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PEP-PRO-RNA SIGNED

Peptide-derived bioavailable macrocycles as inhibitors of protein-RNA and protein-protein interactions

Total Cost €

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EC-Contrib. €

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Partnership

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Project "PEP-PRO-RNA" data sheet

The following table provides information about the project.

Coordinator
STICHTING VU 

Organization address
address: DE BOELELAAN 1105
city: AMSTERDAM
postcode: 1081 HV
website: www.vu.nl

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 Netherlands [NL]
 Total cost 1˙499˙268 €
 EC max contribution 1˙499˙268 € (100%)
 Programme 1. H2020-EU.1.1. (EXCELLENT SCIENCE - European Research Council (ERC))
 Code Call ERC-2015-STG
 Funding Scheme ERC-STG
 Starting year 2016
 Duration (year-month-day) from 2016-03-01   to  2021-02-28

 Partnership

Take a look of project's partnership.

# participants  country  role  EC contrib. [€] 
1    STICHTING VU NL (AMSTERDAM) coordinator 1˙499˙268.00

Map

 Project objective

The objective of this proposal is the elucidation of general principles for the design of bioavailable peptide-derived macrocyclic compounds and their use for the development of inhibitors of protein‒protein (PPI) and protein‒RNA interactions (PRI). Over the last decade, drug discovery faced the problem of decreasing success rates which is mainly caused by the fact that numerous novel biological targets are reluctant to classic small molecule modulation. In particular, that holds true for PPIs and PRIs. Approaches that allow the modulation of these interactions provide access to therapeutic agents targeting crucial biological processes that have been considered undruggable so far. Herein, I propose the use of irregularly structured peptide binding epitopes as starting point for the design of bioactive macrocycles. In a two-step process high target affinity and bioavailability are installed: 1) Peptide macrocyclization for the stabilization of the irregular bioactive secondary structure 2) Evolution of the cyclic peptide into a bioavailable macrocyclic compound Using a well-characterized model system developed in my lab, initial design principles will be elucidated. These principles are subsequently used and refined for the development of macrocyclic PPI and PRI inhibitors. The protein‒protein and protein‒RNA complexes selected as targets are of therapeutic interest and corresponding inhibitors hold the potential to be pursued in subsequent drug discovery campaigns.

 Publications

year authors and title journal last update
List of publications.
2017 Laura Dietrich, Bernd Rathmer, Kenneth Ewan, Tanja Bange, Stefan Heinrichs, Trevor C. Dale, Dennis Schade, Tom N. Grossmann
Cell Permeable Stapled Peptide Inhibitor of Wnt Signaling that Targets β-Catenin Protein-Protein Interactions
published pages: 958-968.e5, ISSN: 2451-9456, DOI: 10.1016/j.chembiol.2017.06.013
Cell Chemical Biology 24/8 2019-07-08
2017 Adrian Glas, Eike-Christian Wamhoff, Dennis M. Krüger, Christoph Rademacher, Tom N. Grossmann
Increased Conformational Flexibility of a Macrocycle-Receptor Complex Contributes to Reduced Dissociation Rates
published pages: , ISSN: 0947-6539, DOI: 10.1002/chem.201702776
Chemistry - A European Journal 2019-07-08
2017 Dennis M. Krüger, Adrian Glas, David Bier, Nicole Pospiech, Kerstin Wallraven, Laura Dietrich, Christian Ottmann, Oliver Koch, Sven Hennig, Tom N. Grossmann
Structure-Based Design of Non-Natural Macrocyclic Peptides that Inhibit Protein-Protein Interactions
published pages: , ISSN: 0022-2623, DOI: 10.1021/acs.jmedchem.7b01221
Journal of Medicinal Chemistry 2019-07-08
2016 Philipp M. Cromm, Kerstin Wallraven, Adrian Glas, David Bier, Alois Fürstner, Christian Ottmann, Tom N. Grossmann
Constraining an Irregular Peptide Secondary Structure through Ring-Closing Alkyne Metathesis
published pages: 1915-1919, ISSN: 1439-4227, DOI: 10.1002/cbic.201600362
ChemBioChem 17/20 2019-07-08
2018 Dennis M. Krüger, Saskia Neubacher, Tom N. Grossmann
Protein–RNA interactions: structural characteristics and hotspot amino acids
published pages: 1457-1465, ISSN: 1355-8382, DOI: 10.1261/rna.066464.118
RNA 24/11 2019-05-09
2018 Marta Pelay-Gimeno, Tanja Bange, Sven Hennig, Tom N. Grossmann
In Situ Cyclization of Native Proteins: Structure-Based Design of a Bicyclic Enzyme
published pages: 11334-11340, ISSN: 0044-8249, DOI: 10.1002/ange.201804506
Angewandte Chemie 130/35 2019-05-09

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