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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.

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

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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