Следене
Alessio Ciulli
Заглавие
Позовавания
Позовавания
Година
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
11062017
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
10522015
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
5952012
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
4962019
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
4432014
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
3532012
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
3152018
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
2962019
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
2842017
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
2692021
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
2402015
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
2302018
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
2292012
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
2282016
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
2222017
Structure‐based design of a macrocyclic PROTAC
A Testa, SJ Hughes, X Lucas, JE Wright, A Ciulli
Angewandte Chemie International Edition 59 (4), 1727-1734, 2020
2092020
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
1932016
Application of Fragment Growing and Fragment Linking to the Discovery of Inhibitors of Mycobacterium tuberculosis Pantothenate Synthetase This research was supported by the …
AW Hung, HL Silvestre, S Wen, A Ciulli, TL Blundell, C Abell
Angewandte Chemie-German Edition 121 (45), 8604, 2009
1872009
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
1772006
Trivalent PROTACs enhance protein degradation via combined avidity and cooperativity
S Imaide, KM Riching, N Makukhin, V Vetma, C Whitworth, SJ Hughes, ...
Nature chemical biology 17 (11), 1157–1167, 2021
1762021
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