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Items: 14


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.


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.


AZD9496: An Oral Estrogen Receptor Inhibitor That Blocks the Growth of ER-Positive and ESR1-Mutant Breast Tumors in Preclinical Models.

Weir HM, Bradbury RH, Lawson M, Rabow AA, Buttar D, Callis RJ, Curwen JO, de Almeida C, Ballard P, Hulse M, Donald CS, Feron LJ, Karoutchi G, MacFaul P, Moss T, Norman RA, Pearson SE, Tonge M, Davies G, Walker GE, Wilson Z, Rowlinson R, Powell S, Sadler C, Richmond G, Ladd B, Pazolli E, Mazzola AM, D'Cruz C, De Savi C.

Cancer Res. 2016 Jun 1;76(11):3307-18. doi: 10.1158/0008-5472.CAN-15-2357. Epub 2016 Mar 28.


In vitro pharmacological profiling of R406 identifies molecular targets underlying the clinical effects of fostamatinib.

Rolf MG, Curwen JO, Veldman-Jones M, Eberlein C, Wang J, Harmer A, Hellawell CJ, Braddock M.

Pharmacol Res Perspect. 2015 Oct;3(5):e00175. doi: 10.1002/prp2.175. Epub 2015 Sep 4.


Optimization of a Novel Binding Motif to (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic Acid (AZD9496), a Potent and Orally Bioavailable Selective Estrogen Receptor Downregulator and Antagonist.

De Savi C, Bradbury RH, Rabow AA, Norman RA, de Almeida C, Andrews DM, Ballard P, Buttar D, Callis RJ, Currie GS, Curwen JO, Davies CD, Donald CS, Feron LJ, Gingell H, Glossop SC, Hayter BR, Hussain S, Karoutchi G, Lamont SG, MacFaul P, Moss TA, Pearson SE, Tonge M, Walker GE, Weir HM, Wilson Z.

J Med Chem. 2015 Oct 22;58(20):8128-40. doi: 10.1021/acs.jmedchem.5b00984. Epub 2015 Oct 7.


The contribution of VEGF signalling to fostamatinib-induced blood pressure elevation.

Skinner M, Philp K, Lengel D, Coverley L, Lamm Bergström E, Glaves P, Musgrove H, Prior H, Braddock M, Huby R, Curwen JO, Duffy P, Harmer AR.

Br J Pharmacol. 2014 May;171(9):2308-20. doi: 10.1111/bph.12559.


The use and refinement of rodent models in anti-cancer drug discovery: a review.

Curwen JO, Wedge SR.

Altern Lab Anim. 2009 Apr;37(2):173-80. Review.


Effect of pretreatment with atenolol and nifedipine on ZD6126-induced cardiac toxicity in rats.

Gould S, Westwood FR, Curwen JO, Ashton SE, Roberts DW, Lovick SC, Ryan AJ.

J Natl Cancer Inst. 2007 Nov 21;99(22):1724-8. Epub 2007 Nov 13.


AZD2171: a highly potent, orally bioavailable, vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor for the treatment of cancer.

Wedge SR, Kendrew J, Hennequin LF, Valentine PJ, Barry ST, Brave SR, Smith NR, James NH, Dukes M, Curwen JO, Chester R, Jackson JA, Boffey SJ, Kilburn LL, Barnett S, Richmond GH, Wadsworth PF, Walker M, Bigley AL, Taylor ST, Cooper L, Beck S, Jürgensmeier JM, Ogilvie DJ.

Cancer Res. 2005 May 15;65(10):4389-400.


ZD6474 inhibits vascular endothelial growth factor signaling, angiogenesis, and tumor growth following oral administration.

Wedge SR, Ogilvie DJ, Dukes M, Kendrew J, Chester R, Jackson JA, Boffey SJ, Valentine PJ, Curwen JO, Musgrove HL, Graham GA, Hughes GD, Thomas AP, Stokes ES, Curry B, Richmond GH, Wadsworth PF, Bigley AL, Hennequin LF.

Cancer Res. 2002 Aug 15;62(16):4645-55.


Novel 4-anilinoquinazolines with C-7 basic side chains: design and structure activity relationship of a series of potent, orally active, VEGF receptor tyrosine kinase inhibitors.

Hennequin LF, Stokes ES, Thomas AP, Johnstone C, Plé PA, Ogilvie DJ, Dukes M, Wedge SR, Kendrew J, Curwen JO.

J Med Chem. 2002 Mar 14;45(6):1300-12.


ZD4190: an orally active inhibitor of vascular endothelial growth factor signaling with broad-spectrum antitumor efficacy.

Wedge SR, Ogilvie DJ, Dukes M, Kendrew J, Curwen JO, Hennequin LF, Thomas AP, Stokes ES, Curry B, Richmond GH, Wadsworth PF.

Cancer Res. 2000 Feb 15;60(4):970-5.


Design and structure-activity relationship of a new class of potent VEGF receptor tyrosine kinase inhibitors.

Hennequin LF, Thomas AP, Johnstone C, Stokes ES, Plé PA, Lohmann JJ, Ogilvie DJ, Dukes M, Wedge SR, Curwen JO, Kendrew J, Lambert-van der Brempt C.

J Med Chem. 1999 Dec 30;42(26):5369-89.


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