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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.

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

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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