Through the “Gatekeeper Door”: Exploiting the Active Kinase Conformation
Zuccotto, Fabio, Ardini, Elena, Casale, Elena, Angiolini, Mauro
Published in Journal of medicinal chemistry (08.04.2010)
Published in Journal of medicinal chemistry (08.04.2010)
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Lysyl-tRNA synthetase as a drug target in malaria and cryptosporidiosis
Baragan˜a, Beatriz, Forte, Barbara, Choi, Ryan, Hewitt, Stephen Nakazawa, Bueren-Calabuig, Juan A., Pisco, Joa˜o Pedro, Peet, Caroline, Dranow, David M., Robinson, David A., Jansen, Chimed, Norcross, Neil R., Vinayak, Sumiti, Anderson, Mark, Brooks, Carrie F., Cooper, Caitlin A., Damerow, Sebastian, Delves, Michael, Dowers, Karen, Duffy, James, Edwards, Thomas E., Hallyburton, Irene, Horst, Benjamin G., Hulverson, Matthew A., Ferguson, Liam, Jiménez-Díaz, María Belén, Jumani, Rajiv S., Lorimer, Donald D., Love, Melissa S., Maher, Steven, Matthews, Holly, McNamara, Case W., Miller, Peter, O’Neill, Sandra, Ojo, Kayode K., Osuna-Cabello, Maria, Pinto, Erika, Post, John, Riley, Jennifer, Rottmann, Matthias, Sanz, Laura M., Scullion, Paul, Sharma, Arvind, Shepherd, Sharon M., Shishikura, Yoko, Simeons, Frederick R. C., Stebbins, Erin E., Stojanovski, Laste, Straschil, Ursula, Tamaki, Fabio K., Tamjar, Jevgenia, Torrie, Leah S., Vantaux, Amélie, Witkowski, Benoît, Wittlin, Sergio, Yogavel, Manickam, Zuccotto, Fabio, Angulo-Barturen, Iñigo, Sinden, Robert, Baum, Jake, Gamo, Francisco-Javier, Mäser, Pascal, Kyle, Dennis E., Winzeler, Elizabeth A., Myler, Peter J., Wyatt, Paul G., Floyd, David, Matthews, David, Sharma, Amit, Striepen, Boris, Huston, Christopher D., Gray, David W., Fairlamb, Alan H., Pisliakov, Andrei V., Walpole, Chris, Read, Kevin D., Van Voorhis, Wesley C., Gilbert, Ian H.
Published in Proceedings of the National Academy of Sciences - PNAS (02.04.2019)
Published in Proceedings of the National Academy of Sciences - PNAS (02.04.2019)
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Discovery of 2‑[1-(4,4-Difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro‑1H‑isoindole-4-carboxamide (NMS-P118): A Potent, Orally Available, and Highly Selective PARP‑1 Inhibitor for Cancer Therapy
Papeo, Gianluca, Posteri, Helena, Borghi, Daniela, Busel, Alina A., Caprera, Francesco, Casale, Elena, Ciomei, Marina, Cirla, Alessandra, Corti, Emiliana, D’Anello, Matteo, Fasolini, Marina, Forte, Barbara, Galvani, Arturo, Isacchi, Antonella, Khvat, Alexander, Krasavin, Mikhail Y., Lupi, Rosita, Orsini, Paolo, Perego, Rita, Pesenti, Enrico, Pezzetta, Daniele, Rainoldi, Sonia, Riccardi-Sirtori, Federico, Scolaro, Alessandra, Sola, Francesco, Zuccotto, Fabio, Felder, Eduard R., Donati, Daniele, Montagnoli, Alessia
Published in Journal of medicinal chemistry (10.09.2015)
Published in Journal of medicinal chemistry (10.09.2015)
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Lysyl-tRNA synthetase, a target for urgently needed M. tuberculosis drugs
Green, Simon R., Davis, Susan H., Damerow, Sebastian, Engelhart, Curtis A., Mathieson, Michael, Baragaña, Beatriz, Robinson, David A., Tamjar, Jevgenia, Dawson, Alice, Tamaki, Fabio K., Buchanan, Kirsteen I., Post, John, Dowers, Karen, Shepherd, Sharon M., Jansen, Chimed, Zuccotto, Fabio, Gilbert, Ian H., Epemolu, Ola, Riley, Jennifer, Stojanovski, Laste, Osuna-Cabello, Maria, Pérez-Herrán, Esther, Rebollo, María José, Guijarro López, Laura, Casado Castro, Patricia, Camino, Isabel, Kim, Heather C., Bean, James M., Nahiyaan, Navid, Rhee, Kyu Y., Wang, Qinglan, Tan, Vee Y., Boshoff, Helena I. M., Converse, Paul J., Li, Si-Yang, Chang, Yong S., Fotouhi, Nader, Upton, Anna M., Nuermberger, Eric L., Schnappinger, Dirk, Read, Kevin D., Encinas, Lourdes, Bates, Robert H., Wyatt, Paul G., Cleghorn, Laura A. T.
Published in Nature communications (11.10.2022)
Published in Nature communications (11.10.2022)
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Identification of inhibitors of an unconventional Trypanosoma brucei kinetochore kinase
Torrie, Leah S, Zuccotto, Fabio, Robinson, David A, Gray, David W, Gilbert, Ian H, De Rycker, Manu
Published in PloS one (31.05.2019)
Published in PloS one (31.05.2019)
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Accurate prediction of dynamic protein–ligand binding using P‐score ranking
Ibrahim, Peter E. G. F., Zuccotto, Fabio, Zachariae, Ulrich, Gilbert, Ian, Bodkin, Mike
Published in Journal of computational chemistry (22.04.2024)
Published in Journal of computational chemistry (22.04.2024)
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Clinical and veterinary trypanocidal benzoxaboroles target CPSF3
Wall, Richard J., Rico, Eva, Lukac, Iva, Zuccotto, Fabio, Elg, Sara, Gilbert, Ian H., Freund, Yvonne, Alley, M. R. K., Field, Mark C., Wyllie, Susan, Horn, David
Published in Proceedings of the National Academy of Sciences - PNAS (18.09.2018)
Published in Proceedings of the National Academy of Sciences - PNAS (18.09.2018)
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A novel multiple-stage antimalarial agent that inhibits protein synthesis
Baragaña, Beatriz, Hallyburton, Irene, Lee, Marcus C S, Norcross, Neil R, Grimaldi, Raffaella, Otto, Thomas D, Proto, William R, Blagborough, Andrew M, Meister, Stephan, Wirjanata, Grennady, Ruecker, Andrea, Upton, Leanna M, Abraham, Tara S, Almeida, Mariana J, Pradhan, Anupam, Porzelle, Achim, Luksch, Torsten, Martínez, María Santos, Luksch, Torsten, Bolscher, Judith M, Woodland, Andrew, Norval, Suzanne, Zuccotto, Fabio, Thomas, John, Simeons, Frederick, Stojanovski, Laste, Osuna-Cabello, Maria, Brock, Paddy M, Churcher, Tom S, Sala, Katarzyna A, Zakutansky, Sara E, Jiménez-Díaz, María Belén, Sanz, Laura Maria, Riley, Jennifer, Basak, Rajshekhar, Campbell, Michael, Avery, Vicky M, Sauerwein, Robert W, Dechering, Koen J, Noviyanti, Rintis, Campo, Brice, Frearson, Julie A, Angulo-Barturen, Iñigo, Ferrer-Bazaga, Santiago, Gamo, Francisco Javier, Wyatt, Paul G, Leroy, Didier, Siegl, Peter, Delves, Michael J, Kyle, Dennis E, Wittlin, Sergio, Marfurt, Jutta, Price, Ric N, Sinden, Robert E, Winzeler, Elizabeth A, Charman, Susan A, Bebrevska, Lidiya, Gray, David W, Campbell, Simon, Fairlamb, Alan H, Willis, Paul A, Rayner, Julian C, Fidock, David A, Read, Kevin D, Gilbert, Ian H
Published in Nature (London) (18.06.2015)
Published in Nature (London) (18.06.2015)
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Cyclin-dependent kinase 12 is a drug target for visceral leishmaniasis
Wyllie, Susan, Thomas, Michael, Patterson, Stephen, Crouch, Sabrinia, De Rycker, Manu, Lowe, Rhiannon, Gresham, Stephanie, Urbaniak, Michael D, Otto, Thomas D, Stojanovski, Laste, Simeons, Frederick R C, Manthri, Sujatha, MacLean, Lorna M, Zuccotto, Fabio, Homeyer, Nadine, Pflaumer, Hannah, Boesche, Markus, Sastry, Lalitha, Connolly, Paul, Albrecht, Sebastian, Berriman, Matt, Drewes, Gerard, Gray, David W, Ghidelli-Disse, Sonja, Dixon, Susan, Fiandor, Jose M, Wyatt, Paul G, Ferguson, Michael A J, Fairlamb, Alan H, Miles, Timothy J, Read, Kevin D, Gilbert, Ian H
Published in Nature (London) (01.08.2018)
Published in Nature (London) (01.08.2018)
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Preclinical candidate for the treatment of visceral leishmaniasis that acts through proteasome inhibition
Wyllie, Susan, Brand, Stephen, Thomas, Michael, De Rycker, Manu, Chung, Chun-wa, Pena, Imanol, Bingham, Ryan P., Bueren-Calabuig, Juan A., Cantizani, Juan, Cebrian, David, Craggs, Peter D., Ferguson, Liam, Goswami, Panchali, Hobrath, Judith, Howe, Jonathan, Jeacock, Laura, Ko, Eun-Jung, Korczynska, Justyna, MacLean, Lorna, Manthri, Sujatha, Martinez, Maria S., Mata-Cantero, Lydia, Moniz, Sonia, Nühs, Andrea, Osuna-Cabello, Maria, Pinto, Erika, Riley, Jennifer, Robinson, Sharon, Rowland, Paul, Simeons, Frederick R. C., Shishikura, Yoko, Spinks, Daniel, Stojanovski, Laste, Thomas, John, Thompson, Stephen, Gaza, Elisabet Viayna, Wall, Richard J., Zuccotto, Fabio, Horn, David, Ferguson, Michael A. J., Fairlamb, Alan H., Fiandor, Jose M., Martin, Julio, Gray, David W., Miles, Timothy J., Gilbert, Ian H., Read, Kevin D., Marco, Maria, Wyatt, Paul G.
Published in Proceedings of the National Academy of Sciences - PNAS (07.05.2019)
Published in Proceedings of the National Academy of Sciences - PNAS (07.05.2019)
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Journal Article
DNDI-6148: A Novel Benzoxaborole Preclinical Candidate for the Treatment of Visceral Leishmaniasis
Mowbray, Charles E, Braillard, Stéphanie, Glossop, Paul A, Whitlock, Gavin A, Jacobs, Robert T, Speake, Jason, Pandi, Bharathi, Nare, Bakela, Maes, Louis, Yardley, Vanessa, Freund, Yvonne, Wall, Richard J, Carvalho, Sandra, Bello, Davide, Van den Kerkhof, Magali, Caljon, Guy, Gilbert, Ian H, Corpas-Lopez, Victoriano, Lukac, Iva, Patterson, Stephen, Zuccotto, Fabio, Wyllie, Susan
Published in Journal of medicinal chemistry (11.11.2021)
Published in Journal of medicinal chemistry (11.11.2021)
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Abstract 4206: EUD-GK-001 is a novel kinase inhibitor with in vitro anti-lymphoma activity
Scalise, Lorenzo, Tarantelli, Chiara, Zuccotto, Fabio, Spriano, Filippo, Mascia, Michele, Cascione, Luciano, Gaudio, Eugenio, Angiolini, Mauro, Bertoni, Francesco
Published in Cancer research (Chicago, Ill.) (15.08.2020)
Published in Cancer research (Chicago, Ill.) (15.08.2020)
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SophosQM: Accurate Binding Affinity Prediction in Compound Optimization
Guareschi, Riccardo, Lukac, Iva, Gilbert, Ian H., Zuccotto, Fabio
Published in ACS omega (02.05.2023)
Published in ACS omega (02.05.2023)
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Identification of a Proteasome-Targeting Arylsulfonamide with Potential for the Treatment of Chagas' Disease
Lima, Marta L, Tulloch, Lindsay B, Corpas-Lopez, Victoriano, Carvalho, Sandra, Wall, Richard J, Milne, Rachel, Rico, Eva, Patterson, Stephen, Gilbert, Ian H, Moniz, Sonia, MacLean, Lorna, Torrie, Leah S, Morgillo, Carmine, Horn, David, Zuccotto, Fabio, Wyllie, Susan
Published in Antimicrobial agents and chemotherapy (18.01.2022)
Published in Antimicrobial agents and chemotherapy (18.01.2022)
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On‐Chip Screening of a Glycomimetic Library with C‐Type Lectins Reveals Structural Features Responsible for Preferential Binding of Dectin‐2 over DC‐SIGN/R and Langerin
Medve, Laura, Achilli, Silvia, Serna, Sonia, Zuccotto, Fabio, Varga, Norbert, Thépaut, Michel, Civera, Monica, Vivès, Corinne, Fieschi, Franck, Reichardt, Niels, Bernardi, Anna
Published in Chemistry : a European journal (25.09.2018)
Published in Chemistry : a European journal (25.09.2018)
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Scaffold-Hopping Strategy on a Series of Proteasome Inhibitors Led to a Preclinical Candidate for the Treatment of Visceral Leishmaniasis
Thomas, Michael, Brand, Stephen, De Rycker, Manu, Zuccotto, Fabio, Lukac, Iva, Dodd, Peter G, Ko, Eun-Jung, Manthri, Sujatha, McGonagle, Kate, Osuna-Cabello, Maria, Riley, Jennifer, Pont, Caterina, Simeons, Frederick, Stojanovski, Laste, Thomas, John, Thompson, Stephen, Viayna, Elisabet, Fiandor, Jose M, Martin, Julio, Wyatt, Paul G, Miles, Timothy J, Read, Kevin D, Marco, Maria, Gilbert, Ian H
Published in Journal of medicinal chemistry (13.05.2021)
Published in Journal of medicinal chemistry (13.05.2021)
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Multiple unbiased approaches identify oxidosqualene cyclase as the molecular target of a promising anti-leishmanial
Paradela, Luciana S., Wall, Richard J., Carvalho, Sandra, Chemi, Giulia, Corpas-Lopez, Victoriano, Moynihan, Eoin, Bello, Davide, Patterson, Stephen, Güther, Maria Lucia S., Fairlamb, Alan H., Ferguson, Michael A.J., Zuccotto, Fabio, Martin, Julio, Gilbert, Ian H., Wyllie, Susan
Published in Cell chemical biology (20.05.2021)
Published in Cell chemical biology (20.05.2021)
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Instability of aquaglyceroporin
Horn, David, Quintana, Juan F, Zuccotto, Fabio, de Koning, Harry P, Bueren-Calabuig, Juan, Field, Mark C
Published in PLoS neglected tropical diseases (09.07.2020)
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Published in PLoS neglected tropical diseases (09.07.2020)
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