; epigenetics; inhibitors; targeted therapy.

Publication types

Review

MeSH terms

Antineoplastic Agents* / pharmacology
Antineoplastic Agents* / therapeutic use
Colorectal Neoplasms* / pathology
Histone Deacetylase Inhibitors / pharmacology
Histone Deacetylase Inhibitors / therapeutic use
Histone Deacetylases / metabolism
Humans

Substances

Antineoplastic Agents
Histone Deacetylase Inhibitors
Histone Deacetylases