Pluripotent Stem Cell-Derived Hepatocytes Phenotypic Screening Reveals Small Molecules Targeting the CDK2/4-C/EBPα/DGAT2 Pathway Preventing ER-Stress Induced Lipid Accumulation
Parafati, Maddalena, Bae, Sang Hyo, Kirby, R Jason, Fitzek, Martina, Iyer, Preeti, Engkvist, Ola, Smith, David M, Malany, Siobhan
Published in International journal of molecular sciences (15.12.2020)
Published in International journal of molecular sciences (15.12.2020)
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A small molecule inhibitor of HER3: a proof-of-concept study
Colomba, Audrey, Fitzek, Martina, George, Roger, Weitsman, Gregory, Roberts, Selene, Zanetti-Domingues, Laura, Hirsch, Michael, Rolfe, Daniel J, Mehmood, Shahid, Madin, Andrew, Claus, Jeroen, Kjaer, Svend, Snijders, Ambrosius P, Ng, Tony, Martin-Fernandez, Marisa, Smith, David M, Parker, Peter J
Published in Biochemical journal (18.09.2020)
Published in Biochemical journal (18.09.2020)
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Phenotypic high-throughput screening platform identifies novel chemotypes for necroptosis inhibition
Brito, Hugo, Marques, Vanda, Afonso, Marta B, Brown, Dean G, Börjesson, Ulf, Selmi, Nidhal, Smith, David M, Roberts, Ieuan O, Fitzek, Martina, Aniceto, Natália, Guedes, Rita C, Moreira, Rui, Rodrigues, Cecília M P
Published in Cell death discovery (2020)
Published in Cell death discovery (2020)
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Journal Article
Identification of epidermal growth factor receptor-tyrosine kinase inhibitor targeting the VP1 pocket of human rhinovirus
Miah, Masum, Davis, Andrew M, Hannoun, Charles, Said, Joanna S, Fitzek, Martina, Preston, Marian, Smith, Dave, Uwamariya, Colores, Kärmander, Ambjörn, Lundbäck, Thomas, Bergström, Tomas, Trybala, Edward
Published in Antimicrobial agents and chemotherapy (06.03.2024)
Published in Antimicrobial agents and chemotherapy (06.03.2024)
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A small-molecule PI3Kα activator for cardioprotection and neuroregeneration
Gong, Grace Q, Bilanges, Benoit, Allsop, Ben, Masson, Glenn R, Roberton, Victoria, Askwith, Trevor, Oxenford, Sally, Madsen, Ralitsa R, Conduit, Sarah E, Bellini, Dom, Fitzek, Martina, Collier, Matt, Najam, Osman, He, Zhenhe, Wahab, Ben, McLaughlin, Stephen H, Chan, A W Edith, Feierberg, Isabella, Madin, Andrew, Morelli, Daniele, Bhamra, Amandeep, Vinciauskaite, Vanesa, Anderson, Karen E, Surinova, Silvia, Pinotsis, Nikos, Lopez-Guadamillas, Elena, Wilcox, Matthew, Hooper, Alice, Patel, Chandni, Whitehead, Maria A, Bunney, Tom D, Stephens, Len R, Hawkins, Phillip T, Katan, Matilda, Yellon, Derek M, Davidson, Sean M, Smith, David M, Phillips, James B, Angell, Richard, Williams, Roger L, Vanhaesebroeck, Bart
Published in Nature (London) (01.06.2023)
Published in Nature (London) (01.06.2023)
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Discovery of (R)-8-(1-(3,5-Difluorophenylamino)ethyl)-N,N-dimethy12-morpholino-4-oxo-4H-chromene-6-carboxamide (AZD8186): A Potent and Selective Inhibitor of PI3K beta and P13K delta for the Treatment of PTEN-Deficient Cancers
Barlaam, Bernard, Cosulich, Sabina, Degorce, Sebastien, Fitzek, Martina, Green, Stephen, Hancox, Urs, Lambert-van der Brempt, Christine, Lohmann, Jean-Jacques, Maudet, Mickael, Morgentin, Remy, Pasquet, Marie-Jeanne, Peru, Aurelien, Ple, Patrick, Saleh, Twana, Vautier, Michel, Walker, Mike, Ward, Lara, Warin, Nicolas
Published in Journal of medicinal chemistry (22.01.2015)
Published in Journal of medicinal chemistry (22.01.2015)
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Fragment-Based Screening Identifies New Quinazolinone-Based Inositol Hexakisphosphate Kinase (IP6K) Inhibitors
Heitmann, Tyler, Liao, Gangling, de León, Pablo, Ernst, Glen, Buchler, Ingrid, Wei, Huijun, Shlevkov, Evgeny, Brown, Dean, Fitzek, Martina, Collier, Matthew, Smith, David M., Barrow, James C.
Published in ACS medicinal chemistry letters (14.12.2023)
Published in ACS medicinal chemistry letters (14.12.2023)
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A phenotypic screen of Marfan syndrome iPSC-derived vascular smooth muscle cells uncovers GSK3β as a new target
Davaapil, Hongorzul, McNamara, Madeline, Granata, Alessandra, Macrae, Robyn G.C., Hirano, Mei, Fitzek, Martina, Aragon-Martin, J.A., Child, Anne, Smith, David M., Sinha, Sanjay
Published in Stem cell reports (14.02.2023)
Published in Stem cell reports (14.02.2023)
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Inhibition of PI3Kβ signaling with AZD8186 inhibits growth of PTEN-deficient breast and prostate tumors alone and in combination with docetaxel
Hancox, Urs, Cosulich, Sabina, Hanson, Lyndsey, Trigwell, Cath, Lenaghan, Carol, Ellston, Rebecca, Dry, Hannah, Crafter, Claire, Barlaam, Bernard, Fitzek, Martina, Smith, Paul D, Ogilvie, Donald, D'Cruz, Celina, Castriotta, Lillian, Wedge, Stephen R, Ward, Lara, Powell, Steve, Lawson, Mandy, Davies, Barry R, Harrington, Elizabeth A, Foster, Emily, Cumberbatch, Marie, Green, Stephen, Barry, Simon T
Published in Molecular cancer therapeutics (01.01.2015)
Published in Molecular cancer therapeutics (01.01.2015)
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Discovery of ( R )-8-(1-(3,5-Difluorophenylamino)ethyl)- N , N -dimethyl-2-morpholino-4-oxo-4 H -chromene-6-carboxamide (AZD8186): A Potent and Selective Inhibitor of PI3Kβ and PI3Kδ for the Treatment of PTEN-Deficient Cancers
Barlaam, Bernard, Cosulich, Sabina, Degorce, Sébastien, Fitzek, Martina, Green, Stephen, Hancox, Urs, Lambert-van der Brempt, Christine, Lohmann, Jean-Jacques, Maudet, Mickaël, Morgentin, Rémy, Pasquet, Marie-Jeanne, Péru, Aurélien, Plé, Patrick, Saleh, Twana, Vautier, Michel, Walker, Mike, Ward, Lara, Warin, Nicolas
Published in Journal of medicinal chemistry (22.01.2015)
Published in Journal of medicinal chemistry (22.01.2015)
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Discovery of 1-(4-(5-(5-amino-6-(5-tert-butyl-1,3,4-oxadiazol-2-yl)pyrazin-2-yl)-1-ethyl-1,2,4-triazol-3-yl)piperidin-1-yl)-3-hydroxypropan-1-one (AZD8835): A potent and selective inhibitor of PI3Kα and PI3Kδ for the treatment of cancers
Barlaam, Bernard, Cosulich, Sabina, Delouvrié, Bénédicte, Ellston, Rebecca, Fitzek, Martina, Germain, Hervé, Green, Stephen, Hancox, Urs, Harris, Craig S., Hudson, Kevin, Lambert-van der Brempt, Christine, Lebraud, Honorine, Magnien, Françoise, Lamorlette, Maryannick, Le Griffon, Antoine, Morgentin, Rémy, Ouvry, Gilles, Page, Ken, Pasquet, Georges, Polanska, Urszula, Ruston, Linette, Saleh, Twana, Vautier, Michel, Ward, Lara
Published in Bioorganic & medicinal chemistry letters (15.11.2015)
Published in Bioorganic & medicinal chemistry letters (15.11.2015)
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Abstract 4813: Comparative activity profiling of tyrosine kinase inhibitors (TKIs) against exon 20 insertions and the wild-type form of epidermal growth factor receptor (EGFR)
Ward, Richard A., Bianco, Ambra, Colclough, Nicola, Cross, Darren, Cuomo, Emanuela M., Finlay, M. Raymond V., Fitzek, Martina, Floc’h, Nicolas, Gagrica, Sladjana, Hammond, Beverley, Martin, Matthew J., McKerrecher, Darren, O’Neill, Daniel J., Orme, Jonathan P., Smith, Paul D., Staniszewska, Anna D., Urosevic, Jelena, Whalley, Nicky, Yates, James W.
Published in Cancer research (Chicago, Ill.) (01.07.2019)
Published in Cancer research (Chicago, Ill.) (01.07.2019)
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Discovery of 9-(1-anilinoethyl)-2-morpholino-4-oxo-pyrido[1,2-a]pyrimidine-7-carboxamides as PI3Kβ/δ inhibitors for the treatment of PTEN-deficient tumours
Barlaam, Bernard, Cosulich, Sabina, Degorce, Sébastien, Fitzek, Martina, Giordanetto, Fabrizio, Green, Stephen, Inghardt, Tord, Hennequin, Laurent, Hancox, Urs, Lambert-van der Brempt, Christine, Morgentin, Rémy, Pass, Sarah, Plé, Patrick, Saleh, Twana, Ward, Lara
Published in Bioorganic & medicinal chemistry letters (15.08.2014)
Published in Bioorganic & medicinal chemistry letters (15.08.2014)
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Journal Article
Design of selective PI3Kα inhibitors starting from a promiscuous pan kinase scaffold
Barlaam, Bernard, Cosulich, Sabina, Fitzek, Martina, Green, Stephen, Harris, Craig S., Hudson, Kevin, Lambert-van der Brempt, Christine, Ouvry, Gilles, Page, Ken, Ruston, Linette, Ward, Lara, Delouvrié, Bénédicte
Published in Bioorganic & medicinal chemistry letters (01.07.2015)
Published in Bioorganic & medicinal chemistry letters (01.07.2015)
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Journal Article
Discovery of a series of 8-(1-phenylpyrrolidin-2-yl)-6-carboxamide-2-morpholino-4H-chromen-4-one as PI3Kβ/δ inhibitors for the treatment of PTEN-deficient tumours
Barlaam, Bernard, Cosulich, Sabina, Degorce, Sébastien, Ellston, Rebecca, Fitzek, Martina, Green, Stephen, Hancox, Urs, Lambert-van der Brempt, Christine, Lohmann, Jean-Jacques, Maudet, Mickaël, Morgentin, Rémy, Plé, Patrick, Ward, Lara, Warin, Nicolas
Published in Bioorganic & medicinal chemistry letters (01.05.2017)
Published in Bioorganic & medicinal chemistry letters (01.05.2017)
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Journal Article
Discovery of novel imidazo[1,2-a]pyridines as inhibitors of the insulin-like growth factor-1 receptor tyrosine kinase
Ducray, Richard, Simpson, Iain, Jung, Frederic H., Nissink, J. Willem M., Kenny, Peter W., Fitzek, Martina, Walker, Graeme E., Ward, Lara T., Hudson, Kevin
Published in Bioorganic & medicinal chemistry letters (15.08.2011)
Published in Bioorganic & medicinal chemistry letters (15.08.2011)
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Journal Article
Discovery of a series of 8-(2,3-dihydro-1,4-benzoxazin-4-ylmethyl)-2-morpholino-4-oxo-chromene-6-carboxamides as PI3Kβ/δ inhibitors for the treatment of PTEN-deficient tumours
Barlaam, Bernard, Cosulich, Sabina, Degorce, Sébastien, Fitzek, Martina, Green, Stephen, Hancox, Urs, Lambert-van der Brempt, Christine, Lohmann, Jean-Jacques, Maudet, Mickaël, Morgentin, Rémy, Péru, Aurélien, Plé, Patrick, Saleh, Twana, Ward, Lara, Warin, Nicolas
Published in Bioorganic & medicinal chemistry letters (01.05.2016)
Published in Bioorganic & medicinal chemistry letters (01.05.2016)
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Abstract 2830: Discovery of AZD8835, a potent and selective inhibitor of PI3Kα and PI3Kδ for the treatment of PIK3CA -dependent cancers
Barlaam, Bernard, Cosulich, Sabina, Delouvrie, Benedicte, Fitzek, Martina, Germain, Herve, Green, Stephen, Harris, Craig S., Hudson, Kevin, Lambert-van der Brempt, Christine, Lamorlette, Maryannick, Antoine, Le Griffon, Morgentin, Remy, Ouvry, Gilles, Page, Ken, Pasquet, Georges, Ruston, Linette, Saleh, Twana, Vautier, Michel, Ward, Lara
Published in Cancer research (Chicago, Ill.) (01.08.2015)
Published in Cancer research (Chicago, Ill.) (01.08.2015)
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Journal Article
Phenotypic high-throughput screening platform identifies novel chemotypes for necroptosis inhibition
Brito, Hugo, Marques, Vanda, Afonso, Marta B, Brown, Dean G, Börjesson, Ulf, Selmi, Nidhal, Smith, David M, Roberts, Ieuan O, Fitzek, Martina, Aniceto, Natália, Guedes, Rita C, Moreira, Rui, Rodrigues, Cecília M P
Published in Cell death discovery (11.02.2020)
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Published in Cell death discovery (11.02.2020)
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