An Irreversible Inhibitor of HSP72 that Unexpectedly Targets Lysine‐56

por Pettinger, Jonathan, Le Bihan, Yann‐Vaï, Widya, Marcella, van Montfort, Rob L. M., Jones, Keith, Cheeseman, Matthew D.
Publicado 2017

5-Hydroxy-5-methylhydantoin DNA lesion, a molecular trap for DNA glycosylases

por Le Bihan, Yann-Vaï, Angeles Izquierdo, Maria, Coste, Franck, Aller, Pierre, Culard, Françoise, Gehrke, Tim H., Essalhi, Kadija, Carell, Thomas, Castaing, Bertrand
Publicado 2011

The orientation of the C-terminal domain of the Saccharomyces cerevisiae Rap1 protein is determined by its binding to DNA

por Matot, Béatrice, Le Bihan, Yann-Vaï, Lescasse, Rachel, Pérez, Javier, Miron, Simona, David, Gabriel, Castaing, Bertrand, Weber, Patrick, Raynal, Bertrand, Zinn-Justin, Sophie, Gasparini, Sylvaine, Le Du, Marie-Hélène
Publicado 2012

Pyrido[3,4-d]pyrimidin-4(3H)-one metabolism mediated by aldehyde oxidase is blocked by C2-substitution

por Hayes, Angela, Mok, N. Yi, Liu, Manjuan, Thai, Ching, Henley, Alan T., Atrash, Butrus, Lanigan, Rachel M., Sejberg, Jimmy, Le Bihan, Yann-Vaï, Bavetsias, Vassilios, Blagg, Julian, Raynaud, Florence I.
Publicado 2016

Discovery and Characterization of a Cryptic Secondary Binding Site in the Molecular Chaperone HSP70

por O’Connor, Suzanne, Le Bihan, Yann-Vaï, Westwood, Isaac M., Liu, Manjuan, Mak, Oi Wei, Zazeri, Gabriel, Povinelli, Ana P. R., Jones, Alan M., van Montfort, Rob, Reynisson, Jóhannes, Collins, Ian
Publicado 2022

A higher-order entity formed by the flexible assembly of RAP1 with TRF2

por Gaullier, Guillaume, Miron, Simona, Pisano, Sabrina, Buisson, Rémi, Le Bihan, Yann-Vaï, Tellier-Lebègue, Carine, Messaoud, Wala, Roblin, Pierre, Guimarães, Beatriz G., Thai, Robert, Giraud-Panis, Marie-Josèphe, Gilson, Eric, Le Du, Marie-Hélène
Publicado 2016

The N-terminal domains of TRF1 and TRF2 regulate their ability to condense telomeric DNA

por Poulet, Anaïs, Pisano, Sabrina, Faivre-Moskalenko, Cendrine, Pei, Bei, Tauran, Yannick, Haftek-Terreau, Zofia, Brunet, Frédéric, Le Bihan, Yann-Vaï, Ledu, Marie-Hélène, Montel, Fabien, Hugo, Nicolas, Amiard, Simon, Argoul, Françoise, Chaboud, Annie, Gilson, Eric, Giraud-Panis, Marie-Josèphe
Publicado 2012

Privileged Structures and Polypharmacology within and between Protein Families

por Meyers, Joshua, Chessum, Nicola E. A., Ali, Salyha, Mok, N. Yi, Wilding, Birgit, Pasqua, A. Elisa, Rowlands, Martin, Tucker, Michael J., Evans, Lindsay E., Rye, Carl S., O’Fee, Lisa, Le Bihan, Yann-Vaï, Burke, Rosemary, Carter, Michael, Workman, Paul, Blagg, Julian, Brown, Nathan, van Montfort, Rob L. M., Jones, Keith, Cheeseman, Matthew D.
Publicado 2018

iTAG an optimized IMiD-induced degron for targeted protein degradation in human and murine cells

por 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
Publicado 2023

Into Deep Water: Optimizing BCL6 Inhibitors by Growing into a Solvated Pocket

por 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
Publicado 2021

Optimizing Shape Complementarity Enables the Discovery of Potent Tricyclic BCL6 Inhibitors

por 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
Publicado 2022

C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (K...

por Le Bihan, Yann-Vaï, Lanigan, Rachel M., Atrash, Butrus, McLaughlin, Mark G., Velupillai, Srikannathasan, Malcolm, Andrew G., England, Katherine S., Ruda, Gian Filippo, Mok, N. Yi, Tumber, Anthony, Tomlin, Kathy, Saville, Harry, Shehu, Erald, McAndrew, Craig, Carmichael, LeAnne, Bennett, James M., Jeganathan, Fiona, Eve, Paul, Donovan, Adam, Hayes, Angela, Wood, Francesca, Raynaud, Florence I., Fedorov, Oleg, Brennan, Paul E., Burke, Rosemary, van Montfort, Rob L.M., Rossanese, Olivia W., Blagg, Julian, Bavetsias, Vassilios
Publicado 2019

Discovery of an In Vivo Chemical Probe for BCL6 Inhibition by Optimization of Tricyclic Quinolinones

por Harnden, Alice C., Davis, Owen A., Box, Gary M., Hayes, Angela, Johnson, Louise D., Henley, Alan T., de Haven Brandon, Alexis K., Valenti, Melanie, Cheung, Kwai-Ming J., Brennan, Alfie, Huckvale, Rosemary, Pierrat, Olivier A., Talbot, Rachel, Bright, Michael D., Akpinar, Hafize Aysin, Miller, Daniel S. J., Tarantino, Dalia, Gowan, Sharon, de Klerk, Selby, McAndrew, Peter Craig, Le Bihan, Yann-Vaï, Meniconi, Mirco, Burke, Rosemary, Kirkin, Vladimir, van Montfort, Rob L. M., Raynaud, Florence I., Rossanese, Olivia W., Bellenie, Benjamin R., Hoelder, Swen
Publicado 2023

Achieving In Vivo Target Depletion through the Discovery and Optimization of Benzimidazolone BCL6 Degraders

por 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
Publicado 2020

Improved Binding Affinity and Pharmacokinetics Enable Sustained Degradation of BCL6 In Vivo

por Huckvale, Rosemary, Harnden, Alice C., Cheung, Kwai-Ming J., Pierrat, Olivier A., Talbot, Rachel, Box, Gary M., Henley, Alan T., de Haven Brandon, Alexis K., Hallsworth, Albert E., Bright, Michael D., Akpinar, Hafize Aysin, Miller, Daniel S. J., Tarantino, Dalia, Gowan, Sharon, Hayes, Angela, Gunnell, Emma A., Brennan, Alfie, Davis, Owen A., Johnson, Louise D., de Klerk, Selby, McAndrew, Craig, Le Bihan, Yann-Vaï, Meniconi, Mirco, Burke, Rosemary, Kirkin, Vladimir, van Montfort, Rob L. M., Raynaud, Florence I., Rossanese, Olivia W., Bellenie, Benjamin R., Hoelder, Swen
Publicado 2022

Discovering cell-active BCL6 inhibitors: effectively combining biochemical HTS with multiple biophysical techniques, X-ray crystallography and cell-based assays

por 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.
Publicado 2022

8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors

por Bavetsias, Vassilios, Lanigan, Rachel M., Ruda, Gian Filippo, Atrash, Butrus, McLaughlin, Mark G., Tumber, Anthony, Mok, N. Yi, Le Bihan, Yann-Vaï, Dempster, Sally, Boxall, Katherine J., Jeganathan, Fiona, Hatch, Stephanie B., Savitsky, Pavel, Velupillai, Srikannathasan, Krojer, Tobias, England, Katherine S., Sejberg, Jimmy, Thai, Ching, Donovan, Adam, Pal, Akos, Scozzafava, Giuseppe, Bennett, James M., Kawamura, Akane, Johansson, Catrine, Szykowska, Aleksandra, Gileadi, Carina, Burgess-Brown, Nicola A., von Delft, Frank, Oppermann, Udo, Walters, Zoe, Shipley, Janet, Raynaud, Florence I., Westaway, Susan M., Prinjha, Rab K., Fedorov, Oleg, Burke, Rosemary, Schofield, Christopher J., Westwood, Isaac M., Bountra, Chas, Müller, Susanne, van Montfort, Rob L. M., Brennan, Paul E., Blagg, Julian
Publicado 2016