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Items: 26


Molecular profiling and combinatorial activity of CCT068127: a potent CDK2 and CDK9 inhibitor.

Whittaker SR, Barlow C, Martin MP, Mancusi C, Wagner S, Self A, Barrie E, Te Poele R, Sharp S, Brown N, Wilson S, Jackson W, Fischer PM, Clarke PA, Walton MI, McDonald E, Blagg J, Noble M, Garrett MD, Workman P.

Mol Oncol. 2018 Mar;12(3):287-304. doi: 10.1002/1878-0261.12148. Epub 2018 Jan 28.


Discovery of a Chemical Probe Bisamide (CCT251236): An Orally Bioavailable Efficacious Pirin Ligand from a Heat Shock Transcription Factor 1 (HSF1) Phenotypic Screen.

Cheeseman MD, Chessum NE, Rye CS, Pasqua AE, Tucker MJ, Wilding B, Evans LE, Lepri S, Richards M, Sharp SY, Ali S, Rowlands M, O'Fee L, Miah A, Hayes A, Henley AT, Powers M, Te Poele R, De Billy E, Pellegrino L, Raynaud F, Burke R, van Montfort RL, Eccles SA, Workman P, Jones K.

J Med Chem. 2017 Jan 12;60(1):180-201. doi: 10.1021/acs.jmedchem.6b01055. Epub 2016 Dec 22.


Discovery of 4,6-disubstituted pyrimidines as potent inhibitors of the heat shock factor 1 (HSF1) stress pathway and CDK9.

Rye CS, Chessum NE, Lamont S, Pike KG, Faulder P, Demeritt J, Kemmitt P, Tucker J, Zani L, Cheeseman MD, Isaac R, Goodwin L, Boros J, Raynaud F, Hayes A, Henley AT, de Billy E, Lynch CJ, Sharp SY, Te Poele R, Fee LO, Foote KM, Green S, Workman P, Jones K.

Medchemcomm. 2016 Aug 1;7(8):1580-1586. Epub 2016 Jun 13.


AT13148 is a novel, oral multi-AGC kinase inhibitor with potent pharmacodynamic and antitumor activity.

Yap TA, Walton MI, Grimshaw KM, Te Poele RH, Eve PD, Valenti MR, de Haven Brandon AK, Martins V, Zetterlund A, Heaton SP, Heinzmann K, Jones PS, Feltell RE, Reule M, Woodhead SJ, Davies TG, Lyons JF, Raynaud FI, Eccles SA, Workman P, Thompson NT, Garrett MD.

Clin Cancer Res. 2012 Jul 15;18(14):3912-23. doi: 10.1158/1078-0432.CCR-11-3313. Epub 2012 Jul 10.


Mechanism-based screen for G1/S checkpoint activators identifies a selective activator of EIF2AK3/PERK signalling.

Stockwell SR, Platt G, Barrie SE, Zoumpoulidou G, Te Poele RH, Aherne GW, Wilson SC, Sheldrake P, McDonald E, Venet M, Soudy C, Elustondo F, Rigoreau L, Blagg J, Workman P, Garrett MD, Mittnacht S.

PLoS One. 2012;7(1):e28568. doi: 10.1371/journal.pone.0028568. Epub 2012 Jan 12.


Histone deacetylase inhibition increases levels of choline kinase α and phosphocholine facilitating noninvasive imaging in human cancers.

Beloueche-Babari M, Arunan V, Troy H, te Poele RH, te Fong AC, Jackson LE, Payne GS, Griffiths JR, Judson IR, Workman P, Leach MO, Chung YL.

Cancer Res. 2012 Feb 15;72(4):990-1000. doi: 10.1158/0008-5472.CAN-11-2688. Epub 2011 Dec 22.


Correlation of overall survival with gene expression profiles in a prospective study of resectable esophageal cancer.

Rao S, Welsh L, Cunningham D, te-Poele RH, Benson M, Norman A, Saffery C, Giddings I, Workman P, Clarke PA.

Clin Colorectal Cancer. 2011 Mar 1;10(1):48-56. doi: 10.3816/CCC.2011.n.007.


Molecular pharmacology of phosphatidylinositol 3-kinase inhibition in human glioma.

Guillard S, Clarke PA, Te Poele R, Mohri Z, Bjerke L, Valenti M, Raynaud F, Eccles SA, Workman P.

Cell Cycle. 2009 Feb 1;8(3):443-53. Epub 2009 Feb 16.


Mechanism of action of the Aurora kinase inhibitor CCT129202 and in vivo quantification of biological activity.

Chan F, Sun C, Perumal M, Nguyen QD, Bavetsias V, McDonald E, Martins V, Wilsher NE, Raynaud FI, Valenti M, Eccles S, Te Poele R, Workman P, Aboagye EO, Linardopoulos S.

Mol Cancer Ther. 2007 Dec;6(12 Pt 1):3147-57.


The cyclin-dependent kinase inhibitor seliciclib (R-roscovitine; CYC202) decreases the expression of mitotic control genes and prevents entry into mitosis.

Whittaker SR, Te Poele RH, Chan F, Linardopoulos S, Walton MI, Garrett MD, Workman P.

Cell Cycle. 2007 Dec 15;6(24):3114-31. Epub 2007 Oct 5.


AHR- and DNA-damage-mediated gene expression responses induced by benzo(a)pyrene in human cell lines.

Hockley SL, Arlt VM, Brewer D, Te Poele R, Workman P, Giddings I, Phillips DH.

Chem Res Toxicol. 2007 Dec;20(12):1797-810. Epub 2007 Oct 19.


Mechanisms of acquired resistance to 2-(4-Amino-3-methylphenyl)benzothiazole in breast cancer cell lines.

Bradshaw TD, Stone EL, Trapani V, Leong CO, Matthews CS, te Poele R, Stevens MF.

Breast Cancer Res Treat. 2008 Jul;110(1):57-68. Epub 2007 Aug 3.


Role of E2F3 expression in modulating cellular proliferation rate in human bladder and prostate cancer cells.

Olsson AY, Feber A, Edwards S, Te Poele R, Giddings I, Merson S, Cooper CS.

Oncogene. 2007 Feb 15;26(7):1028-37. Epub 2006 Aug 14.


Niacin induces PPARgamma expression and transcriptional activation in macrophages via HM74 and HM74a-mediated induction of prostaglandin synthesis pathways.

Knowles HJ, te Poele RH, Workman P, Harris AL.

Biochem Pharmacol. 2006 Feb 28;71(5):646-56. Epub 2006 Jan 18. Erratum in: Biochem Pharmacol. 2006 May 28;71(11):1662. Te Poole, Robert [corrected to te Poele, Robert H].


Pharmacokinetically guided phase I trial of topotecan and etoposide phosphate in recurrent ovarian cancer.

Levitt NC, Propper DJ, Madhusudan S, Braybrooke JP, Echeta C, Te Poele R, Davies SL, Flanagan E, Hickson ID, Joel S, Ganesan TS.

Br J Cancer. 2005 Jul 11;93(1):60-9.


Expression analysis onto microarrays of randomly selected cDNA clones highlights HOXB13 as a marker of human prostate cancer.

Edwards S, Campbell C, Flohr P, Shipley J, Giddings I, Te-Poele R, Dodson A, Foster C, Clark J, Jhavar S, Kovacs G, Cooper CS.

Br J Cancer. 2005 Jan 31;92(2):376-81.


Disruption of WT1 gene expression and exon 5 splicing following cytotoxic drug treatment: antisense down-regulation of exon 5 alters target gene expression and inhibits cell survival.

Renshaw J, Orr RM, Walton MI, Te Poele R, Williams RD, Wancewicz EV, Monia BP, Workman P, Pritchard-Jones K.

Mol Cancer Ther. 2004 Nov;3(11):1467-84.


Gene expression microarray technologies in the development of new therapeutic agents.

Clarke PA, te Poele R, Workman P.

Eur J Cancer. 2004 Nov;40(17):2560-91. Review.


Antigens up the nose: identification of putative biomarkers for nasal tolerance induction functional studies combined with proteomics.

Boots AM, Verhaert PD, te Poele RJ, Evers S, Coenen-de Roo CJ, Cleven J, Bos ES.

J Proteome Res. 2004 Sep-Oct;3(5):1056-62.


Cannabis-induced cytotoxicity in leukemic cell lines: the role of the cannabinoid receptors and the MAPK pathway.

Powles T, te Poele R, Shamash J, Chaplin T, Propper D, Joel S, Oliver T, Liu WM.

Blood. 2005 Feb 1;105(3):1214-21. Epub 2004 Sep 28.


DNA damage is able to induce senescence in tumor cells in vitro and in vivo.

te Poele RH, Okorokov AL, Jardine L, Cummings J, Joel SP.

Cancer Res. 2002 Mar 15;62(6):1876-83.


Gene expression microarray analysis in cancer biology, pharmacology, and drug development: progress and potential.

Clarke PA, te Poele R, Wooster R, Workman P.

Biochem Pharmacol. 2001 Nov 15;62(10):1311-36. Review.


Re: Loss of DNA mismatch repair: effects on the rate of mutation to drug resistance.

Liu WM, te Poele RH, Joel SP.

J Natl Cancer Inst. 1998 Feb 4;90(3):246-7. No abstract available.


An efficient system for active bovine pancreatic ribonuclease expression in Escherichia coli.

Okorokov AL, Panov KI, te Poele RH, Breukelman HJ, Furia A, Karpeisky MYa, Beintema JJ.

Protein Expr Purif. 1995 Aug;6(4):472-80.


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