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SHAPPI

Scaffold hybridization approach targeting PPIs

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EC-Contrib. €

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Partnership

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Project "SHAPPI" data sheet

The following table provides information about the project.

Coordinator
UNIVERSITY OF LEEDS 

Organization address
address: WOODHOUSE LANE
city: LEEDS
postcode: LS2 9JT
website: www.leeds.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]
 Project website https://wilson.leeds.ac.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 2017-05-01   to  2019-04-30

 Partnership

Take a look of project's partnership.

# participants  country  role  EC contrib. [€] 
1    UNIVERSITY OF LEEDS UK (LEEDS) coordinator 183˙454.00

Map

 Project objective

Protein-protein interactions (PPIs) control all cellular processes relevant to health and disease, hence an outstanding challenge in chemical biology is to develop generic approaches for PPI inhibition. Such inhibitors (or chemical probes) represent unique tools to understand biological processes and starting points for drug discovery, for treatment of multiple illnesses for which effective treatments don’t currently exist e.g. cancer.

SHAPPI will allow Zsofia Hegedus (the fellow) to join the laboratory of Andrew Wilson (host supervisor) at the University of Leeds (Host) and develop research expertise in the area of inhibiting protein-protein interactions. In doing so, she will (a) enhance her prospects to become an independent academic group leader and (b) address the need to train researchers in this key area of chemical biology and (c) develop cutting edge methods that advance peptidomimetic approaches for inhibition of protein-protein interactions. Scaffold hybridization will allow the combination of molecular scaffolds capable of hot spot mimicry with molecules that influence selectivity or potency. In combination with reversible chemistry this will allow generation of dynamic combinatorial libraries of rapid identification of selective and potent inhibitors. The fellowship will explore proteomimetic-peptide conjugates and peptide-small molecule dynamic combinatorial libraries to accelerate development of selective PPI inhibitors using two model interactions; HIF-1α/p300 and BID/BAX, both of which represent important targets for anticancer therapy.

 Publications

year authors and title journal last update
List of publications.
2019 Zsofia Hegedus, Claire M. Grison, Jennifer A. Miles, Silvia Rodriguez-Marin, Stuart L. Warriner, Michael E. Webb, Andrew J. Wilson
A catalytic protein–proteomimetic complex: using aromatic oligoamide foldamers as activators of RNase S
published pages: 3956-3962, ISSN: 2041-6520, DOI: 10.1039/c9sc00374f
Chemical Science 10/14 2019-09-25
2019 May Bakail, Silvia Rodriguez‐Marin, Zsófia Hegedüs, Marie E. Perrin, Françoise Ochsenbein, Andrew J. Wilson
Recognition of ASF1 by Using Hydrocarbon‐Constrained Peptides
published pages: 891-895, ISSN: 1439-4227, DOI: 10.1002/cbic.201800633
ChemBioChem 20/7 2019-09-25

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