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Items: 46


Combination of mTORC1/2 inhibitor vistusertib plus fulvestrant in vitro and in vivo targets oestrogen receptor-positive endocrine-resistant breast cancer.

Pancholi S, Leal MF, Ribas R, Simigdala N, Schuster E, Chateau-Joubert S, Zabaglo L, Hills M, Dodson A, Gao Q, Johnston SR, Dowsett M, Cosulich SC, Maragoni E, Martin LA.

Breast Cancer Res. 2019 Dec 4;21(1):135. doi: 10.1186/s13058-019-1222-0.


How is the acyl chain composition of phosphoinositides created and does it matter?

Barneda D, Cosulich S, Stephens L, Hawkins P.

Biochem Soc Trans. 2019 Oct 31;47(5):1291-1305. doi: 10.1042/BST20190205.


MYC-Driven Small-Cell Lung Cancer is Metabolically Distinct and Vulnerable to Arginine Depletion.

Chalishazar MD, Wait SJ, Huang F, Ireland AS, Mukhopadhyay A, Lee Y, Schuman SS, Guthrie MR, Berrett KC, Vahrenkamp JM, Hu Z, Kudla M, Modzelewska K, Wang G, Ingolia NT, Gertz J, Lum DH, Cosulich SC, Bomalaski JS, DeBerardinis RJ, Oliver TG.

Clin Cancer Res. 2019 Aug 15;25(16):5107-5121. doi: 10.1158/1078-0432.CCR-18-4140. Epub 2019 Jun 4.


AKT/mTORC2 Inhibition Activates FOXO1 Function in CLL Cells Reducing B-Cell Receptor-Mediated Survival.

Cosimo E, Tarafdar A, Moles MW, Holroyd AK, Malik N, Catherwood MA, Hay J, Dunn KM, Macdonald AM, Guichard SM, O'Rourke D, Leach MT, Sansom OJ, Cosulich SC, McCaig AM, Michie AM.

Clin Cancer Res. 2019 Mar 1;25(5):1574-1587. doi: 10.1158/1078-0432.CCR-18-2036. Epub 2018 Dec 17.


Combination of dual mTORC1/2 inhibition and immune-checkpoint blockade potentiates anti-tumour immunity.

Langdon S, Hughes A, Taylor MA, Kuczynski EA, Mele DA, Delpuech O, Jarvis L, Staniszewska A, Cosulich S, Carnevalli LS, Sinclair C.

Oncoimmunology. 2018 May 7;7(8):e1458810. doi: 10.1080/2162402X.2018.1458810. eCollection 2018.


Combined Inhibition of mTOR and CDK4/6 Is Required for Optimal Blockade of E2F Function and Long-term Growth Inhibition in Estrogen Receptor-positive Breast Cancer.

Michaloglou C, Crafter C, Siersbaek R, Delpuech O, Curwen JO, Carnevalli LS, Staniszewska AD, Polanska UM, Cheraghchi-Bashi A, Lawson M, Chernukhin I, McEwen R, Carroll JS, Cosulich SC.

Mol Cancer Ther. 2018 May;17(5):908-920. doi: 10.1158/1535-7163.MCT-17-0537. Epub 2018 Feb 26.


Evaluation of the combination of the dual m-TORC1/2 inhibitor vistusertib (AZD2014) and paclitaxel in ovarian cancer models.

Wong Te Fong AC, Thavasu P, Gagrica S, Swales KE, Leach MO, Cosulich SC, Chung YL, Banerji U.

Oncotarget. 2017 Dec 6;8(69):113874-113884. doi: 10.18632/oncotarget.23022. eCollection 2017 Dec 26.


PTEN Regulates PI(3,4)P2 Signaling Downstream of Class I PI3K.

Malek M, Kielkowska A, Chessa T, Anderson KE, Barneda D, Pir P, Nakanishi H, Eguchi S, Koizumi A, Sasaki J, Juvin V, Kiselev VY, Niewczas I, Gray A, Valayer A, Spensberger D, Imbert M, Felisbino S, Habuchi T, Beinke S, Cosulich S, Le Novère N, Sasaki T, Clark J, Hawkins PT, Stephens LR.

Mol Cell. 2017 Nov 2;68(3):566-580.e10. doi: 10.1016/j.molcel.2017.09.024. Epub 2017 Oct 19.


Discovery of a novel aminopyrazine series as selective PI3Kα inhibitors.

Barlaam B, Cosulich S, Fitzek M, Germain H, Green S, Hanson LL, Harris CS, Hancox U, Hudson K, Lambert-van der Brempt C, Lamorlette M, Magnien F, Ouvry G, Page K, Ruston L, Ward L, Delouvrié B.

Bioorg Med Chem Lett. 2017 Jul 1;27(13):3030-3035. doi: 10.1016/j.bmcl.2017.05.028. Epub 2017 May 10.


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 B, Cosulich S, Degorce S, Ellston R, Fitzek M, Green S, Hancox U, Lambert-van der Brempt C, Lohmann JJ, Maudet M, Morgentin R, Plé P, Ward L, Warin N.

Bioorg Med Chem Lett. 2017 May 1;27(9):1949-1954. doi: 10.1016/j.bmcl.2017.03.027. Epub 2017 Mar 14.


Targeting mTOR pathway inhibits tumor growth in different molecular subtypes of triple-negative breast cancers.

Hatem R, El Botty R, Chateau-Joubert S, Servely JL, Labiod D, de Plater L, Assayag F, Coussy F, Callens C, Vacher S, Reyal F, Cosulich S, Diéras V, Bièche I, Marangoni E.

Oncotarget. 2016 Jul 26;7(30):48206-48219. doi: 10.18632/oncotarget.10195.


Overcoming mTOR resistance mutations with a new-generation mTOR inhibitor.

Rodrik-Outmezguine VS, Okaniwa M, Yao Z, Novotny CJ, McWhirter C, Banaji A, Won H, Wong W, Berger M, de Stanchina E, Barratt DG, Cosulich S, Klinowska T, Rosen N, Shokat KM.

Nature. 2016 Jun 9;534(7606):272-6. doi: 10.1038/nature17963. Epub 2016 May 18.


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 B, Cosulich S, Degorce S, Fitzek M, Green S, Hancox U, Lambert-van der Brempt C, Lohmann JJ, Maudet M, Morgentin R, Péru A, Plé P, Saleh T, Ward L, Warin N.

Bioorg Med Chem Lett. 2016 May 1;26(9):2318-23. doi: 10.1016/j.bmcl.2016.03.034. Epub 2016 Mar 11.


Intermittent High-Dose Scheduling of AZD8835, a Novel Selective Inhibitor of PI3Kα and PI3Kδ, Demonstrates Treatment Strategies for PIK3CA-Dependent Breast Cancers.

Hudson K, Hancox UJ, Trigwell C, McEwen R, Polanska UM, Nikolaou M, Morentin Gutierrez P, Avivar-Valderas A, Delpuech O, Dudley P, Hanson L, Ellston R, Jones A, Cumberbatch M, Cosulich SC, Ward L, Cruzalegui F, Green S.

Mol Cancer Ther. 2016 May;15(5):877-89. doi: 10.1158/1535-7163.MCT-15-0687. Epub 2016 Feb 2.


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 B, Cosulich S, Delouvrié B, Ellston R, Fitzek M, Germain H, Green S, Hancox U, Harris CS, Hudson K, Lambert-van der Brempt C, Lebraud H, Magnien F, Lamorlette M, Le Griffon A, Morgentin R, Ouvry G, Page K, Pasquet G, Polanska U, Ruston L, Saleh T, Vautier M, Ward L.

Bioorg Med Chem Lett. 2015 Nov 15;25(22):5155-62. doi: 10.1016/j.bmcl.2015.10.002. Epub 2015 Oct 9.


AZD2014, an Inhibitor of mTORC1 and mTORC2, Is Highly Effective in ER+ Breast Cancer When Administered Using Intermittent or Continuous Schedules.

Guichard SM, Curwen J, Bihani T, D'Cruz CM, Yates JW, Grondine M, Howard Z, Davies BR, Bigley G, Klinowska T, Pike KG, Pass M, Chresta CM, Polanska UM, McEwen R, Delpuech O, Green S, Cosulich SC.

Mol Cancer Ther. 2015 Nov;14(11):2508-18. doi: 10.1158/1535-7163.MCT-15-0365. Epub 2015 Sep 10.


Novel Role for p110β PI 3-Kinase in Male Fertility through Regulation of Androgen Receptor Activity in Sertoli Cells.

Guillermet-Guibert J, Smith LB, Halet G, Whitehead MA, Pearce W, Rebourcet D, León K, Crépieux P, Nock G, Strömstedt M, Enerback M, Chelala C, Graupera M, Carroll J, Cosulich S, Saunders PT, Huhtaniemi I, Vanhaesebroeck B.

PLoS Genet. 2015 Jul 1;11(7):e1005304. doi: 10.1371/journal.pgen.1005304. eCollection 2015 Jul.


Design of selective PI3Kα inhibitors starting from a promiscuous pan kinase scaffold.

Barlaam B, Cosulich S, Fitzek M, Green S, Harris CS, Hudson K, Lambert-van der Brempt C, Ouvry G, Page K, Ruston L, Ward L, Delouvrié B.

Bioorg Med Chem Lett. 2015 Jul 1;25(13):2679-85. doi: 10.1016/j.bmcl.2015.04.084. Epub 2015 Apr 29.


Discovery of (R)-8-(1-(3,5-difluorophenylamino)ethyl)-N,N-dimethyl-2-morpholino-4-oxo-4H-chromene-6-carboxamide (AZD8186): a potent and selective inhibitor of PI3Kβ and PI3Kδ for the treatment of PTEN-deficient cancers.

Barlaam B, Cosulich S, Degorce S, Fitzek M, Green S, Hancox U, Lambert-van der Brempt C, Lohmann JJ, Maudet M, Morgentin R, Pasquet MJ, Péru A, Plé P, Saleh T, Vautier M, Walker M, Ward L, Warin N.

J Med Chem. 2015 Jan 22;58(2):943-62. doi: 10.1021/jm501629p. Epub 2015 Jan 7.


Inhibition of PI3Kβ signaling with AZD8186 inhibits growth of PTEN-deficient breast and prostate tumors alone and in combination with docetaxel.

Hancox U, Cosulich S, Hanson L, Trigwell C, Lenaghan C, Ellston R, Dry H, Crafter C, Barlaam B, Fitzek M, Smith PD, Ogilvie D, D'Cruz C, Castriotta L, Wedge SR, Ward L, Powell S, Lawson M, Davies BR, Harrington EA, Foster E, Cumberbatch M, Green S, Barry ST.

Mol Cancer Ther. 2015 Jan;14(1):48-58. doi: 10.1158/1535-7163.MCT-14-0406. Epub 2014 Nov 14.


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 B, Cosulich S, Degorce S, Fitzek M, Giordanetto F, Green S, Inghardt T, Hennequin L, Hancox U, Lambert-van der Brempt C, Morgentin R, Pass S, Plé P, Saleh T, Ward L.

Bioorg Med Chem Lett. 2014 Aug 15;24(16):3928-35. doi: 10.1016/j.bmcl.2014.06.040. Epub 2014 Jun 21.


Identification of a subset of human non-small cell lung cancer patients with high PI3Kβ and low PTEN expression, more prevalent in squamous cell carcinoma.

Cumberbatch M, Tang X, Beran G, Eckersley S, Wang X, Ellston RP, Dearden S, Cosulich S, Smith PD, Behrens C, Kim ES, Su X, Fan S, Gray N, Blowers DP, Wistuba II, Womack C.

Clin Cancer Res. 2014 Feb 1;20(3):595-603. doi: 10.1158/1078-0432.CCR-13-1638. Epub 2013 Nov 27.


Signaling via class IA Phosphoinositide 3-kinases (PI3K) in human, breast-derived cell lines.

Juvin V, Malek M, Anderson KE, Dion C, Chessa T, Lecureuil C, Ferguson GJ, Cosulich S, Hawkins PT, Stephens LR.

PLoS One. 2013 Oct 4;8(10):e75045. doi: 10.1371/journal.pone.0075045. eCollection 2013.


Kinase-substrate enrichment analysis provides insights into the heterogeneity of signaling pathway activation in leukemia cells.

Casado P, Rodriguez-Prados JC, Cosulich SC, Guichard S, Vanhaesebroeck B, Joel S, Cutillas PR.

Sci Signal. 2013 Mar 26;6(268):rs6. doi: 10.1126/scisignal.2003573.


Stable isotope-labelling analysis of the impact of inhibition of the mammalian target of rapamycin on protein synthesis.

Huo Y, Iadevaia V, Yao Z, Kelly I, Cosulich S, Guichard S, Foster LJ, Proud CG.

Biochem J. 2012 May 15;444(1):141-51. doi: 10.1042/BJ20112107.


Preclinical pharmacology of AZD5363, an inhibitor of AKT: pharmacodynamics, antitumor activity, and correlation of monotherapy activity with genetic background.

Davies BR, Greenwood H, Dudley P, Crafter C, Yu DH, Zhang J, Li J, Gao B, Ji Q, Maynard J, Ricketts SA, Cross D, Cosulich S, Chresta CC, Page K, Yates J, Lane C, Watson R, Luke R, Ogilvie D, Pass M.

Mol Cancer Ther. 2012 Apr;11(4):873-87. doi: 10.1158/1535-7163.MCT-11-0824-T. Epub 2012 Jan 31.


Diverse heterocyclic scaffolds as allosteric inhibitors of AKT.

Kettle JG, Brown S, Crafter C, Davies BR, Dudley P, Fairley G, Faulder P, Fillery S, Greenwood H, Hawkins J, James M, Johnson K, Lane CD, Pass M, Pink JH, Plant H, Cosulich SC.

J Med Chem. 2012 Feb 9;55(3):1261-73. doi: 10.1021/jm201394e. Epub 2012 Jan 27.


AZD8055 is a potent, selective, and orally bioavailable ATP-competitive mammalian target of rapamycin kinase inhibitor with in vitro and in vivo antitumor activity.

Chresta CM, Davies BR, Hickson I, Harding T, Cosulich S, Critchlow SE, Vincent JP, Ellston R, Jones D, Sini P, James D, Howard Z, Dudley P, Hughes G, Smith L, Maguire S, Hummersone M, Malagu K, Menear K, Jenkins R, Jacobsen M, Smith GC, Guichard S, Pass M.

Cancer Res. 2010 Jan 1;70(1):288-98. doi: 10.1158/0008-5472.CAN-09-1751. Epub 2009 Dec 22.


Ku-0063794 is a specific inhibitor of the mammalian target of rapamycin (mTOR).

García-Martínez JM, Moran J, Clarke RG, Gray A, Cosulich SC, Chresta CM, Alessi DR.

Biochem J. 2009 Jun 12;421(1):29-42. doi: 10.1042/BJ20090489.


PPAR alpha and the regulation of cell division and apoptosis.

Roberts RA, Chevalier S, Hasmall SC, James NH, Cosulich SC, Macdonald N.

Toxicology. 2002 Dec 27;181-182:167-70. Review.


Role of cytokines in non-genotoxic hepatocarcinogenesis: cause or effect?

Roberts RA, James NH, Cosulich S, Hasmall SC, Orphanides G.

Toxicol Lett. 2001 Mar 31;120(1-3):301-6. Review.


A dominant negative form of IKK2 prevents suppression of apoptosis by the peroxisome proliferator nafenopin.

Cosulich SC, James NH, Needham MR, Newham PP, Bundell KR, Roberts RA.

Carcinogenesis. 2000 Sep;21(9):1757-60.


Role of MAP kinase signalling pathways in the mode of action of peroxisome proliferators.

Cosulich S, James N, Roberts R.

Carcinogenesis. 2000 Apr;21(4):579-84.


Role for tumor necrosis factor alpha receptor 1 and interleukin-1 receptor in the suppression of mouse hepatocyte apoptosis by the peroxisome proliferator nafenopin.

West DA, James NH, Cosulich SC, Holden PR, Brindle R, Rolfe M, Roberts RA.

Hepatology. 1999 Dec;30(6):1417-24.


Bcl-2 regulates a caspase-3/caspase-2 apoptotic cascade in cytosolic extracts.

Swanton E, Savory P, Cosulich S, Clarke P, Woodman P.

Oncogene. 1999 Mar 11;18(10):1781-7.


Bcl-2 regulates amplification of caspase activation by cytochrome c.

Cosulich SC, Savory PJ, Clarke PR.

Curr Biol. 1999 Feb 11;9(3):147-50.


Regulation of apoptosis by BH3 domains in a cell-free system.

Cosulich SC, Worrall V, Hedge PJ, Green S, Clarke PR.

Curr Biol. 1997 Dec 1;7(12):913-20.


Cleavage of rabaptin-5 blocks endosome fusion during apoptosis.

Cosulich SC, Horiuchi H, Zerial M, Clarke PR, Woodman PG.

EMBO J. 1997 Oct 15;16(20):6182-91.


Cleavage and inactivation of DNA-dependent protein kinase catalytic subunit during apoptosis in Xenopus egg extracts.

Le Romancer M, Cosulich SC, Jackson SP, Clarke PR.

J Cell Sci. 1996 Dec;109 ( Pt 13):3121-7.


Apoptosis: does stress kill?

Cosulich S, Clarke P.

Curr Biol. 1996 Dec 1;6(12):1586-8. Review.


Bcl-2 regulates activation of apoptotic proteases in a cell-free system.

Cosulich SC, Green S, Clarke PR.

Curr Biol. 1996 Aug 1;6(8):997-1005.


A common requirement for p21c-ras function in the mitogenic signaling pathways of Swiss 3T3 fibroblasts.

Roden RB, Shachar-Hill Y, Cosulich SC, Hesketh TR, Metcalfe JC.

Cell Growth Differ. 1993 Dec;4(12):957-64.


Effects of fluorinated inositols on the proliferation of Swiss 3T3 fibroblasts.

Cosulich SC, Offer J, Smith GA, Hesketh R, Metcalfe JC.

Biochem J. 1993 Jun 15;292 ( Pt 3):719-24.

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