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TEDCIP SIGNED

Targeting epigenetic demethylases: development of covalent inhibitors and PROTACs (Proteolysis Targeting Chimeras).

Total Cost €

0

EC-Contrib. €

0

Partnership

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 TEDCIP project word cloud

Explore the words cloud of the TEDCIP project. It provides you a very rough idea of what is the project "TEDCIP" about.

readers    dna    certain    gene    erasers    aberrant    diseases    phenotype    e3    containing    plastic    kdm    potent    neurological    itself    underlying    residues    structural    inherited    methylated    modification    partly    influence    tags    oxygenases    ligases    therapeutic    unlike    genome    similarities    ubiquitination    despite    catalyzed    kdms    2og    removal    epigenetic    chemical    recruiting    tails    heritable    regulate    selective    proteins    fe    mainly    manner    lysine    protein    modifications    aging    patterns    epigenetics    levels    inhibitors    dependent    onset    environmental    methyl    sequence    oxoglutarate    writers    individual    mechanisms    protacs    cardiovascular    progression    subsequent    demethylases    covalent    cell    cancer    transferases    involve    disease    jmjc    domains    dynamically    reported    methylation    mediated    groups    drugs    induce    histone    proteasome    degradation    selectivity    lysines    types    intracellular    proteolysis    expression    chimeras    domain    identification    inflammation   

Project "TEDCIP" data sheet

The following table provides information about the project.

Coordinator
THE CHANCELLOR, MASTERS AND SCHOLARS OF THE UNIVERSITY OF OXFORD 

Organization address
address: WELLINGTON SQUARE UNIVERSITY OFFICES
city: OXFORD
postcode: OX1 2JD
website: www.ox.ac.uk

contact info
title: n.a.
name: n.a.
surname: n.a.
function: n.a.
email: n.a.
telephone: n.a.
fax: n.a.

 Coordinator Country United Kingdom [UK]
 Total cost 183˙454 €
 EC max contribution 183˙454 € (100%)
 Programme 1. H2020-EU.1.3.2. (Nurturing excellence by means of cross-border and cross-sector mobility)
 Code Call H2020-MSCA-IF-2016
 Funding Scheme MSCA-IF-EF-ST
 Starting year 2017
 Duration (year-month-day) from 2017-08-01   to  2019-07-31

 Partnership

Take a look of project's partnership.

# participants  country  role  EC contrib. [€] 
1    THE CHANCELLOR, MASTERS AND SCHOLARS OF THE UNIVERSITY OF OXFORD UK (OXFORD) coordinator 183˙454.00

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 Project objective

Epigenetics is the study of heritable changes in phenotype that does not involve changes in the underlying DNA sequence. Epigenetic modifications are partly inherited, but unlike the genome itself, are cell specific, plastic, and its mechanisms are affected by different factors and processes such as aging, environmental factors or the use of drugs. The epigenetic changes are the result of epigenetic tags (chemical tags) that can determine gene expression. There are two main types of epigenetic modifications: DNA methylation and histone modifications. Many diseases such as cancer, inflammation, neurological and cardiovascular diseases can be related to aberrant histone modification patterns. Since Histone modifications are mainly carried out by three types of proteins (writers, readers and erasers) there is great therapeutic interest in these proteins, since they may influence disease onset and progression. However, the identification of potent and selective inhibitors is challenging due to structural similarities between individual domains of the ‘epigenetic’ proteins. Histone demethylases and methyl transferases, dynamically regulate the histone methylation levels. Removal of methyl groups from methylated lysines on histone tails is catalyzed by lysine demethylases (KDMs) in a sequence- and methylation-state dependent manner. Among the different KDMs, the JmjC-domain containing KDMs are Fe(II)- and 2-oxoglutarate (2OG)-dependent oxygenases. Despite some KDM inhibitors have been reported, achieving selectivity remains a major challenge. In order to achieve the required selectivity, two different approaches are considered in the current proposal: 1) development of covalent inhibitors with specific residues of certain KDMs and 2) development of Proteolysis Targeting Chimeras (PROTACs) to control intracellular protein levels by recruiting the KDMs to E3 ligases to induce their ubiquitination and subsequent proteasome mediated degradation.

 Publications

year authors and title journal last update
List of publications.
2019 Saleta Vazquez‐Rodriguez
Epigenetic Drug Discovery. Edited by Wolfgang Sippl and Manfred Jung
published pages: , ISSN: 1860-7179, DOI: 10.1002/cmdc.201900615
ChemMedChem 2019-12-17
2019 Saleta Vazquez-Rodriguez, Miranda Wright, Catherine M. Rogers, Adam P. Cribbs, Srikannathasan Velupillai, Martin Philpott, Henry Lee, James E. Dunford, Kilian V. M. Huber, Matthew B. Robers, James D. Vasta, Marie-Laetitia Thezenas, Sarah Bonham, Benedikt Kessler, James Bennett, Oleg Fedorov, Florence Raynaud, Adam Donovan, Julian Blagg, Vassilios Bavetsias, Udo Oppermann, Chas Bountra, Akane Kawam
Design, Synthesis and Characterization of Covalent KDM5 Inhibitors
published pages: 515-519, ISSN: 1433-7851, DOI: 10.1002/anie.201810179
Angewandte Chemie International Edition 58/2 2019-11-08

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