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 | 315 | 2018 |
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 | 296 | 2019 |
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 | 284 | 2017 |
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 | 222 | 2017 |
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 | 209 | 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 | 171 | 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 | 146 | 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 | 117 | 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 | 80 | 2023 |
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 | 62 | 2021 |
Adenosine A1 receptor activation modulates human equilibrative nucleoside transporter 1 (hENT1) activity via PKC-mediated phosphorylation of serine-281 SJ Hughes, X Cravetchi, G Vilas, JR Hammond Cellular signalling 27 (5), 1008-1018, 2015 | 38 | 2015 |
Probing the ATP site of GRP78 with nucleotide triphosphate analogs SJ Hughes, T Antoshchenko, Y Chen, H Lu, JC Pizarro, HW Park PloS one 11 (5), e0154862, 2016 | 37 | 2016 |
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 | 27 | 2020 |
Discovery of Potent Pantothenamide Inhibitors of Staphylococcus aureus Pantothenate Kinase through a Minimal SAR Study: Inhibition Is Due to Trapping of the … SJ Hughes, L Barnard, K Mottaghi, W Tempel, T Antoshchenko, BS Hong, ... ACS Infectious Diseases 2 (9), 627-641, 2016 | 24 | 2016 |
Structural characterization of a new N‐substituted pantothenamide bound to pantothenate kinases from Klebsiella pneumoniae and Staphylococcus aureus SJ Hughes, T Antoshchenko, KP Kim, D Smil, HW Park Proteins: Structure, Function, and Bioinformatics 82 (7), 1542-1548, 2014 | 23 | 2014 |
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 | 20 | 2021 |
Chimeric rhinoviruses displaying MPER epitopes elicit anti-HIV neutralizing responses G Yi, M Lapelosa, R Bradley, TM Mariano, DE Dietz, S Hughes, T Wrin, ... PloS one 8 (9), e72205, 2013 | 19 | 2013 |
Identification of cysteines involved in the effects of methanethiosulfonate reagents on human equilibrative nucleoside transporter 1 JS Park, SJ Hughes, FKM Cunningham, JR Hammond Molecular pharmacology 80 (4), 735-746, 2011 | 17 | 2011 |
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, ... | 10 | 2017 |
Trivalent PROTACs enhance protein degradation through cooperativity and avidity S Imaide, KM Riching, V Vetma, C Whitworth, SJ Hughes, N Trainor, ... | 6 | 2020 |