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Items: 10

1.

Combined Inhibition of PI3Kβ and mTOR Inhibits Growth of PTEN-null Tumors.

Lynch JT, Polanska UM, Hancox U, Delpuech O, Maynard J, Trigwell C, Eberlein C, Lenaghan C, Polanski R, Avivar-Valderas A, Cumberbatch M, Klinowska T, Critchlow SE, Cruzalegui F, Barry ST.

Mol Cancer Ther. 2018 Nov;17(11):2309-2319. doi: 10.1158/1535-7163.MCT-18-0183. Epub 2018 Aug 10.

2.

Discovery of a Potent, Selective, Orally Bioavailable, and Efficacious Novel 2-(Pyrazol-4-ylamino)-pyrimidine Inhibitor of the Insulin-like Growth Factor-1 Receptor (IGF-1R).

Degorce SL, Boyd S, Curwen JO, Ducray R, Halsall CT, Jones CD, Lach F, Lenz EM, Pass M, Pass S, Trigwell C.

J Med Chem. 2016 May 26;59(10):4859-66. doi: 10.1021/acs.jmedchem.6b00203. Epub 2016 Apr 22.

PMID:
27078757
3.

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.

4.

Feedback suppression of PI3Kα signaling in PTEN-mutated tumors is relieved by selective inhibition of PI3Kβ.

Schwartz S, Wongvipat J, Trigwell CB, Hancox U, Carver BS, Rodrik-Outmezguine V, Will M, Yellen P, de Stanchina E, Baselga J, Scher HI, Barry ST, Sawyers CL, Chandarlapaty S, Rosen N.

Cancer Cell. 2015 Jan 12;27(1):109-22. doi: 10.1016/j.ccell.2014.11.008. Epub 2014 Dec 24.

5.

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.

6.

Discovery of AZD8931, an Equipotent, Reversible Inhibitor of Signaling by EGFR, HER2, and HER3 Receptors.

Barlaam B, Anderton J, Ballard P, Bradbury RH, Hennequin LF, Hickinson DM, Kettle JG, Kirk G, Klinowska T, Lambert-van der Brempt C, Trigwell C, Vincent J, Ogilvie D.

ACS Med Chem Lett. 2013 May 31;4(8):742-6. doi: 10.1021/ml400146c. eCollection 2013 Aug 8.

7.

AZD8931, an equipotent, reversible inhibitor of signaling by epidermal growth factor receptor, ERBB2 (HER2), and ERBB3: a unique agent for simultaneous ERBB receptor blockade in cancer.

Hickinson DM, Klinowska T, Speake G, Vincent J, Trigwell C, Anderton J, Beck S, Marshall G, Davenport S, Callis R, Mills E, Grosios K, Smith P, Barlaam B, Wilkinson RW, Ogilvie D.

Clin Cancer Res. 2010 Feb 15;16(4):1159-69. doi: 10.1158/1078-0432.CCR-09-2353. Epub 2010 Feb 9.

8.

Neutral 5-substituted 4-indazolylaminoquinazolines as potent, orally active inhibitors of erbB2 receptor tyrosine kinase.

Barlaam B, Acton DG, Ballard P, Bradbury RH, Cross D, Ducray R, Germain H, Hudson K, Klinowska T, Magnien F, Ogilvie DJ, Olivier A, Ross HS, Smith R, Trigwell CB, Vautier M, Wright L.

Bioorg Med Chem Lett. 2008 Mar 15;18(6):1799-803. doi: 10.1016/j.bmcl.2008.02.035. Epub 2008 Feb 16.

PMID:
18313293
9.

Novel 3-alkoxy-1H-pyrazolo[3,4-d]pyrimidines as EGFR and erbB2 receptor tyrosine kinase inhibitors.

Ducray R, Ballard P, Barlaam BC, Hickinson MD, Kettle JG, Ogilvie DJ, Trigwell CB.

Bioorg Med Chem Lett. 2008 Feb 1;18(3):959-62. doi: 10.1016/j.bmcl.2007.12.035. Epub 2007 Dec 23.

PMID:
18182285
10.

A new series of neutral 5-substituted 4-anilinoquinazolines as potent, orally active inhibitors of erbB2 receptor tyrosine kinase.

Barlaam B, Ballard P, Bradbury RH, Ducray R, Germain H, Hickinson DM, Hudson K, Kettle JG, Klinowska T, Magnien F, Ogilvie DJ, Olivier A, Pearson SE, Scott JS, Suleman A, Trigwell CB, Vautier M, Whittaker RD, Wood R.

Bioorg Med Chem Lett. 2008 Jan 15;18(2):674-8. Epub 2007 Nov 21.

PMID:
18061446

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