Aurora Kinase Inhibitors: Current Status and Outlook

por Bavetsias, Vassilios, Linardopoulos, Spiros
Publicado 2015

Aurora B prevents premature removal of spindle assembly checkpoint proteins from the kinetochore: A key role for Aurora B in mitosis

por Gurden, Mark D., Anderhub, Simon J., Faisal, Amir, Linardopoulos, Spiros
Publicado 2016

Aurora-A expressing tumour cells are deficient for homology-directed DNA double strand-break repair and sensitive to PARP inhibition

por Sourisseau, Tony, Maniotis, Despina, McCarthy, Afshan, Tang, Chan, Lord, Christopher J, Ashworth, Alan, Linardopoulos, Spiros
Publicado 2010

RNAi screen reveals synthetic lethality between cyclin G-associated kinase and FBXW7 by inducing aberrant mitoses

por Dolly, Saoirse O, Gurden, Mark D, Drosopoulos, Konstantinos, Clarke, Paul, de Bono, Johann, Kaye, Stan, Workman, Paul, Linardopoulos, Spiros
Publicado 2017

Metabolism of the dual FLT-3/Aurora kinase inhibitor CCT241736 in preclinical and human in vitro models: Implication for the choice of toxicology species

por Wood, Francesca L., Shepherd, Sam, Hayes, Angela, Liu, Manjuan, Grira, Katia, Mok, Yi, Atrash, Butrus, Faisal, Amir, Bavetsias, Vassilios, Linardopoulos, Spiros, Blagg, Julian, Raynaud, Florence I.
Publicado 2019

7-(Pyrazol-4-yl)-3H-imidazo[4,5-b]pyridine-based derivatives for kinase inhibition: Co-crystallisation studies with Aurora-A reveal distinct differences in the orientation of the p...

por Bavetsias, Vassilios, Pérez-Fuertes, Yolanda, McIntyre, Patrick J., Atrash, Butrus, Kosmopoulou, Magda, O’Fee, Lisa, Burke, Rosemary, Sun, Chongbo, Faisal, Amir, Bush, Katherine, Avery, Sian, Henley, Alan, Raynaud, Florence I., Linardopoulos, Spiros, Bayliss, Richard, Blagg, Julian
Publicado 2015

Selective FLT3 inhibition of FLT3-ITD(+) acute myeloid leukaemia resulting in secondary D835Y mutation: a model for emerging clinical resistance patterns

por Moore, Andrew S., Faisal, Amir, de Castro, David Gonzalez, Bavetsias, Vassilios, Sun, Chongbo, Atrash, Butrus, Valenti, Melanie, de Haven Brandon, Alexis, Avery, Sian, Mair, Debbie, Mirabella, Fabio, Swansbury, John, Pearson, Andrew D.J., Workman, Paul, Blagg, Julian, Raynaud, Florence I., Eccles, Suzanne A., Linardopoulos, Spiros
Publicado 2012

Aurora Isoform Selectivity: Design and Synthesis of Imidazo[4,5-b]pyridine Derivatives as Highly Selective Inhibitors of Aurora-A Kinase in Cells

por Bavetsias, Vassilios, Faisal, Amir, Crumpler, Simon, Brown, Nathan, Kosmopoulou, Magda, Joshi, Amar, Atrash, Butrus, Pérez-Fuertes, Yolanda, Schmitt, Jessica A., Boxall, Katherine J., Burke, Rosemary, Sun, Chongbo, Avery, Sian, Bush, Katherine, Henley, Alan, Raynaud, Florence I., Workman, Paul, Bayliss, Richard, Linardopoulos, Spiros, Blagg, Julian
Publicado 2013

Optimization of Imidazo[4,5-b]pyridine-Based Kinase Inhibitors: Identification of a Dual FLT3/Aurora Kinase Inhibitor as an Orally Bioavailable Preclinical Development Candidate fo...

por Bavetsias, Vassilios, Crumpler, Simon, Sun, Chongbo, Avery, Sian, Atrash, Butrus, Faisal, Amir, Moore, Andrew S., Kosmopoulou, Magda, Brown, Nathan, Sheldrake, Peter W., Bush, Katherine, Henley, Alan, Box, Gary, Valenti, Melanie, de Haven Brandon, Alexis, Raynaud, Florence I., Workman, Paul, Eccles, Suzanne A., Bayliss, Richard, Linardopoulos, Spiros, Blagg, Julian
Publicado 2012

Discovery of 2-(3-Benzamidopropanamido)thiazole-5-carboxylate Inhibitors of the Kinesin HSET (KIFC1) and the Development of Cellular Target Engagement Probes

por 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
Publicado 2023

Integrated genomics and functional validation identifies malignant cell specific dependencies in triple negative breast cancer

por Patel, Nirmesh, Weekes, Daniel, Drosopoulos, Konstantinos, Gazinska, Patrycja, Noel, Elodie, Rashid, Mamun, Mirza, Hasan, Quist, Jelmar, Brasó-Maristany, Fara, Mathew, Sumi, Ferro, Riccardo, Pereira, Ana Mendes, Prince, Cynthia, Noor, Farzana, Francesch-Domenech, Erika, Marlow, Rebecca, de Rinaldis, Emanuele, Grigoriadis, Anita, Linardopoulos, Spiros, Marra, Pierfrancesco, Tutt, Andrew N. J.
Publicado 2018

The discovery of potent ribosomal S6 kinase inhibitors by high-throughput screening and structure-guided drug design

por 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.
Publicado 2013

Characterisation of CCT271850, a selective, oral and potent MPS1 inhibitor, used to directly measure in vivo MPS1 inhibition vs therapeutic efficacy

por Faisal, Amir, Mak, Grace W Y, Gurden, Mark D, Xavier, Cristina P R, Anderhub, Simon J, Innocenti, Paolo, Westwood, Isaac M, Naud, Sébastien, Hayes, Angela, Box, Gary, Valenti, Melanie R, De Haven Brandon, Alexis K, O'Fee, Lisa, Schmitt, Jessica, Woodward, Hannah L, Burke, Rosemary, vanMontfort, Rob L M, Blagg, Julian, Raynaud, Florence I, Eccles, Suzanne A, Hoelder, Swen, Linardopoulos, Spiros
Publicado 2017

Structure-Based Design of Orally Bioavailable 1H-Pyrrolo[3,2-c]pyridine Inhibitors of Mitotic Kinase Monopolar Spindle 1 (MPS1)

por Naud, Sébastien, Westwood, Isaac M., Faisal, Amir, Sheldrake, Peter, Bavetsias, Vassilios, Atrash, Butrus, Cheung, Kwai-Ming J., Liu, Manjuan, Hayes, Angela, Schmitt, Jessica, Wood, Amy, Choi, Vanessa, Boxall, Kathy, Mak, Grace, Gurden, Mark, Valenti, Melanie, de Haven Brandon, Alexis, Henley, Alan, Baker, Ross, McAndrew, Craig, Matijssen, Berry, Burke, Rosemary, Hoelder, Swen, Eccles, Suzanne A., Raynaud, Florence I., Linardopoulos, Spiros, van Montfort, Rob L. M., Blagg, Julian
Publicado 2013

Introduction of a Methyl Group Curbs Metabolism of Pyrido[3,4-d]pyrimidine Monopolar Spindle 1 (MPS1) Inhibitors and Enables the Discovery of the Phase 1 Clinical Candidate N(2)-(2...

por Woodward, Hannah L., Innocenti, Paolo, Cheung, Kwai-Ming J., Hayes, Angela, Roberts, Jennie, Henley, Alan T., Faisal, Amir, Mak, Grace Wing-Yan, Box, Gary, Westwood, Isaac M., Cronin, Nora, Carter, Michael, Valenti, Melanie, De Haven Brandon, Alexis, O’Fee, Lisa, Saville, Harry, Schmitt, Jessica, Burke, Rosemary, Broccatelli, Fabio, van Montfort, Rob L. M., Raynaud, Florence I., Eccles, Suzanne A., Linardopoulos, Spiros, Blagg, Julian, Hoelder, Swen
Publicado 2018