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Anchoring ligandable binding sites at E3 ligase surfaces for plug-and-play PROTACs.

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Publications

Structural basis of PROTAC cooperative recognition for selective protein degradation

Author(s): Morgan S Gadd, Andrea Testa, Xavier Lucas, Kwok-Ho Chan, Wenzhang Chen, Douglas J Lamont, Michael Zengerle, Alessio Ciulli
Published in: Nature Chemical Biology, Issue 13/5, 2017, Page(s) 514-521, ISSN 1552-4450
DOI: 10.1038/nchembio.2329

Structural basis of molecular recognition of helical histone H3 tail by PHD finger domains

Author(s): Alessio Bortoluzzi, Anastasia Amato, Xavier Lucas, Manuel Blank, Alessio Ciulli
Published in: Biochemical Journal, Issue 474/10, 2017, Page(s) 1633-1651, ISSN 0264-6021
DOI: 10.1042/BCJ20161053

Recognition of substrate degrons by E3 ubiquitin ligases and modulation by small-molecule mimicry strategies

Author(s): Xavier Lucas, Alessio Ciulli
Published in: Current Opinion in Structural Biology, Issue 44, 2017, Page(s) 101-110, ISSN 0959-440X
DOI: 10.1016/j.sbi.2016.12.015

Targeting Ligandable Pockets on Plant Homeodomain (PHD) Zinc Finger Domains by a Fragment-Based Approach

Author(s): Anastasia Amato, Xavier Lucas, Alessio Bortoluzzi, David Wright, Alessio Ciulli
Published in: ACS Chemical Biology, Issue 13/4, 2018, Page(s) 915-921, ISSN 1554-8929
DOI: 10.1021/acschembio.7b01093

Thioamide substitution to probe the hydroxyproline recognition of VHL ligands


Published in: ISSN 0968-0896
DOI: 10.1016/j.bmc.2018.03.034

3-Fluoro-4-hydroxyprolines: Synthesis, Conformational Analysis, and Stereoselective Recognition by the VHL E3 Ubiquitin Ligase for Targeted Protein Degradation

Author(s): 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
Published in: Journal of the American Chemical Society, Issue 140/29, 2018, Page(s) 9299-9313, ISSN 0002-7863
DOI: 10.1021/jacs.8b05807

Surface Probing by Fragment-Based Screening and Computational Methods Identifies Ligandable Pockets on the von Hippel–Lindau (VHL) E3 Ubiquitin Ligase

Author(s): Xavier Lucas, Inge Van Molle, Alessio Ciulli
Published in: Journal of Medicinal Chemistry, Issue 61/16, 2018, Page(s) 7387-7393, ISSN 0022-2623
DOI: 10.1021/acs.jmedchem.8b00842