Discovery of Mcl-1-specific inhibitor AZD5991 and preclinical activity in multiple myeloma and acute myeloid leukemia
Tron, Adriana E, Belmonte, Matthew A, Adam, Ammar, Aquila, Brian M, Boise, Lawrence H, Chiarparin, Elisabetta, Cidado, Justin, Embrey, Kevin J, Gangl, Eric, Gibbons, Francis D, Gregory, Gareth P, Hargreaves, David, Hendricks, J Adam, Johannes, Jeffrey W, Johnstone, Ricky W, Kazmirski, Steven L, Kettle, Jason G, Lamb, Michelle L, Matulis, Shannon M, Nooka, Ajay K, Packer, Martin J, Peng, Bo, Rawlins, Philip B, Robbins, Daniel W, Schuller, Alwin G, Su, Nancy, Yang, Wenzhan, Ye, Qing, Zheng, Xiaolan, Secrist, J Paul, Clark, Edwin A, Wilson, David M, Fawell, Stephen E, Hird, Alexander W
Published in Nature communications (17.12.2018)
Published in Nature communications (17.12.2018)
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Journal Article
Differential uptake, kinetics and mechanisms of intracellular trafficking of next-generation antisense oligonucleotides across human cancer cell lines
Linnane, Emily, Davey, Paul, Zhang, Pei, Puri, Sanyogitta, Edbrooke, Mark, Chiarparin, Elisabetta, Revenko, Alexey S, Macleod, A Robert, Norman, Jim C, Ross, Sarah J
Published in Nucleic acids research (21.05.2019)
Published in Nucleic acids research (21.05.2019)
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Journal Article
Reducing the Lipophilicity of Perfluoroalkyl Groups by CF2–F/CF2–Me or CF3/CH3 Exchange
Jeffries, Benjamin, Wang, Zhong, Graton, Jérôme, Holland, Simon D, Brind, Thomasin, Greenwood, Ryan D. R, Le Questel, Jean-Yves, Scott, James S, Chiarparin, Elisabetta, Linclau, Bruno
Published in Journal of medicinal chemistry (13.12.2018)
Published in Journal of medicinal chemistry (13.12.2018)
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Journal Article
A protein tertiary structure mimetic modulator of the Hippo signalling pathway
Adihou, Hélène, Gopalakrishnan, Ranganath, Förster, Tim, Guéret, Stéphanie M., Gasper, Raphael, Geschwindner, Stefan, Carrillo García, Carmen, Karatas, Hacer, Pobbati, Ajaybabu V., Vazquez‐Chantada, Mercedes, Davey, Paul, Wassvik, Carola M., Pang, Jeremy Kah Sheng, Soh, Boon Seng, Hong, Wanjin, Chiarparin, Elisabetta, Schade, Dennis, Plowright, Alleyn T., Valeur, Eric, Lemurell, Malin, Grossmann, Tom N., Waldmann, Herbert
Published in Nature communications (27.10.2020)
Published in Nature communications (27.10.2020)
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Journal Article
Observing an Antisense Drug Complex in Intact Human Cells by in‐Cell NMR Spectroscopy
Schlagnitweit, Judith, Friebe Sandoz, Sarah, Jaworski, Aleksander, Guzzetti, Ileana, Aussenac, Fabien, Carbajo, Rodrigo J., Chiarparin, Elisabetta, Pell, Andrew J., Petzold, Katja
Published in Chembiochem : a European journal of chemical biology (01.10.2019)
Published in Chembiochem : a European journal of chemical biology (01.10.2019)
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Journal Article
Free Ligand 1D NMR Conformational Signatures To Enhance Structure Based Drug Design of a Mcl‑1 Inhibitor (AZD5991) and Other Synthetic Macrocycles
Balazs, Amber Y. S, Carbajo, Rodrigo J, Davies, Nichola L, Dong, Yu, Hird, Alexander W, Johannes, Jeffrey W, Lamb, Michelle L, McCoull, William, Raubo, Piotr, Robb, Graeme R, Packer, Martin J, Chiarparin, Elisabetta
Published in Journal of medicinal chemistry (14.11.2019)
Published in Journal of medicinal chemistry (14.11.2019)
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Journal Article
Experimental free ligand conformations: a missing link in structure-based drug discovery
Chiarparin, Elisabetta, Packer, Martin J, Wilson, David M
Published in Future medicinal chemistry (01.01.2019)
Published in Future medicinal chemistry (01.01.2019)
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Journal Article
Structure of the Epigenetic Oncogene MMSET and Inhibition by N‑Alkyl Sinefungin Derivatives
Tisi, Dominic, Chiarparin, Elisabetta, Tamanini, Emiliano, Pathuri, Puja, Coyle, Joseph E, Hold, Adam, Holding, Finn P, Amin, Nader, Martin, Agnes C. L, Rich, Sharna J, Berdini, Valerio, Yon, Jeff, Acklam, Paul, Burke, Rosemary, Drouin, Ludovic, Harmer, Jenny E, Jeganathan, Fiona, van Montfort, Rob L. M, Newbatt, Yvette, Tortorici, Marcello, Westlake, Maura, Wood, Amy, Hoelder, Swen, Heightman, Tom D
Published in ACS chemical biology (18.11.2016)
Published in ACS chemical biology (18.11.2016)
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Journal Article
Lipophilicity trends upon fluorination of isopropyl, cyclopropyl and 3-oxetanyl groups
Jeffries, Benjamin, Wang, Zhong, Troup, Robert I, Goupille, Anaïs, Le Questel, Jean-Yves, Fallan, Charlene, Scott, James S, Chiarparin, Elisabetta, Graton, Jérôme, Linclau, Bruno
Published in Beilstein journal of organic chemistry (02.09.2020)
Published in Beilstein journal of organic chemistry (02.09.2020)
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Journal Article
Antisense oligonucleotide activity in tumour cells is influenced by intracellular LBPA distribution and extracellular vesicle recycling
Kapustin, Alexander N, Davey, Paul, Longmire, David, Matthews, Carl, Linnane, Emily, Rustogi, Nitin, Stavrou, Maria, Devine, Paul W A, Bond, Nicholas J, Hanson, Lyndsey, Sonzini, Silvia, Revenko, Alexey, MacLeod, A Robert, Ross, Sarah, Chiarparin, Elisabetta, Puri, Sanyogitta
Published in Communications biology (01.11.2021)
Published in Communications biology (01.11.2021)
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Journal Article
Metabolism-driven in vitro/in vivo disconnect of an oral ERɑ VHL-PROTAC
Hayhow, Thomas G, Williamson, Beth, Lawson, Mandy, Cureton, Natalie, Braybrooke, Erin L, Campbell, Andrew, Carbajo, Rodrigo J, Cheraghchi-Bashi, Azadeh, Chiarparin, Elisabetta, Diène, Coura R, Fallan, Charlene, Fisher, David I, Goldberg, Frederick W, Hopcroft, Lorna, Hopcroft, Philip, Jackson, Anne, Kettle, Jason G, Klinowska, Teresa, Künzel, Ulrike, Lamont, Gillian, Lewis, Hilary J, Maglennon, Gareth, Martin, Scott, Gutierrez, Pablo Morentin, Morrow, Christopher J, Nikolaou, Myria, Nissink, J Willem M, O'Shea, Patrick, Polanski, Radoslaw, Schade, Markus, Scott, James S, Smith, Aaron, Weber, Judith, Wilson, Joanne, Yang, Bin, Crafter, Claire
Published in Communications biology (13.05.2024)
Published in Communications biology (13.05.2024)
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Journal Article
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders
Di Fabio, Romano, Pellacani, Annalisa, Faedo, Stefania, Roth, Adelheid, Piccoli, Laura, Gerrard, Philip, Porter, Rod A., Johnson, Christopher N., Thewlis, Kevin, Donati, Daniele, Stasi, Luigi, Spada, Simone, Stemp, Geoffrey, Nash, David, Branch, Clive, Kindon, Leanda, Massagrande, Mario, Poffe, Alessandro, Braggio, Simone, Chiarparin, Elisabetta, Marchioro, Carla, Ratti, Emiliangelo, Corsi, Mauro
Published in Bioorganic & medicinal chemistry letters (15.09.2011)
Published in Bioorganic & medicinal chemistry letters (15.09.2011)
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Journal Article
Exploring Weak Ligand-Protein Interactions by Long-Lived NMR States: Improved Contrast in Fragment-Based Drug Screening
Buratto, Roberto, Mammoli, Daniele, Chiarparin, Elisabetta, Williams, Glyn, Bodenhausen, Geoffrey
Published in Angewandte Chemie (International ed.) (13.10.2014)
Published in Angewandte Chemie (International ed.) (13.10.2014)
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Journal Article
Systematic Investigation of Lipophilicity Modulation by Aliphatic Fluorination Motifs
Jeffries, Benjamin, Wang, Zhong, Felstead, Hannah R, Le Questel, Jean-Yves, Scott, James S, Chiarparin, Elisabetta, Graton, Jérôme, Linclau, Bruno
Published in Journal of medicinal chemistry (13.02.2020)
Published in Journal of medicinal chemistry (13.02.2020)
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Journal Article
EED-Targeted PROTACs Degrade EED, EZH2, and SUZ12 in the PRC2 Complex
Hsu, Jessie Hao-Ru, Rasmusson, Timothy, Robinson, James, Pachl, Fiona, Read, Jon, Kawatkar, Sameer, O’ Donovan, Daniel H., Bagal, Sharan, Code, Erin, Rawlins, Philip, Argyrou, Argyrides, Tomlinson, Ronald, Gao, Ning, Zhu, Xiahui, Chiarparin, Elisabetta, Jacques, Kelly, Shen, Minhui, Woods, Haley, Bednarski, Emma, Wilson, David M., Drew, Lisa, Castaldi, M. Paola, Fawell, Stephen, Bloecher, Andrew
Published in Cell chemical biology (16.01.2020)
Published in Cell chemical biology (16.01.2020)
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Journal Article
In-Cell Quantification of Drugs by Magic-Angle Spinning Dynamic Nuclear Polarization NMR
Bertarello, Andrea, Berruyer, Pierrick, Artelsmair, Markus, Elmore, Charles S, Heydarkhan-Hagvall, Sepideh, Schade, Markus, Chiarparin, Elisabetta, Schantz, Staffan, Emsley, Lyndon
Published in Journal of the American Chemical Society (20.04.2022)
Published in Journal of the American Chemical Society (20.04.2022)
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Journal Article
Design, Synthesis, and Analytical Evaluation of Fsp 3 ‐Inspired Raman Probes for Cellular Imaging
Steven, Craig F., Lee, Martin, Nichol, Gary S., Davey, Paul R. J., Chiarparin, Elisabetta, Brunton, Valerie G., Hulme, Alison N.
Published in European journal of organic chemistry (12.08.2022)
Published in European journal of organic chemistry (12.08.2022)
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Journal Article
Conformationally Controlled sp3‐Hydrocarbon‐Based α‐Helix Mimetics
Dewis, Lydia I., Rudrakshula, Madhavachary, Williams, Christopher, Chiarparin, Elisabetta, Myers, Eddie L., Butts, Craig P., Aggarwal, Varinder K.
Published in Angewandte Chemie International Edition (05.06.2023)
Published in Angewandte Chemie International Edition (05.06.2023)
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Journal Article
Design, Synthesis, and Analytical Evaluation of Fsp(3)- Inspired Raman Probes for Cellular Imaging
Steven, Craig F., Lee, Martin, Nichol, Gary S., Davey, Paul R. J., Chiarparin, Elisabetta, Brunton, Valerie G., Hulme, Alison N.
Published in European journal of organic chemistry (12.08.2022)
Published in European journal of organic chemistry (12.08.2022)
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Journal Article