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Themed collection Epigenetics

12 articles
Review Article

Targeting epigenetic modifiers: Inhibitors of histone methyltransferases

Reversible histone methylation is an emerging new target in the field of epigenetic regulation. Here, we review histone methyltransferases in light of their role in disease formation and with regard to the state of the art in drug discovery.

Graphical abstract: Targeting epigenetic modifiers: Inhibitors of histone methyltransferases
From the themed collection: Epigenetics
Review Article

Small molecules DNA methyltransferases inhibitors

This review describes current knowledge concerning DNA methyltransferases (DNMT) biology and the two main classes of DNMT inhibtors.

Graphical abstract: Small molecules DNA methyltransferases inhibitors
From the themed collection: MedChemComm 2012 review articles
Review Article

Epigenetics—an emerging and highly promising source of new drug targets

Epigenetic modifications to DNA and its associated histone proteins are major influences on gene expression. This regulatory process is disrupted in cancer and a range of chronic human diseases, and provides attractive new intervention points and targets for drug discovery.

Graphical abstract: Epigenetics—an emerging and highly promising source of new drug targets
From the themed collection: MedChemComm 2012 review articles
Review Article

Development of second generation epigenetic agents

This review focuses on the progress in the development of the second generation of epigenetic modifiers able to modulate histone marks, and restore normal gene transcription.

Graphical abstract: Development of second generation epigenetic agents
From the themed collection: MedChemComm 2012 review articles
Review Article

Inhibition of bromodomain-mediated proteinprotein interactions as a novel therapeutic strategy

Small molecule inhibitors of acetyl lysine–bromodomain interactions emerge as novel epigenetic tools with potential for therapeutic approaches.

Graphical abstract: Inhibition of bromodomain-mediated protein–protein interactions as a novel therapeutic strategy
From the themed collection: MedChemComm 2012 review articles
Review Article

Polyamine-based small molecule epigenetic modulators

Multiple series of HDAC and LSD1 inhibitors have been developed that increase histone lysine methylation and promote the re-expression of aberrantly silenced genes that are important in human cancer..

Graphical abstract: Polyamine-based small molecule epigenetic modulators
From the themed collection: Epigenetics
Concise Article

Rhodanine carboxylic acids as novel inhibitors of histone acetyltransferases

Virtual screening has identified rhodanine containing carboxylic acids as new inhibitors of histone acetyltransferases.

Graphical abstract: Rhodanine carboxylic acids as novel inhibitors of histone acetyltransferases
From the themed collection: Epigenetics
Concise Article

Developing novel non-hydroxamate histone deacetylase inhibitors: the chelidamic warhead

The dimethyl 4-hydroxypyridine-2,6-dicarboxylate is a valuable scaffold for HDAC inhibitor design as a replacement of the well-known hydroxamate function.

Graphical abstract: Developing novel non-hydroxamate histone deacetylase inhibitors: the chelidamic warhead
From the themed collection: Epigenetics
Concise Article

Binding free energy calculations and biological testing of novel thiobarbiturates as inhibitors of the human NAD+ dependent histone deacetylase Sirt2

Novel thiobarbiturates were identified by virtual screening and MM-PBSA calculation as potent sirtuin inhibitors which represent useful probes for cellular studies.

Graphical abstract: Binding free energy calculations and biological testing of novel thiobarbiturates as inhibitors of the human NAD+ dependent histone deacetylase Sirt2
From the themed collection: Epigenetics
Concise Article

Self-hydroxylation of the splicing factor lysyl hydroxylase, JMJD6

The lysyl hydroxylase, JMJD6 undergoes self-hydroxylation resulting in the 5S-hydroxylysine product.

Graphical abstract: Self-hydroxylation of the splicing factor lysyl hydroxylase, JMJD6
From the themed collection: Epigenetics
Concise Article

Click JAHAs: conformationally restricted ferrocene-based histone deacetylase inhibitors

The ferrocene analogue 4b had an IC50 = 4 nM (HDAC1), 180 nM (HDAC8) and was effective in a Xenopus model of tubulin deacetylation. Analogue 4a displayed mainly μM IC50 values against HDACs apart from HDAC6 (IC50 = 69 nM).

Graphical abstract: Click JAHAs: conformationally restricted ferrocene-based histone deacetylase inhibitors
From the themed collection: Epigenetics
Concise Article

Structure–activity relationships of methyl-lysine reader antagonists

The structure–activity relationships for small molecule antagonists of the Malignant Brain Tumor (MBT) domain family of methyl-lysine readers are described and activity demonstrated in histone peptide pull-down assays.

Graphical abstract: Structure–activity relationships of methyl-lysine reader antagonists
From the themed collection: Epigenetics
12 articles

About this collection

MedChemComm is delighted to publish this collection of articles in the emerging field of epigenetics research, guest edited by Dr Mark Bunnage (Pfizer) and Professor Rasmus Prætorius Clausen (University of Copenhagen).

Read their introduction to the issue on the MedChemComm blog.

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