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 |
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 |
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 |
Bifunctional chemical probes inducing protein–protein interactions C Maniaci, A Ciulli Current Opinion in Chemical Biology 52, 145-156, 2019 | 96 | 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 |
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 |
A facile synthesis of ligands for the von Hippel–Lindau E3 ligase C Steinebach, SA Voell, LP Vu, A Bricelj, I Sosič, G Schnakenburg, ... Synthesis 52 (17), 2521-2527, 2020 | 23 | 2020 |
Development of NanoLuc-targeting protein degraders and a universal reporter system to benchmark tag-targeted degradation platforms C Grohmann, CM Magtoto, JR Walker, NK Chua, A Gabrielyan, M Hall, ... Nature Communications 13 (1), 2073, 2022 | 15 | 2022 |
Translating PROTAC chemical series optimization into functional outcomes underlying BRD7 and BRD9 protein degradation KM Riching, JD Vasta, SJ Hughes, V Zoppi, C Maniaci, A Testa, M Urh, ... Current Research in Chemical Biology 1, 100009, 2021 | 15 | 2021 |
Targeted protein degradation via intramolecular bivalent glues O Hsia, M Hinterndorfer, AD Cowan, K Iso, T Ishida, R Sundaramoorthy, ... Nature, 1-8, 2024 | 13 | 2024 |
An intramolecular bivalent degrader glues an intrinsic BRD4-DCAF16 interaction O Hsia bioRxiv, 2023 | 9 | 2023 |
Homo-PROTACs: Bivalent small-molecule dimerizers of the VHL E3 ubiquitin ligase to induce self-degradation. Nat Commun 8: 830 C Maniaci, SJ Hughes, A Testa, W Chen, DJ Lamont, S Rocha, DR Alessi, ... | 9 | 2017 |
Trivalent PROTACs enhance protein degradation through cooperativity and avidity S Imaide, KM Riching, V Vetma, C Whitworth, SJ Hughes, N Trainor, ... | 6 | 2020 |
Small molecules A CIULLI, C MANIACI, SJ HUGHES, A TESTA | 5 | 2018 |
The bromodomain and extra-terminal domain degrader MZ1 exhibits preclinical anti-tumoral activity in diffuse large B-cell lymphoma of the activated B cell-like type C Tarantelli, E Cannas, H Ekeh, C Moscatello, E Gaudio, L Cascione, ... Exploration of Targeted Anti-tumor Therapy 2 (6), 586, 2021 | 4 | 2021 |
DEGRONOPEDIA: a web server for proteome-wide inspection of degrons NA Szulc, F Stefaniak, M Piechota, A Soszyńska, G Piórkowska, ... Nucleic Acids Research, gkae238, 2024 | 2 | 2024 |
Inducible Degradation of Target Proteins Through a Tractable Affinity-Directed PROtein Missile (AdPROM) System L Simpson, T Macartney, A Nardin, L Fulcher, A Testa, C Maniaci, A Ciulli, ... Available at SSRN 3552150, 2020 | 1 | 2020 |