Beyond the Selective Inhibition of Histone Deacetylase 6.

Mini Rev Med Chem

LASSBio, Institute of Biomedical Sciences, Federal University of Rio de Janeiro, 21941-902, Rio de Janeiro, RJ Brazil.

Published: February 2017

Histone deacetylase 6 (HDAC6) catalyses the removal of acetyl groups from the lysine residues of a series of non-histone proteins, e.g., α-tubulin, Hsp90 and cortactin. HDAC6 is a unique deacetylase enzyme that is related to various processes that may be important in oncological, immunological and neurological fields, which makes the study of selective inhibitors extremely important to understand the function of this enzyme and to validate HDAC6 as a drug target through the development of clinical candidates. Therefore, this review describes the structure-activity and structureselectivity relationships of HDAC6 inhibitors, which were divided into two main classes, bulky and lipophilic cap groups and inhibitors with phenyl linkers.

Download full-text PDF

Source
http://dx.doi.org/10.2174/1389557516666160428115959DOI Listing

Publication Analysis

Top Keywords

histone deacetylase
8
selective inhibition
4
inhibition histone
4
deacetylase histone
4
hdac6
4
deacetylase hdac6
4
hdac6 catalyses
4
catalyses removal
4
removal acetyl
4
acetyl groups
4

Similar Publications

Organisms with smaller genomes often perform multiple functions using one multi-subunit protein complex. The Silent Information Regulator complex (SIRc) carries out all of the core functions of heterochromatin. SIR complexes first drive the initiation and spreading of histone deacetylation in an iterative manner.

View Article and Find Full Text PDF

This review provides a comprehensive overview of the role of G9a/EHMT2, focusing on its structure and exploring the impact of its pharmacological and/or gene inhibition in various neurological diseases. In addition, we delve into the advancements in the design and synthesis of G9a/EHMT2 inhibitors, which hold promise not only as a treatment for neurodegeneration diseases but also for other conditions, such as cancer and malaria. Besides, we presented the discovery of dual therapeutic approaches based on G9a inhibition and different epigenetic enzymes like histone deacetylases, DNA methyltransferases, and other lysine methyltransferases.

View Article and Find Full Text PDF

Exosomal circ_0006896 promotes AML progression via interaction with HDAC1 and restriction of antitumor immunity.

Mol Cancer

January 2025

Department of Hematology, Qilu Hospital of Shandong University, No.117, West of Wenhua Road, Jinan, Shandong, 250012, People's Republic of China.

Background: Drug resistance and immune escape continue to contribute to poor prognosis in AML. Increasing evidence suggests that exosomes play a crucial role in AML immune microenvironment.

Methods: Sanger sequencing, RNase R and fluorescence in situ hybridization were performed to confirm the existence of circ_0006896.

View Article and Find Full Text PDF

De novo shoot regeneration, characterized by the emergence of adventitious shoots from excised or damaged tissues or organs in vitro, is regulated by the complex interplay between genetic and epigenetic regulatory mechanisms. However, the specific effect of histone deacetylation on shoot regeneration remains poorly understood. This study investigated the effects of trichostatin A (TSA), a histone deacetylase inhibitor, on shoot regeneration in callus derived from root explants.

View Article and Find Full Text PDF

Advancements in understanding the role and mechanism of sirtuin family (SIRT1-7) in breast cancer management.

Biochem Pharmacol

January 2025

School of Bio-Sciences and Technology, Vellore Institute of Technology, Vellore, Tamil Nadu 632014, India. Electronic address:

Breast cancer (BC) is the most prevalent type of cancer in women worldwide and it is classified into a few distinct molecular subtypes based on the expression of growth factor and hormone receptors. Though significant progress has been achieved in the search for novel medications through traditional and advanced approaches, still we need more efficacious and reliable treatment options to treat different types and stages of BC. Sirtuins (SIRT1-7) a class III histone deacetylase play a major role in combating various cancers including BC.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!