Selective small molecule induced degradation of the BET bromodomain protein BRD4 M Zengerle, KH Chan, A Ciulli ACS chemical biology 10 (8), 1770-1777, 2015 | 939 | 2015 |
Structural basis of PROTAC cooperative recognition for selective protein degradation MS Gadd, A Testa, X Lucas, KH Chan, W Chen, DJ Lamont, M Zengerle, ... Nature chemical biology 13 (5), 514-521, 2017 | 931 | 2017 |
Targeting the von Hippel–Lindau E3 ubiquitin ligase using small molecules to disrupt the VHL/HIF-1α interaction DL Buckley, I Van Molle, PC Gareiss, HS Tae, J Michel, DJ Noblin, ... Journal of the American Chemical Society 134 (10), 4465-4468, 2012 | 514 | 2012 |
BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design W Farnaby, M Koegl, MJ Roy, C Whitworth, E Diers, N Trainor, D Zollman, ... Nature chemical biology 15 (7), 672-680, 2019 | 417 | 2019 |
Structure-guided design and optimization of small molecules targeting the protein–protein interaction between the von Hippel–Lindau (VHL) E3 ubiquitin ligase and the hypoxia … C Galdeano, MS Gadd, P Soares, S Scaffidi, I Van Molle, I Birced, ... Journal of Medicinal Chemistry 57 (20), 8657-8663, 2014 | 394 | 2014 |
Small Molecule Inhibitors of the Interaction Between the E3 Ligase VHL and HIF1α DL Buckley, JL Gustafson, I Van Molle, AG Roth, HS Tae, PC Gareiss, ... Angewandte Chemie (International Ed. in English) 51 (46), 11463, 2012 | 317 | 2012 |
Iterative design and optimization of initially inactive proteolysis targeting chimeras (PROTACs) identify VZ185 as a potent, fast, and selective von Hippel–Lindau (VHL) based … V Zoppi, SJ Hughes, C Maniaci, A Testa, T Gmaschitz, C Wieshofer, ... Journal of medicinal chemistry 62 (2), 699-726, 2018 | 274 | 2018 |
Homo-PROTACs: bivalent small-molecule dimerizers of the VHL E3 ubiquitin ligase to induce self-degradation C Maniaci, SJ Hughes, A Testa, W Chen, DJ Lamont, S Rocha, DR Alessi, ... Nature communications 8 (1), 830, 2017 | 260 | 2017 |
SPR-measured dissociation kinetics of PROTAC ternary complexes influence target degradation rate MJ Roy, S Winkler, SJ Hughes, C Whitworth, M Galant, W Farnaby, ... ACS chemical biology 14 (3), 361-368, 2019 | 249 | 2019 |
Targeting Cullin-RING E3 ubiquitin ligases for drug discovery: structure, assembly and small-molecule modulation E Bulatov, A Ciulli Biochemical Journal 467 (3), 365-386, 2015 | 212 | 2015 |
Impact of target warhead and linkage vector on inducing protein degradation: comparison of bromodomain and extra-terminal (BET) degraders derived from triazolodiazepine (JQ1 … KH Chan, M Zengerle, A Testa, A Ciulli Journal of medicinal chemistry 61 (2), 504-513, 2018 | 210 | 2018 |
Dissecting fragment-based lead discovery at the von Hippel-Lindau protein: hypoxia inducible factor 1α protein-protein interface I Van Molle, A Thomann, DL Buckley, EC So, S Lang, CM Crews, A Ciulli Chemistry & biology 19 (10), 1300-1312, 2012 | 206 | 2012 |
E3 ligase ligands for PROTACs: how they were found and how to discover new ones T Ishida, A Ciulli SLAS DISCOVERY: Advancing the Science of Drug Discovery 26 (4), 484-502, 2021 | 204 | 2021 |
Potent and selective chemical probe of hypoxic signalling downstream of HIF-α hydroxylation via VHL inhibition J Frost, C Galdeano, P Soares, MS Gadd, KM Grzes, L Ellis, O Epemolu, ... Nature communications 7 (1), 13312, 2016 | 200 | 2016 |
Molecular recognition of ternary complexes: a new dimension in the structure-guided design of chemical degraders SJ Hughes, A Ciulli Essays in biochemistry 61 (5), 505-516, 2017 | 199 | 2017 |
Application of fragment growing and fragment linking to the discovery of inhibitors of Mycobacterium tuberculosis pantothenate synthetase AW Hung, HL Silvestre, S Wen, A Ciulli, TL Blundell, C Abell Angewandte Chemie International Edition 48 (45), 8452-8456, 2009 | 184 | 2009 |
Cyclic and macrocyclic peptides as chemical tools to recognise protein surfaces and probe protein–protein interactions TAF Cardote, A Ciulli ChemMedChem 11 (8), 787-794, 2016 | 179 | 2016 |
Probing hot spots at protein− ligand binding sites: A fragment-based approach using biophysical methods A Ciulli, G Williams, AG Smith, TL Blundell, C Abell Journal of medicinal chemistry 49 (16), 4992-5000, 2006 | 176 | 2006 |
Structure‐based design of a macrocyclic PROTAC A Testa, SJ Hughes, X Lucas, JE Wright, A Ciulli Angewandte Chemie 132 (4), 1744-1751, 2020 | 173 | 2020 |
Bromodomain-peptide displacement assays for interactome mapping and inhibitor discovery M Philpott, J Yang, T Tumber, O Fedorov, S Uttarkar, P Filippakopoulos, ... Molecular BioSystems 7 (10), 2899-2908, 2011 | 164 | 2011 |