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Themed collection Epigenetics

15 items
Review Article

Can we use the epigenetic bioactivity of caloric restriction and phytochemicals to promote healthy ageing?

Why is it relevant to propose epigenetic “Nutricures” to prevent diseases linked with ageing?

Graphical abstract: Can we use the epigenetic bioactivity of caloric restriction and phytochemicals to promote healthy ageing?
From the themed collection: Epigenetics
Review Article

Repair of methyl lesions in RNA by oxidative demethylation

Nucleic acid methylation is one of the most important epigenetic modifications that have been studied intensively for the past several decades.

Graphical abstract: Repair of methyl lesions in RNA by oxidative demethylation
From the themed collection: Epigenetics
Review Article

Discovery of an orally active subtype-selective HDAC inhibitor, chidamide, as an epigenetic modulator for cancer treatment

Tumorigenesis is maintained through a complex interplay of multiple cellular biological processes and is regulated to some extent by epigenetic control of gene expression.

Graphical abstract: Discovery of an orally active subtype-selective HDAC inhibitor, chidamide, as an epigenetic modulator for cancer treatment
From the themed collection: Epigenetics
Open Access Review Article

Structural biology and chemistry of protein arginine methyltransferases

PRMT inhibitors can compete with cofactor, substrate, or bind at allosteric sites found in the active or inactive states.

Graphical abstract: Structural biology and chemistry of protein arginine methyltransferases
From the themed collection: Epigenetics
Concise Article

Structure–activity relationship studies of SETD8 inhibitors

Comprehensive SAR studies of the first substrate-competitive SETD8 inhibitor led to the discovery of interesting SAR trends and novel analogs.

Graphical abstract: Structure–activity relationship studies of SETD8 inhibitors
From the themed collection: Epigenetics
Concise Article

Design, synthesis, and preliminary bioactivity studies of substituted purine hydroxamic acid derivatives as novel histone deacetylase (HDAC) inhibitors

Histone deacetylase (HDAC) is a clinically validated target for anti-tumor therapy. In order to increase HDAC inhibition and efficiency, we developed a series of novel substituted purine hydroxamic acids as potent HDAC inhibitors.

Graphical abstract: Design, synthesis, and preliminary bioactivity studies of substituted purine hydroxamic acid derivatives as novel histone deacetylase (HDAC) inhibitors
From the themed collection: Epigenetics
Open Access Concise Article

Optimisation of a triazolopyridine based histone demethylase inhibitor yields a potent and selective KDM2A (FBXL11) inhibitor

Compound 35 is a potent and selective triazolopyridine inhibitor of the lysine demethylase KDM2A (pIC50 7.2).

Graphical abstract: Optimisation of a triazolopyridine based histone demethylase inhibitor yields a potent and selective KDM2A (FBXL11) inhibitor
From the themed collection: Epigenetics
Concise Article

Design and chemoproteomic functional characterization of a chemical probe targeted to bromodomains of BET family proteins

Selectivity of a PFI-1 based BET bromodomain probe was demonstrated using affinity capture in nuclear extracts from human cells.

Graphical abstract: Design and chemoproteomic functional characterization of a chemical probe targeted to bromodomains of BET family proteins
From the themed collection: Epigenetics
Open Access Concise Article

Identification of 2,4-diamino-6,7-dimethoxyquinoline derivatives as G9a inhibitors

With the aim of discovering novel G9a inhibitory chemotypes, we have identified a new quinoline inhibitor scaffold and better defined the pharmacophoric features of the central heterocycle.

Graphical abstract: Identification of 2,4-diamino-6,7-dimethoxyquinoline derivatives as G9a inhibitors
From the themed collection: Epigenetics
Concise Article

3,5-Diamino-1,2,4-triazoles as a novel scaffold for potent, reversible LSD1 (KDM1A) inhibitors

Compounds 6 and 7 represent the first reversible LSD1 inhibitors with minimal cytotoxicity in vitro.

Graphical abstract: 3,5-Diamino-1,2,4-triazoles as a novel scaffold for potent, reversible LSD1 (KDM1A) inhibitors
From the themed collection: Epigenetics
Concise Article

An azumamide C analogue without the zinc-binding functionality

Histone deacetylase (HDAC) inhibitors have attracted considerable attention due to their promise as therapeutic agents.

Graphical abstract: An azumamide C analogue without the zinc-binding functionality
From the themed collection: Epigenetics
Open Access Concise Article

Pyrido- and benzisothiazolones as inhibitors of histone acetyltransferases (HATs)

We present structure–activity studies on pyrido- and benzisothiazolones as histone acetyltransferase (HAT) inhibitors. Distinct subtype-selectivity profiles were obtained in vitro that correlate with cytotoxicity profiles on cancer cells.

Graphical abstract: Pyrido- and benzisothiazolones as inhibitors of histone acetyltransferases (HATs)
From the themed collection: Epigenetics
Concise Article

Structure-based approaches towards identification of fragments for the low-druggability ATAD2 bromodomain

Fragments for the development of ATAD2 bromodomain inhibitors have been identified and characterized by NMR and co-crystallization.

Graphical abstract: Structure-based approaches towards identification of fragments for the low-druggability ATAD2 bromodomain
From the themed collection: Epigenetics
Concise Article

Evaluation of functional groups as acetyl-lysine mimetics for BET bromodomain inhibition

This work provides new insights into a range of acetyl-lysine mimetics as BET bromodomain inhibitors.

Graphical abstract: Evaluation of functional groups as acetyl-lysine mimetics for BET bromodomain inhibition
From the themed collection: Epigenetics
Concise Article

Synthesis of hybrid anticancer agents based on kinase and histone deacetylase inhibitors

A HDAC, kinase inhibitor hybrid, (Z)-N1-(3-((1H-pyrrol-2-yl)methylene)-2-oxoindolin-5-yl)-N8-hydroxyoctanediamide, 6, showed impressive anticancer action in a number of biochemical and cell-based assays.

Graphical abstract: Synthesis of hybrid anticancer agents based on kinase and histone deacetylase inhibitors
From the themed collection: Epigenetics
15 items

About this collection

A MedChemComm themed issue guest edited by Dr Mark Bunnage and Professor James E. Bradner highlighting some of the latest exciting research from across the breadth of epigenetics research.

New articles will be added to this collection as they are published.

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