Alessio Ciulli
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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
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
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
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
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
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 Edition 51 (46), 11463-11467, 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
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), 1-14, 2017
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
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
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
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
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), 1-12, 2016
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
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
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
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
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
A bump-and-hole approach to engineer controlled selectivity of BET bromodomain chemical probes
MGJ Baud, E Lin-Shiao, T Cardote, C Tallant, A Pschibul, KH Chan, ...
Science 346 (6209), 638-641, 2014
Fragment-based approaches to enzyme inhibition
A Ciulli, C Abell
Current opinion in biotechnology 18 (6), 489-496, 2007
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