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ProCenDecl SIGNED

Synthesis and validation of chemical Probes for Centrosome Declustering: development of potent and selective anti-cancer agents.

Total Cost €

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EC-Contrib. €

0

Partnership

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 ProCenDecl project word cloud

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

polimerase    inhibit    chromosomes    completely    investigation    parps    advantage    poly    daughter    anti    cells    discovery    aberrant    microtubules    contrary    form    adp    catastrophe    point    16    centrosomes    selective    family    inhibitors    conjugation    tools    ligation    photoaffinity    clustering    druggability    drugs    tnks1    tankyrase    polymerase    phtalazinone    employed    orally    accumulate    declustering    bipolar    ribose    reports    first    cancer    biorthogonal    spindles    mechanism    inhibitor    acquired    technologies    consequent    derivative    seems    action    chemical    extra    az0108    potent    copies    organization    mode    synthesize    astrazeneca    responsible    exploited    survival    normal    compound    starting    parp    extensive    led    potently    tumor    segregation    uneven    multipolar    organelles    cell    series    proteomics    sar    tendency    mitotic    ribosylation    spindle    prevention    enzyme    leads    az9482    provides    centrosome    pseudo    specificity    library    division   

Project "ProCenDecl" data sheet

The following table provides information about the project.

Coordinator
IMPERIAL COLLEGE OF SCIENCE TECHNOLOGY AND MEDICINE 

Organization address
address: SOUTH KENSINGTON CAMPUS EXHIBITION ROAD
city: LONDON
postcode: SW7 2AZ
website: http://www.imperial.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-2017
 Funding Scheme MSCA-IF-EF-ST
 Starting year 2019
 Duration (year-month-day) from 2019-09-01   to  2021-08-31

 Partnership

Take a look of project's partnership.

# participants  country  role  EC contrib. [€] 
1    IMPERIAL COLLEGE OF SCIENCE TECHNOLOGY AND MEDICINE UK (LONDON) coordinator 183˙454.00

Map

 Project objective

Cancer cells have the tendency to accumulate extra copies of centrosomes, organelles responsible for the microtubules' organization during cell division. In normal cells, an aberrant number of centrosomes leads to the formation of multipolar spindles, uneven segregation of chromosomes between daughter cells and consequent mitotic catastrophe. On the contrary, cancer cells are able to form a pseudo-bipolar mitotic spindle by a process called centrosome clustering, which provides survival advantage for tumor cells. The specificity of this process can be exploited as a potential novel target for the development of highly selective anti-cancer drugs. The mechanism of centrosome clustering is not completely understood. Particularly, from recent reports it seems that ADP ribosylation factors tankyrase (TNKS1) and ADP-ribose polimerase 16 (PARP-16) have a significant role in the prevention of multipolar spindle formation. Based on these findings and the already druggability of poly (ADP-ribose) polymerase (PARP) enzyme family, a SAR study on phtalazinone PARP inhibitors from AstraZeneca's compound library was carried out. This study led to the discovery of AZ9482, a potent inhibitor of centrosome clustering, and AZ0108 an orally available derivative that is able to potently inhibit PARPs 1/2/6. AZ9482 as well as AZ0108 can be used as a starting point to design and synthesize a first series of chemical proteomics tools, that will allow an extensive investigation of the centrosome declustering mechanism. All currently available technologies in the field of target discovery will be employed, including photoaffinity ligation and biorthogonal conjugation. The acquired knowledge can be used to design novel highly specific and potent anti-cancer drugs that inhibit centrosome clustering with a specific mode of action.

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The information about "PROCENDECL" are provided by the European Opendata Portal: CORDIS opendata.

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