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Alessio Ciulli
Researcher at University of Dundee
Publications - 143
Citations - 7759
Alessio Ciulli is an academic researcher from University of Dundee. The author has contributed to research in topics: Ubiquitin ligase & Protein degradation. The author has an hindex of 41, co-authored 128 publications receiving 5401 citations. Previous affiliations of Alessio Ciulli include University of Florence & University of Cambridge.
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Journal ArticleDOI
Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4
TL;DR: Proteolysis Targeted Chimeras (PROTACs) that tether JQ1 to a ligand for the E3 ubiquitin ligase VHL, aimed at triggering the intracellular destruction of BET proteins open up new opportunities to elucidate the cellular phenotypes and therapeutic implications associated with selective targeting of BRD4.
Journal ArticleDOI
Structural basis of PROTAC cooperative recognition for selective protein degradation.
M.S. Gadd,Andrea Testa,Xavier Lucas,Kwok-Ho Chan,Wenzhang Chen,Douglas J. Lamont,Michael Zengerle,Alessio Ciulli +7 more
TL;DR: The results elucidate how PROTAC-induced de novo contacts dictate preferential recruitment of a target protein into a stable and cooperative complex with an E3 ligase for selective degradation.
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.
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BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design.
William Farnaby,Manfred Koegl,Michael J. Roy,Claire Whitworth,Emelyne Diers,Nicole Trainor,David Zollman,Steffen Steurer,Jale Karolyi-Oezguer,Carina Riedmueller,Teresa Gmaschitz,Johannes Wachter,Christian Dank,Michael Galant,Bernadette Sharps,Klaus Rumpel,Elisabeth Traxler,Thomas Gerstberger,Renate Schnitzer,Oliver Petermann,Peter Greb,Harald Weinstabl,Gerd Bader,Andreas Zoephel,Alexander Weiss-Puxbaum,Katharina Ehrenhöfer-Wölfer,Simon Wöhrle,Guido Boehmelt,Joerg Rinnenthal,Heribert Arnhof,Nicola Wiechens,Meng-Ying Wu,Tom Owen-Hughes,Peter Ettmayer,Mark Pearson,Darryl B. McConnell,Alessio Ciulli +36 more
TL;DR: Proteolysis targeting chimera (PROTAC) degraders of the BAF ATPase subunits SMARCA2 andSMARCA4 are developed using a bromodomain ligand and recruitment of the E3 ubiquitin ligase VHL to degrade high profile drug targets and induce cancer cell death.
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.