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Scott J. Hughes
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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
2692018
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
2542017
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
2412019
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
1952017
Structure‐based design of a macrocyclic PROTAC
A Testa, SJ Hughes, X Lucas, JE Wright, A Ciulli
Angewandte Chemie 132 (4), 1744-1751, 2020
1712020
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
1192021
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
1172019
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
932020
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
472021
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
372023
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
332015
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
302016
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
222016
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
222014
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
192013
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
182020
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
172011
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
142021
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, ...
92017
Trivalent PROTACs enhance protein degradation through cooperativity and avidity
S Imaide, KM Riching, V Vetma, C Whitworth, SJ Hughes, N Trainor, ...
62020
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