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Items: 15

1.

Inhibiting PI3Kβ with AZD8186 Regulates Key Metabolic Pathways in PTEN-Null Tumors.

Lynch JT, Polanska UM, Delpuech O, Hancox U, Trinidad AG, Michopoulos F, Lenaghan C, McEwen R, Bradford J, Polanski R, Ellston R, Avivar-Valderas A, Pilling J, Staniszewska A, Cumberbatch M, Critchlow SE, Cruzalegui F, Barry ST.

Clin Cancer Res. 2017 Dec 15;23(24):7584-7595. doi: 10.1158/1078-0432.CCR-17-0676. Epub 2017 Oct 2.

2.

Targeting KRAS-dependent tumors with AZD4785, a high-affinity therapeutic antisense oligonucleotide inhibitor of KRAS.

Ross SJ, Revenko AS, Hanson LL, Ellston R, Staniszewska A, Whalley N, Pandey SK, Revill M, Rooney C, Buckett LK, Klein SK, Hudson K, Monia BP, Zinda M, Blakey DC, Lyne PD, Macleod AR.

Sci Transl Med. 2017 Jun 14;9(394). pii: eaal5253. doi: 10.1126/scitranslmed.aal5253. Erratum in: Sci Transl Med. 2017 Jul 26;9(400):.

PMID:
28615361
3.

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.

PMID:
28347666
4.

Aurora kinase inhibitor nanoparticles target tumors with favorable therapeutic index in vivo.

Ashton S, Song YH, Nolan J, Cadogan E, Murray J, Odedra R, Foster J, Hall PA, Low S, Taylor P, Ellston R, Polanska UM, Wilson J, Howes C, Smith A, Goodwin RJ, Swales JG, Strittmatter N, Takáts Z, Nilsson A, Andren P, Trueman D, Walker M, Reimer CL, Troiano G, Parsons D, De Witt D, Ashford M, Hrkach J, Zale S, Jewsbury PJ, Barry ST.

Sci Transl Med. 2016 Feb 10;8(325):325ra17. doi: 10.1126/scitranslmed.aad2355.

5.

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.

6.

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.

PMID:
26475521
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.

8.

High Efficacy of Combination Therapy Using PI3K/AKT Inhibitors with Androgen Deprivation in Prostate Cancer Preclinical Models.

Marques RB, Aghai A, de Ridder CMA, Stuurman D, Hoeben S, Boer A, Ellston RP, Barry ST, Davies BR, Trapman J, van Weerden WM.

Eur Urol. 2015 Jun;67(6):1177-1185. doi: 10.1016/j.eururo.2014.08.053. Epub 2014 Sep 12.

PMID:
25220373
9.

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.

10.

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.

11.

Novel 4-anilinoquinazolines with C-6 carbon-linked side chains: synthesis and structure-activity relationship of a series of potent, orally active, EGF receptor tyrosine kinase inhibitors.

Hennequin LF, Ballard P, Boyle FT, Delouvrié B, Ellston RP, Halsall CT, Harris CS, Hudson K, Kendrew J, Pease JE, Ross HS, Smith P, Vincent JL.

Bioorg Med Chem Lett. 2006 May 15;16(10):2672-6. Epub 2006 Mar 3.

PMID:
16516473
12.

Imidazo[1,2-a]pyridines: a potent and selective class of cyclin-dependent kinase inhibitors identified through structure-based hybridisation.

Anderson M, Beattie JF, Breault GA, Breed J, Byth KF, Culshaw JD, Ellston RP, Green S, Minshull CA, Norman RA, Pauptit RA, Stanway J, Thomas AP, Jewsbury PJ.

Bioorg Med Chem Lett. 2003 Sep 15;13(18):3021-6.

PMID:
12941325
13.

Cyclin-dependent kinase 4 inhibitors as a treatment for cancer. Part 2: identification and optimisation of substituted 2,4-bis anilino pyrimidines.

Breault GA, Ellston RP, Green S, James SR, Jewsbury PJ, Midgley CJ, Pauptit RA, Minshull CA, Tucker JA, Pease JE.

Bioorg Med Chem Lett. 2003 Sep 15;13(18):2961-6.

PMID:
12941312
14.

Cyclin-dependent kinase 4 inhibitors as a treatment for cancer. Part 1: identification and optimisation of substituted 4,6-bis anilino pyrimidines.

Beattie JF, Breault GA, Ellston RP, Green S, Jewsbury PJ, Midgley CJ, Naven RT, Minshull CA, Pauptit RA, Tucker JA, Pease JE.

Bioorg Med Chem Lett. 2003 Sep 15;13(18):2955-60.

PMID:
12941311
15.

Aurora B couples chromosome alignment with anaphase by targeting BubR1, Mad2, and Cenp-E to kinetochores.

Ditchfield C, Johnson VL, Tighe A, Ellston R, Haworth C, Johnson T, Mortlock A, Keen N, Taylor SS.

J Cell Biol. 2003 Apr 28;161(2):267-80.

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