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Inge Van Molle
Researcher at University of Cambridge
Publications - 17
Citations - 1271
Inge Van Molle is an academic researcher from University of Cambridge. The author has contributed to research in topics: Ubiquitin ligase & Ubiquitin. The author has an hindex of 10, co-authored 13 publications receiving 994 citations.
Papers
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Journal ArticleDOI
Targeting the von Hippel-Lindau E3 ubiquitin ligase using small molecules to disrupt the VHL/HIF-1α interaction.
Dennis L. Buckley,Inge Van Molle,Peter C. Gareiss,Hyun Seop Tae,Julien Michel,Devin J. Noblin,William L. Jorgensen,Alessio Ciulli,Craig M. Crews +8 more
TL;DR: This work has generated the first small molecule targeting the von Hippel–Lindau protein, the substrate recognition subunit of an E3 ligase, and an important target in cancer, chronic anemia, and ischemia, and obtained the crystal structure of VHL bound to the most potent inhibitor.
Journal ArticleDOI
Structure-Guided Design and Optimization of Small Molecules Targeting the Protein-Protein Interaction between the von Hippel-Lindau (VHL) E3 Ubiquitin Ligase and the Hypoxia Inducible Factor (HIF) Alpha Subunit with in Vitro Nanomolar Affinities.
Carles Galdeano,M.S. Gadd,P. Soares,Salvatore Scaffidi,Inge Van Molle,Ipek Birced,Sarah Hewitt,David M. Dias,Alessio Ciulli,Alessio Ciulli +9 more
TL;DR: The design and optimization, guided by X-ray crystal structures, of a ligand series with nanomolar binding affinities of the pVHL:HIF-1α interaction is reported.
Journal ArticleDOI
Small‐Molecule Inhibitors of the Interaction between the E3 Ligase VHL and HIF1α
Dennis L. Buckley,Jeffrey L. Gustafson,Inge Van Molle,Anke G. Roth,Hyun Seop Tae,Peter C. Gareiss,William L. Jorgensen,Alessio Ciulli,Craig M. Crews +8 more
TL;DR: Novel small-molecule inhibitors of the interaction between VHL and its molecular target HIF1α, a transcription factor involved in oxygen sensing are reported.
Journal ArticleDOI
Dissecting Fragment-Based Lead Discovery at the von Hippel-Lindau Protein:Hypoxia Inducible Factor 1α Protein-Protein Interface
Inge Van Molle,Andreas Thomann,Dennis L. Buckley,Ernest C. So,Steffen Lang,Craig M. Crews,Alessio Ciulli +6 more
TL;DR: A systematic deconstruction of lead-like inhibitors of the pVHL:HIF-1α interaction into their component fragments is conducted to assess the tractability of often challenging protein:protein interfaces.
Patent
Compounds&methods for the enhanced degradation of targeted proteins&other polypeptides by an e3 ubiquitin ligase
Craig M. Crews,Dennis Buckley,Alessio Ciulli,William L. Jorgensen,Peter C. Gareiss,Inge Van Molle,Jeffrey L. Gustafson,Hyun-Seop Tae,Julien Michel,Dentin Wade Hoyer,Anke G. Roth,John D. Harling,Ian Edward David Smith,Afjal Hussain Miah,Sebastien Andre Campos,Joelle Le +15 more
TL;DR: In this paper, a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of targeted polypeptides, are described.