• 272 Citations
  • 6 h-Index
20172019
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Research Output 2017 2019

  • 272 Citations
  • 6 h-Index
  • 12 Article
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Article
2019
2 Citations (Scopus)

Cereblon versus VHL: Hijacking E3 ligases against each other using PROTACs

Girardini, M., Maniaci, C., Hughes, S., Testa, A. & Ciulli, A., 15 Jun 2019, In : Bioorganic & Medicinal Chemistry. 27, 12, p. 2466-2479 14 p.

Research output: Contribution to journalArticle

Open Access
Proteolysis
Ubiquitin-Protein Ligases
Degradation
Cullin Proteins
Ubiquitination
33 Downloads (Pure)

Design and Characterization of SGK3-PROTAC1, an Isoform Specific SGK3 Kinase PROTAC Degrader

Tovell, H., Testa, A., Zhou, H., Shpiro, N., Crafter, C., Ciulli, A. & Alessi, D., 20 Sep 2019, In : ACS Chemical Biology. 14, 9, p. 2024-2034 11 p.

Research output: Contribution to journalArticle

Open Access
File
Phosphatidylinositol 3-Kinases
Protein Isoforms
Phosphotransferases
Cells
Degradation
20 Citations (Scopus)
219 Downloads (Pure)

Iterative design and optimization of initially inactive Proteolysis Targeting Chimeras (PROTACs) identify VZ185 as a potent, fast and selective von Hippel-Lindau (VHL)-based dual degrader probe of BRD9 and BRD7

Zoppi, V., Hughes, S. J., Maniaci, C., Testa, A., Gmaschitz, T., Wieshofer, C., Koegl, M., Riching, K. M., Daniels, D. L., Spallarossa, A. & Ciulli, A., 24 Jan 2019, In : Journal of Medicinal Chemistry. 62, 2, p. 699-726 28 p.

Research output: Contribution to journalArticle

Open Access
File
Ubiquitination
Ligases
Proteolysis
Chromatin Assembly and Disassembly
Ubiquitin-Protein Ligases
1 Citation (Scopus)
104 Downloads (Pure)

Rapid and reversible knockdown of endogenously tagged endosomal proteins via an optimized HaloPROTAC degrader

Tovell, H., Testa, A., Maniaci, C., Zhou, H., Prescott, A., Macartney, T., Ciulli, A. & Alessi, D., 17 May 2019, In : ACS Chemical Biology. 14, 5, p. 882-892 11 p.

Research output: Contribution to journalArticle

Open Access
File
Degradation
Clustered Regularly Interspaced Short Palindromic Repeats
Proteins
Ubiquitination
Phosphorylation

Structure-Based Design of a Macrocyclic PROTAC

Testa, A., Hughes, S. J., Lucas, X., Wright, J. E. & Ciulli, A., 19 Nov 2019, In : Angewandte Chemie International Edition.

Research output: Contribution to journalArticle

Molecules
Enzyme Inhibitors
Conformations
Proteins
Crystal structure
2018
17 Citations (Scopus)
78 Downloads (Pure)

3-Fluoro-4-hydroxyprolines: Synthesis, conformational analysis and stereoselective recognition by the VHL E3 ubiquitin ligase for targeted protein degradation

Testa, A., Lucas, X., Castro, G., Chan, K. H., Wright, J., Runcie, A., Gadd, M., Harrison, W. T. A., Ko, E. J., Fletcher, D. & Ciulli, A., 25 Jul 2018, In : Journal of the American Chemical Society. 140, 29, p. 9299-9313 15 p.

Research output: Contribution to journalArticle

Open Access
File
Hydroxyproline
Ubiquitin-Protein Ligases
Proteolysis
Proteins
Degradation
44 Citations (Scopus)
102 Downloads (Pure)
Open Access
File
WEB 2086
Proteolysis
Ligands
Ubiquitin-Protein Ligases
Myeloid Cells
6 Citations (Scopus)
97 Downloads (Pure)

New molecular and therapeutic insights into canine diffuse large B cell lymphoma elucidates the role of the dog as a model for human disease

Aresu, L., Ferraresso, S., Marconato, L., Cascione, L., Napoli, S., Gaudio, E., Kwee, I., Tarantelli, C., Testa, A., Maniaci, C., Ciulli, A., Hillmann, P., Bohnacker, T., Wymann, M. P., Comazzi, S., Milan, M., Riondato, F., Dalla Rovere, G., Giantin, M., Giannuzzi, D. & 1 others, Bertoni, F., 13 Dec 2018, In : Haematologica. 104, 6, p. e256-e259 4 p.

Research output: Contribution to journalArticle

Open Access
File
5 Citations (Scopus)
119 Downloads (Pure)

Optimization of a “Bump-and-Hole” Approach to Allele-Selective BET Bromodomain Inhibition

Runcie, A., Zengerle, M., Chan, K. H., Testa, A., Van Beurden, L., Baud, M., Epemolu, R., Ellis, L., Read, K., Coulthard, V., Brien, A. & Ciulli, A., 7 Mar 2018, In : Chemical Science. 9, 9, p. 2452-2468 17 p., 2452.

Research output: Contribution to journalArticle

Open Access
File
Benzodiazepines
Leucine
Proteins
Cell proliferation
Valine
2017
42 Citations (Scopus)
125 Downloads (Pure)

Homo-PROTACs: bivalent small-molecule dimerizers of the VHL E3 ubiquitin ligase to induce self-degradation

Maniaci, C., Hughes, S. J., Testa, A., Chen, W., Lamont, D. J., Rocha, S., Alessi, D. R., Romeo, R. & Ciulli, A., 10 Oct 2017, In : Nature Communications. 8, p. 1-14 14 p., 830.

Research output: Contribution to journalArticle

Open Access
File
Proteolysis
Ubiquitin-Protein Ligases
Hominidae
degradation
Degradation
2 Citations (Scopus)
127 Downloads (Pure)

Mind the metal: a fragment library-derived zinc impurity binds the E2 ubiquitin-conjugating enzyme Ube2T and induces structural rearrangements

Morreale, F., Testa, A., Chaugule, V., Bortoluzzi, A., Ciulli, A. & Walden, H., 12 Oct 2017, In : Journal of Medicinal Chemistry. 60, 19, p. 8183-8191 9 p.

Research output: Contribution to journalArticle

Open Access
File
Ubiquitin-Conjugating Enzymes
Small Molecule Libraries
Zinc
Metals
Fanconi Anemia
133 Citations (Scopus)
294 Downloads (Pure)

Structural basis of PROTAC cooperative recognition for selective protein degradation

Gadd, M., Testa, A., Lucas, X., Chan, K. H., Chen, W., Lamont, D., Zengerle, M. & Ciulli, A., May 2017, In : Nature Chemical Biology. 13, 5, p. 514-521 11 p.

Research output: Contribution to journalArticle

Open Access
File
Proteolysis
Ubiquitin-Protein Ligases
Calorimetry
Ligases
Mutagenesis