ArticleJournal of medicinal chemistry2018
Surface Probing by Fragment-Based Screening and Computational Methods Identifies Ligandable Pockets on the von Hippel-Lindau (VHL) E3 Ubiquitin Ligase.
Article in Journal of medicinal chemistry, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
What it found
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
20 citing papers in PubMed.
- Harnessing the ubiquitin-proteasome system: advances and challenges of PROTACs in breast cancer.Molecular biology reports · 2026Review
- Rescuing the Function of Missense-Mutated Tumor SuppressorbioRxiv : the preprint server for biology · 2026Article
- Methods to Study the Molecular Mechanism and Drive the Design of Protein Degraders.Chemical reviews · 2026Review
- Discovering Uncharted Binding Pockets on E3 Ligases Leads to the Identification of FBW7 Allosteric Modulators.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2025Article
- NMR-Based Fragment Screen of the von Hippel-Lindau Elongin C&B Complex.ACS medicinal chemistry letters · 2025Article
- Identification of novel 7-hydroxycoumarin derivatives as ELOC binders with potential to modulate CRL2 complex formation.Scientific reports · 2025Article
- The Applications of Computational Tools in PROTAC Development.Current topics in medicinal chemistry · 2025Review
- Chemical rewiring of ubiquitination by degraders and their selectivity routes.Nature structural & molecular biology · 2024Article
- Targeted Protein Degradation: Advances, Challenges, and Prospects for Computational Methods.Journal of chemical information and modeling · 2023Review
- E3 Ligases Meet Their Match: Fragment-Based Approaches to Discover New E3 Ligands and to Unravel E3 Biology.Journal of medicinal chemistry · 2023Review
- Discovery of small molecule ligands for the von Hippel-Lindau (VHL) E3 ligase and their use as inhibitors and PROTAC degraders.Chemical Society reviews · 2022Review
- Targeting the ubiquitin system by fragment-based drug discovery.Frontiers in molecular biosciences · 2022Review
- Trivalent PROTACs enhance protein degradation via combined avidity and cooperativity.Nature chemical biology · 2021Article
- A small molecule HIF-1α stabilizer that accelerates diabetic wound healing.Nature communications · 2021Article
- E3 Ligase Ligands for PROTACs: How They Were Found and How to Discover New Ones.SLAS discovery : advancing life sciences R & D · 2021Review
- A suite of mathematical solutions to describe ternary complex formation and their application to targeted protein degradation by heterobifunctional ligands.The Journal of biological chemistry · 2020Article
- Structure-Based Discovery of SD-36 as a Potent, Selective, and Efficacious PROTAC Degrader of STAT3 Protein.Journal of medicinal chemistry · 2019Article
- PROTACs- a game-changing technology.Expert opinion on drug discovery · 2019Review
- Small molecule PROTACs: an emerging technology for targeted therapy in drug discovery.RSC advances · 2019Review
- Spy vs. spy: selecting the best reporter forChemical communications (Cambridge, England) · 2019Article
Corrections and comments
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Authors and funding
3 authors.
Funding
Abstract
Beyond the targeting of E3 ubiquitin ligases to inhibit protein homeostasis, E3 ligase binders can be repurposed as targeted protein degraders (PROTACs or molecular glues). We sought to identify new binders of the VHL E3 ligase by biophysical fragment-based screening followed by X-ray crystallographic soaking. We identified fragments binding at the ElonginC:Cullin2 interface and a new cryptic pocket in VHL, along with other potential ligandable sites predicted computationally and found to bind solvent molecules in crystal structures. The elucidated interactions provide starting points for future ligand development.
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Registered trials
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