Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds
Chan, Kwok-Ho, Zengerle, Michael, Testa, Andrea, Ciulli, Alessio
Published in Journal of medicinal chemistry (25.01.2018)
Published in Journal of medicinal chemistry (25.01.2018)
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Journal Article
Structure‐Based Design of a Macrocyclic PROTAC
Testa, Andrea, Hughes, Scott J., Lucas, Xavier, Wright, Jane E., Ciulli, Alessio
Published in Angewandte Chemie International Edition (20.01.2020)
Published in Angewandte Chemie International Edition (20.01.2020)
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Journal Article
Structural basis of PROTAC cooperative recognition for selective protein degradation
Gadd, Morgan S, Testa, Andrea, Lucas, Xavier, Chan, Kwok-Ho, Chen, Wenzhang, Lamont, Douglas J, Zengerle, Michael, Ciulli, Alessio
Published in Nature chemical biology (01.05.2017)
Published in Nature chemical biology (01.05.2017)
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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 Dual Degrader Probe of BRD9 and BRD7
Zoppi, Vittoria, Hughes, Scott J, Maniaci, Chiara, Testa, Andrea, Gmaschitz, Teresa, Wieshofer, Corinna, Koegl, Manfred, Riching, Kristin M, Daniels, Danette L, Spallarossa, Andrea, Ciulli, Alessio
Published in Journal of medicinal chemistry (24.01.2019)
Published in Journal of medicinal chemistry (24.01.2019)
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Journal Article
Trivalent PROTACs enhance protein degradation via combined avidity and cooperativity
Imaide, Satomi, Riching, Kristin M., Makukhin, Nikolai, Vetma, Vesna, Whitworth, Claire, Hughes, Scott J., Trainor, Nicole, Mahan, Sarah D., Murphy, Nancy, Cowan, Angus D., Chan, Kwok-Ho, Craigon, Conner, Testa, Andrea, Maniaci, Chiara, Urh, Marjeta, Daniels, Danette L., Ciulli, Alessio
Published in Nature chemical biology (01.11.2021)
Published in Nature chemical biology (01.11.2021)
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Journal Article
Homo-PROTACs: bivalent small-molecule dimerizers of the VHL E3 ubiquitin ligase to induce self-degradation
Maniaci, Chiara, Hughes, Scott J., Testa, Andrea, Chen, Wenzhang, Lamont, Douglas J., Rocha, Sonia, Alessi, Dario R., Romeo, Roberto, Ciulli, Alessio
Published in Nature communications (10.10.2017)
Published in Nature communications (10.10.2017)
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Journal Article
SPR-Measured Dissociation Kinetics of PROTAC Ternary Complexes Influence Target Degradation Rate
Roy, Michael J, Winkler, Sandra, Hughes, Scott J, Whitworth, Claire, Galant, Michael, Farnaby, William, Rumpel, Klaus, Ciulli, Alessio
Published in ACS chemical biology (15.03.2019)
Published in ACS chemical biology (15.03.2019)
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Journal Article
Structural insights into substrate recognition by the SOCS2 E3 ubiquitin ligase
Kung, Wei-Wei, Ramachandran, Sarath, Makukhin, Nikolai, Bruno, Elvira, Ciulli, Alessio
Published in Nature communications (10.06.2019)
Published in Nature communications (10.06.2019)
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Journal Article
BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design
Farnaby, William, Koegl, Manfred, Roy, Michael J., Whitworth, Claire, Diers, Emelyne, Trainor, Nicole, Zollman, David, Steurer, Steffen, Karolyi-Oezguer, Jale, Riedmueller, Carina, Gmaschitz, Teresa, Wachter, Johannes, Dank, Christian, Galant, Michael, Sharps, Bernadette, Rumpel, Klaus, Traxler, Elisabeth, Gerstberger, Thomas, Schnitzer, Renate, Petermann, Oliver, Greb, Peter, Weinstabl, Harald, Bader, Gerd, Zoephel, Andreas, Weiss-Puxbaum, Alexander, Ehrenhöfer-Wölfer, Katharina, Wöhrle, Simon, Boehmelt, Guido, Rinnenthal, Joerg, Arnhof, Heribert, Wiechens, Nicola, Wu, Meng-Ying, Owen-Hughes, Tom, Ettmayer, Peter, Pearson, Mark, McConnell, Darryl B., Ciulli, Alessio
Published in Nature chemical biology (01.07.2019)
Published in Nature chemical biology (01.07.2019)
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Journal Article
A selective and orally bioavailable VHL-recruiting PROTAC achieves SMARCA2 degradation in vivo
Kofink, Christiane, Trainor, Nicole, Mair, Barbara, Wöhrle, Simon, Wurm, Melanie, Mischerikow, Nikolai, Roy, Michael J., Bader, Gerd, Greb, Peter, Garavel, Géraldine, Diers, Emelyne, McLennan, Ross, Whitworth, Claire, Vetma, Vesna, Rumpel, Klaus, Scharnweber, Maximilian, Fuchs, Julian E., Gerstberger, Thomas, Cui, Yunhai, Gremel, Gabriela, Chetta, Paolo, Hopf, Stefan, Budano, Nicole, Rinnenthal, Joerg, Gmaschitz, Gerhard, Mayer, Moriz, Koegl, Manfred, Ciulli, Alessio, Weinstabl, Harald, Farnaby, William
Published in Nature communications (10.10.2022)
Published in Nature communications (10.10.2022)
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Journal Article
Potent and selective chemical probe of hypoxic signalling downstream of HIF-α hydroxylation via VHL inhibition
Frost, Julianty, Galdeano, Carles, Soares, Pedro, Gadd, Morgan S., Grzes, Katarzyna M., Ellis, Lucy, Epemolu, Ola, Shimamura, Satoko, Bantscheff, Marcus, Grandi, Paola, Read, Kevin D., Cantrell, Doreen A., Rocha, Sonia, Ciulli, Alessio
Published in Nature communications (04.11.2016)
Published in Nature communications (04.11.2016)
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