Changing the HTS Paradigm: AI-Driven Iterative Screening for Hit Finding

par Dreiman, Gabriel H. S., Bictash, Magda, Fish, Paul V., Griffin, Lewis, Svensson, Fredrik
Publié dans SLAS Discov (2020)

Small-molecule inhibitors of carboxylesterase Notum

par Zhao, Yuguang, Jolly, Sarah, Benvegnu, Stefano, Jones, E Yvonne, Fish, Paul V
Publié dans Future Med Chem (2021)

An improved, scalable synthesis of Notum inhibitor LP-922056 using 1-chloro-1,2-benziodoxol-3-one as a superior electrophilic chlorinating agent

par Willis, Nicky J, Bayle, Elliott D, Papageorgiou, George, Steadman, David, Atkinson, Benjamin N, Mahy, William, Fish, Paul V
Publié dans Beilstein J Org Chem (2019)

Carboxylesterase Notum Is a Druggable Target to Modulate Wnt Signaling

par Bayle, Elliott D., Svensson, Fredrik, Atkinson, Benjamin N., Steadman, David, Willis, Nicky J., Woodward, Hannah L., Whiting, Paul, Vincent, Jean-Paul, Fish, Paul V.
Publié dans J Med Chem (2021)

Design, Synthesis, and Evaluation of Tetrasubstituted Pyridines as Potent 5-HT(2C) Receptor Agonists

par Rouquet, Guy, Moore, Dianna E., Spain, Malcolm, Allwood, Daniel M., Battilocchio, Claudio, Blakemore, David C., Fish, Paul V., Jenkinson, Stephen, Jessiman, Alan S., Ley, Steven V., McMurray, Gordon, Storer, R. Ian
Publié dans ACS Med Chem Lett (2015)

Discovery of 2-phenoxyacetamides as inhibitors of the Wnt-depalmitoleating enzyme NOTUM from an X-ray fragment screen

par Atkinson, Benjamin N., Steadman, David, Zhao, Yuguang, Sipthorp, James, Vecchia, Luca, Ruza, Reinis R., Jeganathan, Fiona, Lines, Georgie, Frew, Sarah, Monaghan, Amy, Kjær, Svend, Bictash, Magda, Jones, E. Yvonne, Fish, Paul V.
Publié dans Medchemcomm (2019)

Scaffold-hopping identifies furano[2,3-d]pyrimidine amides as potent Notum inhibitors

par Atkinson, Benjamin N., Steadman, David, Mahy, William, Zhao, Yuguang, Sipthorp, James, Bayle, Elliott D., Svensson, Fredrik, Papageorgiou, George, Jeganathan, Fiona, Frew, Sarah, Monaghan, Amy, Bictash, Magda, Jones, E. Yvonne, Fish, Paul V.
Publié dans Bioorg Med Chem Lett (2020)

PFI-1 – A highly Selective Protein Interaction Inhibitor Targeting BET Bromodomains

par Picaud, Sarah, Costa, David Da, Thanasopoulou, Angeliki, Filippakopoulos, Panagis, Fish, Paul V., Philpott, Martin, Fedorov, Oleg, Brennan, Paul, Bunnage, Mark E., Owen, Dafydd R., Bradner, James E., Taniere, Philippe, O’Sullivan, Brendan, Müller, Susanne, Schwaller, Juerg, Stankovic, Tatjana, Knapp, Stefan
Publié 2013

Identification of a Chemical Probe for Bromo and Extra C-Terminal Bromodomain Inhibition through Optimization of a Fragment-Derived Hit

par Fish, Paul V., Filippakopoulos, Panagis, Bish, Gerwyn, Brennan, Paul E., Bunnage, Mark E., Cook, Andrew S., Federov, Oleg, Gerstenberger, Brian S., Jones, Hannah, Knapp, Stefan, Marsden, Brian, Nocka, Karl, Owen, Dafydd R., Philpott, Martin, Picaud, Sarah, Primiano, Michael J., Ralph, Michael J., Sciammetta, Nunzio, Trzupek, John D.
Publié 2012

Probing the SAM Binding Site of SARS-CoV-2 nsp14 in vitro Using SAM Competitive Inhibitors Guides Developing Selective bi-substrate Inhibitors

par Devkota, Kanchan, Schapira, Matthieu, Perveen, Sumera, Yazdi, Aliakbar Khalili, Li, Fengling, Chau, Irene, Ghiabi, Pegah, Hajian, Taraneh, Loppnau, Peter, Bolotokova, Albina, Satchell, Karla J.F., Wang, Ke, Li, Deyao, Liu, Jing, Smil, David, Luo, Minkui, Jin, Jian, Fish, Paul V., Brown, Peter J., Vedadi, Masoud
Publié dans bioRxiv (2021)

Identification of 2,4-disubstituted imidazopyridines as hemozoin formation inhibitors with fast killing kinetics and in vivo efficacy in the Plasmodium falciparum NSG mouse model

par Horatscheck, André, Andrijevic, Ana, Nchinda, Aloysius T., Le Manach, Claire, Paquet, Tanya, Khonde, Lutete Peguy, Dam, Jean, Pawar, Kailash, Taylor, Dale, Lawrence, Nina, Brunschwig, Christel, Gibhard, Liezl, Njoroge, Mathew, Reader, Janette, van der Watt, Mariëtte, Wicht, Kathryn, de Sousa, Ana Carolina C., Okombo, John, Maepa, Keletso, Egan, Timothy J., Birkholtz, Lyn-Marie, Basarab, Gregory S., Wittlin, Sergio, Fish, Paul V., Street, Leslie J., Duffy, James, Chibale, Kelly
Publié dans J Med Chem (2020)

Selective Targeting of Bromodomains of the Bromodomain-PHD Fingers Family Impairs Osteoclast Differentiation

par Meier, Julia C., Tallant, Cynthia, Fedorov, Oleg, Witwicka, Hanna, Hwang, Sung-Yong, van Stiphout, Ruud G., Lambert, Jean-Philippe, Rogers, Catherine, Yapp, Clarence, Gerstenberger, Brian S., Fedele, Vita, Savitsky, Pavel, Heidenreich, David, Daniels, Danette L., Owen, Dafydd R., Fish, Paul V., Igoe, Niall M., Bayle, Elliott D., Haendler, Bernard, Oppermann, Udo C.T., Buffa, Francesca, Brennan, Paul E., Müller, Susanne, Gingras, Anne Claude, Odgren, Paul R., Birnbaum, Mark J., Knapp, Stefan
Publié dans ACS Chem Biol (2017)

(R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells

par Barsyte-Lovejoy, Dalia, Li, Fengling, Oudhoff, Menno J., Tatlock, John H., Dong, Aiping, Zeng, Hong, Wu, Hong, Freeman, Spencer A., Schapira, Matthieu, Senisterra, Guillermo A., Kuznetsova, Ekaterina, Marcellus, Richard, Allali-Hassani, Abdellah, Kennedy, Steven, Lambert, Jean-Philippe, Couzens, Amber L., Aman, Ahmed, Gingras, Anne-Claude, Al-Awar, Rima, Fish, Paul V., Gerstenberger, Brian S., Roberts, Lee, Benn, Caroline L., Grimley, Rachel L., Braam, Mitchell J. S., Rossi, Fabio M. V., Sudol, Marius, Brown, Peter J., Bunnage, Mark E., Owen, Dafydd R., Zaph, Colby, Vedadi, Masoud, Arrowsmith, Cheryl H.
Publié 2014

Apc-mutant cells deploy Notum to bias clonal competition and drive cancer

par Flanagan, Dustin J., Pentinmikko, Nalle, Luopajärvi, Kalle, Willis, Nicky J., Gilroy, Kathryn, Raven, Alexander P., Mcgarry, Lynn, Englund, Johanna I., Webb, Anna, Scharaw, Sandra, Nasreddin, Nadia, Hodder, Michael C., Ridgway, Rachel A., Minnee, Emma, Sphyris, Nathalie, Gilchrist, Ella, Najumudeen, Arafath K., Romagnolo, Beatrice, Perret, Christine, Williams, Ann C., Clevers, Hans, Nummela, Pirjo, Lähde, Marianne, Alitalo, Kari, Hietakangas, Ville, Hedley, Ann, Clark, William, Nixon, Colin, Kirschner, Kristina, Yvonne Jones, E., Ristimäki, Ari, Leedham, Simon, Fish, Paul V., Vincent, Jean-Paul, Katajisto, Pekka, Sansom, Owen J.
Publié dans Nature (2021)

UCT943, a Next-Generation Plasmodium falciparum PI4K Inhibitor Preclinical Candidate for the Treatment of Malaria

par Brunschwig, Christel, Lawrence, Nina, Taylor, Dale, Abay, Efrem, Njoroge, Mathew, Basarab, Gregory S., Le Manach, Claire, Paquet, Tanya, Cabrera, Diego Gonzàlez, Nchinda, Aloysius T., de Kock, Carmen, Wiesner, Lubbe, Denti, Paolo, Waterson, David, Blasco, Benjamin, Leroy, Didier, Witty, Michael J., Donini, Cristina, Duffy, James, Wittlin, Sergio, White, Karen L., Charman, Susan A., Jiménez-Díaz, Maria Belén, Angulo-Barturen, Iñigo, Herreros, Esperanza, Gamo, Francisco Javier, Rochford, Rosemary, Mancama, Dalu, Coetzer, Theresa L., van der Watt, Mariëtte E., Reader, Janette, Birkholtz, Lyn-Marie, Marsh, Kennan C., Solapure, Suresh M., Burke, John E., McPhail, Jacob A., Vanaerschot, Manu, Fidock, David A., Fish, Paul V., Siegl, Peter, Smith, Dennis A., Wirjanata, Grennady, Noviyanti, Rintis, Price, Ric N., Marfurt, Jutta, Silue, Kigbafori D., Street, Leslie J., Chibale, Kelly
Publié dans Antimicrob Agents Chemother (2018)

Erratum for Brunschwig et al., “UCT943, a Next-Generation Plasmodium falciparum PI4K Inhibitor Preclinical Candidate for the Treatment of Malaria”

par Brunschwig, Christel, Lawrence, Nina, Taylor, Dale, Abay, Efrem, Njoroge, Mathew, Basarab, Gregory S., Le Manach, Claire, Paquet, Tanya, Gonzàlez Cabrera, Diego, Nchinda, Aloysius T., de Kock, Carmen, Wiesner, Lubbe, Denti, Paolo, Waterson, David, Blasco, Benjamin, Leroy, Didier, Witty, Michael J., Donini, Cristina, Duffy, James, Wittlin, Sergio, White, Karen L., Charman, Susan A., Jiménez-Díaz, Maria Belén, Angulo-Barturen, Iñigo, Herreros, Esperanza, Gamo, Francisco Javier, Rochford, Rosemary, Mancama, Dalu, Coetzer, Theresa L., van der Watt, Mariëtte E., Reader, Janette, Birkholtz, Lyn-Marie, Marsh, Kennan C., Solapure, Suresh M., Burke, John E., McPhail, Jacob A., Vanaerschot, Manu, Fidock, David A., Fish, Paul V., Siegl, Peter, Smith, Dennis A., Wirjanata, Grennady, Noviyanti, Rintis, Price, Ric N., Marfurt, Jutta, Silue, Kigbafori D., Street, Leslie J., Chibale, Kelly
Publié dans Antimicrob Agents Chemother (2018)