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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
9392015
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
9312017
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
5142012
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
4172019
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
3942014
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
3172012
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
2742018
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
2602017
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
2492019
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
2122015
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
2102018
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
2062012
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
2042021
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
2002016
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
1992017
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
1842009
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
1792016
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
1762006
Structure‐based design of a macrocyclic PROTAC
A Testa, SJ Hughes, X Lucas, JE Wright, A Ciulli
Angewandte Chemie 132 (4), 1744-1751, 2020
1732020
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
1642011
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