iTAG an optimized IMiD-induced degron for targeted protein degradation in human and murine cells
Bouguenina, Habib, Nicolaou, Stephanos, Le Bihan, Yann-Vaï, Bowling, Elizabeth A., Calderon, Cheyenne, Caldwell, John J., Harrington, Brinley, Hayes, Angela, McAndrew, P. Craig, Mitsopoulos, Costas, Sialana, Fernando Jr, Scarpino, Andrea, Stubbs, Mark, Thapaliya, Arjun, Tyagi, Siddhartha, Wang, Hannah Z., Wood, Francesca, Burke, Rosemary, Raynaud, Florence, Choudhary, Jyoti, van Montfort, Rob L.M., Sadok, Amine, Westbrook, Thomas F., Collins, Ian, Chopra, Rajesh
Published in iScience (21.07.2023)
Published in iScience (21.07.2023)
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Identification of autophosphorylation inhibitors of the inositol-requiring enzyme 1 alpha (IRE1α) by high-throughput screening using a DELFIA assay
Newbatt, Yvette, Hardcastle, Anthea, McAndrew, P Craig, Strover, Jade A, Mirza, Amin, Morgan, Gareth J, Burke, Rosemary, Davies, Faith E, Collins, Ian, van Montfort, Rob L M
Published in Journal of biomolecular screening (01.03.2013)
Published in Journal of biomolecular screening (01.03.2013)
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Demonstrating In-Cell Target Engagement Using a Pirin Protein Degradation Probe (CCT367766)
Chessum, Nicola E. A, Sharp, Swee Y, Caldwell, John J, Pasqua, A. Elisa, Wilding, Birgit, Colombano, Giampiero, Collins, Ian, Ozer, Bugra, Richards, Meirion, Rowlands, Martin, Stubbs, Mark, Burke, Rosemary, McAndrew, P. Craig, Clarke, Paul A, Workman, Paul, Cheeseman, Matthew D, Jones, Keith
Published in Journal of medicinal chemistry (08.02.2018)
Published in Journal of medicinal chemistry (08.02.2018)
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Achieving In Vivo Target Depletion through the Discovery and Optimization of Benzimidazolone BCL6 Degraders
Bellenie, Benjamin R, Cheung, Kwai-Ming J, Varela, Ana, Pierrat, Olivier A, Collie, Gavin W, Box, Gary M, Bright, Michael D, Gowan, Sharon, Hayes, Angela, Rodrigues, Matthew J, Shetty, Kartika N, Carter, Michael, Davis, Owen A, Henley, Alan T, Innocenti, Paolo, Johnson, Louise D, Liu, Manjuan, de Klerk, Selby, Le Bihan, Yann-Vaï, Lloyd, Matthew G, McAndrew, P. Craig, Shehu, Erald, Talbot, Rachel, Woodward, Hannah L, Burke, Rosemary, Kirkin, Vladimir, van Montfort, Rob L. M, Raynaud, Florence I, Rossanese, Olivia W, Hoelder, Swen
Published in Journal of medicinal chemistry (23.04.2020)
Published in Journal of medicinal chemistry (23.04.2020)
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Determination of Ligand-Binding Affinity (K d) Using Transverse Relaxation Rate (R 2) in the Ligand-Observed 1H NMR Experiment and Applications to Fragment-Based Drug Discovery
Liu, Manjuan, Mirza, Amin, McAndrew, P. Craig, Thapaliya, Arjun, Pierrat, Olivier A., Stubbs, Mark, Hahner, Tamas, Chessum, Nicola E. A., Innocenti, Paolo, Caldwell, John, Cheeseman, Matthew D., Bellenie, Benjamin R., van Montfort, Rob L. M., Newton, Gary K., Burke, Rosemary, Collins, Ian, Hoelder, Swen
Published in Journal of medicinal chemistry (10.08.2023)
Published in Journal of medicinal chemistry (10.08.2023)
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Discovery of 2‑(3-Benzamidopropanamido)thiazole-5-carboxylate Inhibitors of the Kinesin HSET (KIFC1) and the Development of Cellular Target Engagement Probes
Saint-Dizier, François, Matthews, Thomas P., Gregson, Aaron M., Prevet, Hugues, McHardy, Tatiana, Colombano, Giampiero, Saville, Harry, Rowlands, Martin, Ewens, Caroline, McAndrew, P. Craig, Tomlin, Kathy, Guillotin, Delphine, Mak, Grace Wing-Yan, Drosopoulos, Konstantinos, Poursaitidis, Ioannis, Burke, Rosemary, van Montfort, Rob, Linardopoulos, Spiros, Collins, Ian
Published in Journal of medicinal chemistry (23.02.2023)
Published in Journal of medicinal chemistry (23.02.2023)
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Journal Article
Determination of Ligand-Binding Affinity ( K d ) Using Transverse Relaxation Rate ( R 2 ) in the Ligand-Observed 1 H NMR Experiment and Applications to Fragment-Based Drug Discovery
Liu, Manjuan, Mirza, Amin, McAndrew, P Craig, Thapaliya, Arjun, Pierrat, Olivier A, Stubbs, Mark, Hahner, Tamas, Chessum, Nicola E A, Innocenti, Paolo, Caldwell, John, Cheeseman, Matthew D, Bellenie, Benjamin R, van Montfort, Rob L M, Newton, Gary K, Burke, Rosemary, Collins, Ian, Hoelder, Swen
Published in Journal of medicinal chemistry (10.08.2023)
Published in Journal of medicinal chemistry (10.08.2023)
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A Degron Blocking Strategy Towards Improved CRL4CRBN Recruiting PROTAC Selectivity
Habib Bouguenina, Scarpino, Andrea, O'Hanlon, Jack A, Warne, Justin, Wang, Hannah Z, Laura Chan Wah Hak, Sadok, Amine, McAndrew, P Craig, Stubbs, Mark, Pierrat, Olivier A, Hahner, Tamas, Cabry, Marc P, Yann‐Vaï Le Bihan, Mitsopoulos, Costas, Sialana, Fernando J, Roumeliotis, Theodoros I, Burke, Rosemary, Rob L M van Montfort, Choudhari, Jyoti, Chopra, Rajesh, Caldwell, John J, Collins, Ian
Published in Chembiochem : a European journal of chemical biology (01.12.2023)
Published in Chembiochem : a European journal of chemical biology (01.12.2023)
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Optimizing Shape Complementarity Enables the Discovery of Potent Tricyclic BCL6 Inhibitors
Davis, Owen A., Cheung, Kwai-Ming J., Brennan, Alfie, Lloyd, Matthew G., Rodrigues, Matthew J., Pierrat, Olivier A., Collie, Gavin W., Le Bihan, Yann-Vaï, Huckvale, Rosemary, Harnden, Alice C., Varela, Ana, Bright, Michael D., Eve, Paul, Hayes, Angela, Henley, Alan T., Carter, Michael D., McAndrew, P. Craig, Talbot, Rachel, Burke, Rosemary, van Montfort, Rob L. M., Raynaud, Florence I., Rossanese, Olivia W., Meniconi, Mirco, Bellenie, Benjamin R., Hoelder, Swen
Published in Journal of medicinal chemistry (23.06.2022)
Published in Journal of medicinal chemistry (23.06.2022)
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A Degron Blocking Strategy Towards Improved CRL4 CRBN Recruiting PROTAC Selectivity
Bouguenina, Habib, Scarpino, Andrea, O'Hanlon, Jack A, Warne, Justin, Wang, Hannah Z, Wah Hak, Laura Chan, Sadok, Amine, McAndrew, P Craig, Stubbs, Mark, Pierrat, Olivier A, Hahner, Tamas, Cabry, Marc P, Le Bihan, Yann-Vaï, Mitsopoulos, Costas, Sialana, Fernando J, Roumeliotis, Theodoros I, Burke, Rosemary, van Montfort, Rob L M, Choudhari, Jyoti, Chopra, Rajesh, Caldwell, John J, Collins, Ian
Published in Chembiochem : a European journal of chemical biology (01.12.2023)
Published in Chembiochem : a European journal of chemical biology (01.12.2023)
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Into Deep Water: Optimizing BCL6 Inhibitors by Growing into a Solvated Pocket
Lloyd, Matthew G, Huckvale, Rosemary, Cheung, Kwai-Ming J, Rodrigues, Matthew J, Collie, Gavin W, Pierrat, Olivier A, Gatti Iou, Mahad, Carter, Michael, Davis, Owen A, McAndrew, P. Craig, Gunnell, Emma, Le Bihan, Yann-Vaï, Talbot, Rachel, Henley, Alan T, Johnson, Louise D, Hayes, Angela, Bright, Michael D, Raynaud, Florence I, Meniconi, Mirco, Burke, Rosemary, van Montfort, Rob L. M, Rossanese, Olivia W, Bellenie, Benjamin R, Hoelder, Swen
Published in Journal of medicinal chemistry (09.12.2021)
Published in Journal of medicinal chemistry (09.12.2021)
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Molecular mechanisms of human IRE1 activation through dimerization and ligand binding
Joshi, Amar, Newbatt, Yvette, McAndrew, P Craig, Stubbs, Mark, Burke, Rosemary, Richards, Mark W, Bhatia, Chitra, Caldwell, John J, McHardy, Tatiana, Collins, Ian, Bayliss, Richard
Published in Oncotarget (30.05.2015)
Published in Oncotarget (30.05.2015)
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Discovering cell-active BCL6 inhibitors: effectively combining biochemical HTS with multiple biophysical techniques, X-ray crystallography and cell-based assays
Pierrat, Olivier A., Liu, Manjuan, Collie, Gavin W., Shetty, Kartika, Rodrigues, Matthew J., Le Bihan, Yann-Vaï, Gunnell, Emma A., McAndrew, P. Craig, Stubbs, Mark, Rowlands, Martin G., Yahya, Norhakim, Shehu, Erald, Talbot, Rachel, Pickard, Lisa, Bellenie, Benjamin R., Cheung, Kwai-Ming J., Drouin, Ludovic, Innocenti, Paolo, Woodward, Hannah, Davis, Owen A., Lloyd, Matthew G., Varela, Ana, Huckvale, Rosemary, Broccatelli, Fabio, Carter, Michael, Galiwango, David, Hayes, Angela, Raynaud, Florence I., Bryant, Christopher, Whittaker, Steven, Rossanese, Olivia W., Hoelder, Swen, Burke, Rosemary, van Montfort, Rob L. M.
Published in Scientific reports (03.11.2022)
Published in Scientific reports (03.11.2022)
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The discovery of potent ribosomal S6 kinase inhibitors by high-throughput screening and structure-guided drug design
Couty, Sylvain, Westwood, Isaac M, Kalusa, Andrew, Cano, Celine, Travers, Jon, Boxall, Kathy, Chow, Chiau Ling, Burns, Sam, Schmitt, Jessica, Pickard, Lisa, Barillari, Caterina, McAndrew, P Craig, Clarke, Paul A, Linardopoulos, Spiros, Griffin, Roger J, Aherne, G Wynne, Raynaud, Florence I, Workman, Paul, Jones, Keith, van Montfort, Rob L M
Published in Oncotarget (01.10.2013)
Published in Oncotarget (01.10.2013)
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Journal Article
Front Cover: A Degron Blocking Strategy Towards Improved CRL4CRBN Recruiting PROTAC Selectivity
Habib Bouguenina, Scarpino, Andrea, O'Hanlon, Jack A, Warne, Justin, Wang, Hannah Z, Laura Chan Wah Hak, Sadok, Amine, McAndrew, P Craig, Stubbs, Mark, Pierrat, Olivier A, Hahner, Tamas, Cabry, Marc P, Yann‐Vaï Le Bihan, Mitsopoulos, Costas, Sialana, Fernando J, Roumeliotis, Theodoros I, Burke, Rosemary, Rob L M van Montfort, Choudhari, Jyoti, Chopra, Rajesh, Caldwell, John J, Collins, Ian
Published in Chembiochem : a European journal of chemical biology (01.12.2023)
Published in Chembiochem : a European journal of chemical biology (01.12.2023)
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Journal Article
Front Cover: A Degron Blocking Strategy Towards Improved CRL4 CRBN Recruiting PROTAC Selectivity (ChemBioChem 23/2023)
Bouguenina, Habib, Scarpino, Andrea, O'Hanlon, Jack A., Warne, Justin, Wang, Hannah Z., Wah Hak, Laura Chan, Sadok, Amine, McAndrew, P. Craig, Stubbs, Mark, Pierrat, Olivier A., Hahner, Tamas, Cabry, Marc P., Le Bihan, Yann‐Vaï, Mitsopoulos, Costas, Sialana, Fernando J., Roumeliotis, Theodoros I., Burke, Rosemary, van Montfort, Rob L. M., Choudhari, Jyoti, Chopra, Rajesh, Caldwell, John J., Collins, Ian
Published in Chembiochem : a European journal of chemical biology (01.12.2023)
Published in Chembiochem : a European journal of chemical biology (01.12.2023)
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Journal Article
Erratum: iTAG an optimized IMiD-induced degron for targeted protein degradation in human and murine cells
Bouguenina, Habib, Nicolaou, Stephanos, Bihan, Yann-Vaï Le, Bowling, Elizabeth A, Calderon, Cheyenne, Caldwell, John J, Harrington, Brinley, Hayes, Angela, McAndrew, P Craig, Mitsopoulos, Costas, Sialana, Fernando Jr, Scarpino, Andrea, Stubbs, Mark, Thapaliya, Arjun, Tyagi, Siddhartha, Wang, Hannah Z, Wood, Francesca, Burke, Rosemary, Raynaud, Florence, Choudhary, Jyoti, van Montfort, Rob L M, Sadok, Amine, Westbrook, Thomas F, Collins, Ian, Chopra, Rajesh
Published in iScience (17.05.2024)
Published in iScience (17.05.2024)
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Journal Article
iTAG an optimized IMiD-induced degron for targeted protein degradation in human and murine cells
Bouguenina, Habib, Nicolaou, Stephanos, Bihan, Yann-Vaï Le, Bowling, Elizabeth A., Calderon, Cheyenne, Caldwell, John J., Harrington, Brinley, Hayes, Angela, McAndrew, P. Craig, Mitsopoulos, Costas, Sialana, Fernando Jr, Scarpino, Andrea, Stubbs, Mark, Thapaliya, Arjun, Tyagi, Siddhartha, Wang, Hannah Z., Wood, Francesca, Burke, Rosemary, Raynaud, Florence, Choudhary, Jyoti, van Montfort, Rob L.M., Sadok, Amine, Westbrook, Thomas F., Collins, Ian, Chopra, Rajesh
Published in iScience (17.05.2024)
Published in iScience (17.05.2024)
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