Explore the words cloud of the ANCHOR E3s project. It provides you a very rough idea of what is the project "ANCHOR E3s" about.
The following table provides information about the project.
UNIVERSITY OF DUNDEE
|Coordinator Country||United Kingdom [UK]|
|Total cost||183˙454 €|
|EC max contribution||183˙454 € (100%)|
1. H2020-EU.1.3.2. (Nurturing excellence by means of cross-border and cross-sector mobility)
|Duration (year-month-day)||from 2016-08-01 to 2018-07-31|
Take a look of project's partnership.
|1||UNIVERSITY OF DUNDEE||UK (DUNDEE)||coordinator||183˙454.00|
The Anchor E3s project proposes to establish, for the first time, an efficient protocol for the discovery and characterisation of accessible binding sites at any patch of a protein surface, regardless of its involvement in biological function. One of the motivation of the research is to develop a general approach to discover new “anchor” ligands that can enable improved plug-and-play proteolysis targeting chimeras (PROTACs) as chemical degraders of any protein of interest. The project will build on results from the host lab who identified a series of low molecular-weight fragments addressing novel patches at the surface of Cullin RING E3 ubiquitin ligases (CRLs) with currently unknown functionality, demonstrating that accessible and “ligandable” binding sites can be found on CRL surfaces. A combination of structure-based computational techniques informed by biophysical experiments and X-ray crystallography will be used to reveal, characterise, and target new ligandable binding sites at CRL surfaces. Promising anchor fragments will then be identified and grown into suitable binders, and eventually linked to assemble novel PROTACs, which will be assessed in cellular assays. The ultimate goal of the research is to develop and establish the PROTAC approach as an efficient and universal chemical biology platform for target validation, regardless of the perceived “druggability” of the targeted protein.
|year||authors and title||journal||last update|
Xavier Lucas, Inge Van Molle, Alessio Ciulli
Surface Probing by Fragment-Based Screening and Computational Methods Identifies Ligandable Pockets on the von Hippelâ€“Lindau (VHL) E3 Ubiquitin Ligase
published pages: 7387-7393, ISSN: 0022-2623, DOI: 10.1021/acs.jmedchem.8b00842
|Journal of Medicinal Chemistry 61/16||2019-06-13|
Alessio Bortoluzzi, Anastasia Amato, Xavier Lucas, Manuel Blank, Alessio Ciulli
Structural basis of molecular recognition of helical histone H3 tail by PHD finger domains
published pages: 1633-1651, ISSN: 0264-6021, DOI: 10.1042/BCJ20161053
|Biochemical Journal 474/10||2019-06-13|
Morgan S Gadd, Andrea Testa, Xavier Lucas, Kwok-Ho Chan, Wenzhang Chen, Douglas J Lamont, Michael Zengerle, Alessio Ciulli
Structural basis of PROTAC cooperative recognition for selective protein degradation
published pages: 514-521, ISSN: 1552-4450, DOI: 10.1038/nchembio.2329
|Nature Chemical Biology 13/5||2019-06-13|
Anastasia Amato, Xavier Lucas, Alessio Bortoluzzi, David Wright, Alessio Ciulli
Targeting Ligandable Pockets on Plant Homeodomain (PHD) Zinc Finger Domains by a Fragment-Based Approach
published pages: 915-921, ISSN: 1554-8929, DOI: 10.1021/acschembio.7b01093
|ACS Chemical Biology 13/4||2019-06-13|
Pedro Soares, Xavier Lucas, Alessio Ciulli
Thioamide substitution to probe the hydroxyproline recognition of VHL ligands
published pages: 2992-2995, ISSN: 0968-0896, DOI: 10.1016/j.bmc.2018.03.034
|Bioorganic & Medicinal Chemistry 26/11||2019-06-13|
Xavier Lucas, Alessio Ciulli
Recognition of substrate degrons by E3 ubiquitin ligases and modulation by small-molecule mimicry strategies
published pages: 101-110, ISSN: 0959-440X, DOI: 10.1016/j.sbi.2016.12.015
|Current Opinion in Structural Biology 44||2019-06-13|
Andrea Testa, Xavier Lucas, Guilherme V. Castro, Kwok-Ho Chan, Jane E. Wright, Andrew C. Runcie, Morgan S. Gadd, William T. A. Harrison, Eun-Jung Ko, Daniel Fletcher, Alessio Ciulli
3-Fluoro-4-hydroxyprolines: Synthesis, Conformational Analysis, and Stereoselective Recognition by the VHL E3 Ubiquitin Ligase for Targeted Protein Degradation
published pages: 9299-9313, ISSN: 0002-7863, DOI: 10.1021/jacs.8b05807
|Journal of the American Chemical Society 140/29||2019-06-13|
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The information about "ANCHOR E3S" are provided by the European Opendata Portal: CORDIS opendata.
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