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 | 932 | 2017 |
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 |
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 |
Structure‐Based Design of a Macrocyclic PROTAC A Testa, SJ Hughes, X Lucas, JE Wright, A Ciulli Angewandte Chemie 132 (4), 1744-1751, 2020 | 172 | 2020 |
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 | 126 | 2021 |
Cereblon versus VHL: Hijacking E3 ligases against each other using PROTACs M Girardini, C Maniaci, SJ Hughes, A Testa, A Ciulli Bioorganic & medicinal chemistry 27 (12), 2466-2479, 2019 | 122 | 2019 |
3-Fluoro-4-hydroxyprolines: Synthesis, Conformational Analysis, and Stereoselective Recognition by the VHL E3 Ubiquitin Ligase for Targeted Protein Degradation A Testa, X Lucas, GV Castro, KH Chan, JE Wright, AC Runcie, MS Gadd, ... Journal of the American Chemical Society 140 (29), 9299-9313, 2018 | 122 | 2018 |
Rapid and Reversible Knockdown of Endogenously Tagged Endosomal Proteins via an Optimized HaloPROTAC Degrader H Tovell, A Testa, C Maniaci, H Zhou, AR Prescott, T Macartney, A Ciulli, ... ACS chemical biology 14 (5), 882-892, 2019 | 102 | 2019 |
Understanding and improving the membrane permeability of VH032-based PROTACs VG Klein, CE Townsend, A Testa, M Zengerle, C Maniaci, SJ Hughes, ... ACS medicinal chemistry letters 11 (9), 1732-1738, 2020 | 96 | 2020 |
Design and characterization of SGK3-PROTAC1, an isoform specific SGK3 kinase PROTAC degrader H Tovell, A Testa, H Zhou, N Shpiro, C Crafter, A Ciulli, DR Alessi ACS chemical biology 14 (9), 2024-2034, 2019 | 87 | 2019 |
New molecular and therapeutic insights into canine diffuse large B cell lymphoma elucidates the role of the dog as a model for human disease L Aresu, S Ferraresso, L Marconato, L Cascione, S Napoli, E Gaudio, ... Blood, The Journal of the American Society of Hematology 132 (Supplement 1 …, 2018 | 61 | 2018 |
The rise and rise of protein degradation: Opportunities and challenges ahead SJ Hughes, A Testa, N Thompson, I Churcher Drug discovery today 26 (12), 2889-2897, 2021 | 52 | 2021 |
Development of BromoTag: A “Bump-and-Hole”–PROTAC System to Induce Potent, Rapid, and Selective Degradation of Tagged Target Proteins AG Bond, C Craigon, KH Chan, A Testa, A Karapetsas, R Fasimoye, ... Journal of Medicinal Chemistry 64 (20), 15477-15502, 2021 | 48 | 2021 |
Inducible degradation of target proteins through a tractable affinity-directed protein missile system LM Simpson, TJ Macartney, A Nardin, LJ Fulcher, S Röth, A Testa, ... Cell Chemical Biology 27 (9), 1164-1180. e5, 2020 | 45 | 2020 |
Functional E3 ligase hotspots and resistance mechanisms to small-molecule degraders A Hanzl, R Casement, H Imrichova, SJ Hughes, E Barone, A Testa, ... Nature chemical biology 19 (3), 323-333, 2023 | 42 | 2023 |
Optimization of a “bump-and-hole” approach to allele-selective BET bromodomain inhibition AC Runcie, M Zengerle, KH Chan, A Testa, L van Beurden, MGJ Baud, ... Chemical Science 9 (9), 2452-2468, 2018 | 40 | 2018 |
PET Tracers To Study Clinically Relevant Hepatic Transporters A Testa, M Zanda, CS Elmore, P Sharma Molecular pharmaceutics 12 (7), 2203-2216, 2015 | 35 | 2015 |
Mind the metal: a fragment library-derived zinc impurity binds the E2 ubiquitin-conjugating enzyme Ube2T and induces structural rearrangements FE Morreale, A Testa, VK Chaugule, A Bortoluzzi, A Ciulli, H Walden Journal of medicinal chemistry 60 (19), 8183-8191, 2017 | 24 | 2017 |
Diastereoselective Protocols for the Synthesis of 2, 3-trans-and 2, 3-cis-6-Methoxy-morpholine-2-carboxylic Acid Derivatives M Penso, F Foschi, S Pellegrino, A Testa, ML Gelmi The Journal of organic chemistry 77 (7), 3454-3461, 2012 | 24 | 2012 |