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Items: 1 to 50 of 104

1.

Correction: In vitro Biological Characterization of a Novel, Synthetic Diaryl Pyrazole Resorcinol Class of Heat Shock Protein 90 Inhibitors.

Sharp SY, Boxall K, Rowlands M, Prodromou C, Roe SM, Maloney A, Powers M, Clarke PA, Box G, Sanderson S, Patterson L, Matthews TP, Cheung KJ, Ball K, Hayes A, Raynaud F, Marais R, Pearl L, Eccles S, Aherne W, McDonald E, Workman P.

Cancer Res. 2019 Jan 1;79(1):287. doi: 10.1158/0008-5472.CAN-18-3578. No abstract available.

PMID:
30602624
2.

Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.

Mallinger A, Crumpler S, Pichowicz M, Waalboer D, Stubbs M, Adeniji-Popoola O, Wood B, Smith E, Thai C, Henley AT, Georgi K, Court W, Hobbs S, Box G, Ortiz-Ruiz MJ, Valenti M, De Haven Brandon A, TePoele R, Leuthner B, Workman P, Aherne W, Poeschke O, Dale T, Wienke D, Esdar C, Rohdich F, Raynaud F, Clarke PA, Eccles SA, Stieber F, Schiemann K, Blagg J.

J Med Chem. 2015 Feb 26;58(4):1717-35. doi: 10.1021/jm501436m. Epub 2015 Feb 13.

3.

Small-molecule inhibitors of the protein methyltransferase SET7/9 identified in a high-throughput screen.

Francis NJ, Rowlands M, Workman P, Jones K, Aherne W.

J Biomol Screen. 2012 Sep;17(8):1102-9. doi: 10.1177/1087057112452137. Epub 2012 Jul 5.

PMID:
22772057
4.

Mechanism-based screen establishes signalling framework for DNA damage-associated G1 checkpoint response.

Richardson E, Stockwell SR, Li H, Aherne W, Cuomo ME, Mittnacht S.

PLoS One. 2012;7(2):e31627. doi: 10.1371/journal.pone.0031627. Epub 2012 Feb 27.

5.

Targeting the Hsp90 molecular chaperone with novel macrolactams. Synthesis, structural, binding, and cellular studies.

Day JE, Sharp SY, Rowlands MG, Aherne W, Hayes A, Raynaud FI, Lewis W, Roe SM, Prodromou C, Pearl LH, Workman P, Moody CJ.

ACS Chem Biol. 2011 Dec 16;6(12):1339-47. doi: 10.1021/cb200196e. Epub 2011 Oct 4.

PMID:
21932796
6.

Structure of the Ire1 autophosphorylation complex and implications for the unfolded protein response.

Ali MM, Bagratuni T, Davenport EL, Nowak PR, Silva-Santisteban MC, Hardcastle A, McAndrews C, Rowlands MG, Morgan GJ, Aherne W, Collins I, Davies FE, Pearl LH.

EMBO J. 2011 Mar 2;30(5):894-905. doi: 10.1038/emboj.2011.18. Epub 2011 Feb 11.

7.

A phase I study of the heat shock protein 90 inhibitor alvespimycin (17-DMAG) given intravenously to patients with advanced solid tumors.

Pacey S, Wilson RH, Walton M, Eatock MM, Hardcastle A, Zetterlund A, Arkenau HT, Moreno-Farre J, Banerji U, Roels B, Peachey H, Aherne W, de Bono JS, Raynaud F, Workman P, Judson I.

Clin Cancer Res. 2011 Mar 15;17(6):1561-70. doi: 10.1158/1078-0432.CCR-10-1927. Epub 2011 Jan 28. Erratum in: Clin Cancer Res. 2018 Nov 1;24(21):5488.

8.

CCT241533 is a potent and selective inhibitor of CHK2 that potentiates the cytotoxicity of PARP inhibitors.

Anderson VE, Walton MI, Eve PD, Boxall KJ, Antoni L, Caldwell JJ, Aherne W, Pearl LH, Oliver AW, Collins I, Garrett MD.

Cancer Res. 2011 Jan 15;71(2):463-72. doi: 10.1158/0008-5472.CAN-10-1252.

9.

Preclinical pharmacology, antitumor activity, and development of pharmacodynamic markers for the novel, potent AKT inhibitor CCT128930.

Yap TA, Walton MI, Hunter LJ, Valenti M, de Haven Brandon A, Eve PD, Ruddle R, Heaton SP, Henley A, Pickard L, Vijayaraghavan G, Caldwell JJ, Thompson NT, Aherne W, Raynaud FI, Eccles SA, Workman P, Collins I, Garrett MD.

Mol Cancer Ther. 2011 Feb;10(2):360-71. doi: 10.1158/1535-7163.MCT-10-0760. Epub 2010 Dec 29.

10.

Serum angiogenic profile of patients with glioblastoma identifies distinct tumor subtypes and shows that TIMP-1 is a prognostic factor.

Crocker M, Ashley S, Giddings I, Petrik V, Hardcastle A, Aherne W, Pearson A, Bell BA, Zacharoulis S, Papadopoulos MC.

Neuro Oncol. 2011 Jan;13(1):99-108. doi: 10.1093/neuonc/noq170. Epub 2010 Dec 16.

11.

Discovery of 2-(6-{[(6-fluoroquinolin-2-yl)methyl]amino}bicyclo[3.1.0]hex-3-yl)-N-hydroxypyrimidine-5-carboxamide (CHR-3996), a class I selective orally active histone deacetylase inhibitor.

Moffat D, Patel S, Day F, Belfield A, Donald A, Rowlands M, Wibawa J, Brotherton D, Stimson L, Clark V, Owen J, Bawden L, Box G, Bone E, Mortenson P, Hardcastle A, van Meurs S, Eccles S, Raynaud F, Aherne W.

J Med Chem. 2010 Dec 23;53(24):8663-78. doi: 10.1021/jm101177s. Epub 2010 Nov 16.

PMID:
21080647
12.

Design and synthesis of novel pyrimidine hydroxamic acid inhibitors of histone deacetylases.

Donald AD, Clark VL, Patel S, Day FA, Rowlands MG, Wibata J, Stimson L, Hardcastle A, Eccles SA, McNamara D, Needham LA, Raynaud FI, Aherne W, Moffat DF.

Bioorg Med Chem Lett. 2010 Nov 15;20(22):6657-60. doi: 10.1016/j.bmcl.2010.09.016. Epub 2010 Sep 21.

PMID:
20884208
13.

Identification by high-throughput screening of viridin analogs as biochemical and cell-based inhibitors of the cell cycle-regulated nek2 kinase.

Hayward DG, Newbatt Y, Pickard L, Byrne E, Mao G, Burns S, Sahota NK, Workman P, Collins I, Aherne W, Fry AM.

J Biomol Screen. 2010 Sep;15(8):918-927. doi: 10.1177/1087057110376537. Epub 2010 Jul 27.

14.

Inhibition of Hsp90 with resorcylic acid macrolactones: synthesis and binding studies.

Day JE, Sharp SY, Rowlands MG, Aherne W, Lewis W, Roe SM, Prodromou C, Pearl LH, Workman P, Moody CJ.

Chemistry. 2010 Sep 10;16(34):10366-72. doi: 10.1002/chem.201001119.

PMID:
20661961
15.

A useful approach to identify novel small-molecule inhibitors of Wnt-dependent transcription.

Ewan K, Pajak B, Stubbs M, Todd H, Barbeau O, Quevedo C, Botfield H, Young R, Ruddle R, Samuel L, Battersby A, Raynaud F, Allen N, Wilson S, Latinkic B, Workman P, McDonald E, Blagg J, Aherne W, Dale T.

Cancer Res. 2010 Jul 15;70(14):5963-73. doi: 10.1158/0008-5472.CAN-10-1028. Epub 2010 Jul 7.

16.

Detection of the ATPase activity of the molecular chaperones Hsp90 and Hsp72 using the TranscreenerTM ADP assay kit.

Rowlands M, McAndrew C, Prodromou C, Pearl L, Kalusa A, Jones K, Workman P, Aherne W.

J Biomol Screen. 2010 Mar;15(3):279-86. doi: 10.1177/1087057109360253. Epub 2010 Feb 10.

PMID:
20147598
17.

Targeting the Hsp90 chaperone: synthesis of novel resorcylic acid macrolactone inhibitors of Hsp90.

Day JE, Sharp SY, Rowlands MG, Aherne W, Workman P, Moody CJ.

Chemistry. 2010 Mar 1;16(9):2758-63. doi: 10.1002/chem.200902766.

PMID:
20087915
18.

Phase I pharmacokinetic and pharmacodynamic study of LAQ824, a hydroxamate histone deacetylase inhibitor with a heat shock protein-90 inhibitory profile, in patients with advanced solid tumors.

de Bono JS, Kristeleit R, Tolcher A, Fong P, Pacey S, Karavasilis V, Mita M, Shaw H, Workman P, Kaye S, Rowinsky EK, Aherne W, Atadja P, Scott JW, Patnaik A.

Clin Cancer Res. 2008 Oct 15;14(20):6663-73. doi: 10.1158/1078-0432.CCR-08-0376.

19.

NVP-AUY922: a novel heat shock protein 90 inhibitor active against xenograft tumor growth, angiogenesis, and metastasis.

Eccles SA, Massey A, Raynaud FI, Sharp SY, Box G, Valenti M, Patterson L, de Haven Brandon A, Gowan S, Boxall F, Aherne W, Rowlands M, Hayes A, Martins V, Urban F, Boxall K, Prodromou C, Pearl L, James K, Matthews TP, Cheung KM, Kalusa A, Jones K, McDonald E, Barril X, Brough PA, Cansfield JE, Dymock B, Drysdale MJ, Finch H, Howes R, Hubbard RE, Surgenor A, Webb P, Wood M, Wright L, Workman P.

Cancer Res. 2008 Apr 15;68(8):2850-60. doi: 10.1158/0008-5472.CAN-07-5256.

20.

Noninvasive magnetic resonance spectroscopic pharmacodynamic markers of a novel histone deacetylase inhibitor, LAQ824, in human colon carcinoma cells and xenografts.

Chung YL, Troy H, Kristeleit R, Aherne W, Jackson LE, Atadja P, Griffiths JR, Judson IR, Workman P, Leach MO, Beloueche-Babari M.

Neoplasia. 2008 Apr;10(4):303-13.

21.

4,5-diarylisoxazole Hsp90 chaperone inhibitors: potential therapeutic agents for the treatment of cancer.

Brough PA, Aherne W, Barril X, Borgognoni J, Boxall K, Cansfield JE, Cheung KM, Collins I, Davies NG, Drysdale MJ, Dymock B, Eccles SA, Finch H, Fink A, Hayes A, Howes R, Hubbard RE, James K, Jordan AM, Lockie A, Martins V, Massey A, Matthews TP, McDonald E, Northfield CJ, Pearl LH, Prodromou C, Ray S, Raynaud FI, Roughley SD, Sharp SY, Surgenor A, Walmsley DL, Webb P, Wood M, Workman P, Wright L.

J Med Chem. 2008 Jan 24;51(2):196-218. Epub 2007 Nov 20.

PMID:
18020435
22.

A chemical inhibitor of PPM1D that selectively kills cells overexpressing PPM1D.

Rayter S, Elliott R, Travers J, Rowlands MG, Richardson TB, Boxall K, Jones K, Linardopoulos S, Workman P, Aherne W, Lord CJ, Ashworth A.

Oncogene. 2008 Feb 14;27(8):1036-44. Epub 2007 Aug 13.

PMID:
17700519
23.

Application of meso scale technology for the measurement of phosphoproteins in human tumor xenografts.

Gowan SM, Hardcastle A, Hallsworth AE, Valenti MR, Hunter LJ, de Haven Brandon AK, Garrett MD, Raynaud F, Workman P, Aherne W, Eccles SA.

Assay Drug Dev Technol. 2007 Jun;5(3):391-401.

PMID:
17638539
24.

Inhibition of the heat shock protein 90 molecular chaperone in vitro and in vivo by novel, synthetic, potent resorcinylic pyrazole/isoxazole amide analogues.

Sharp SY, Prodromou C, Boxall K, Powers MV, Holmes JL, Box G, Matthews TP, Cheung KM, Kalusa A, James K, Hayes A, Hardcastle A, Dymock B, Brough PA, Barril X, Cansfield JE, Wright L, Surgenor A, Foloppe N, Hubbard RE, Aherne W, Pearl L, Jones K, McDonald E, Raynaud F, Eccles S, Drysdale M, Workman P.

Mol Cancer Ther. 2007 Apr;6(4):1198-211.

25.

Gene and protein expression profiling of human ovarian cancer cells treated with the heat shock protein 90 inhibitor 17-allylamino-17-demethoxygeldanamycin.

Maloney A, Clarke PA, Naaby-Hansen S, Stein R, Koopman JO, Akpan A, Yang A, Zvelebil M, Cramer R, Stimson L, Aherne W, Banerji U, Judson I, Sharp S, Powers M, deBilly E, Salmons J, Walton M, Burlingame A, Waterfield M, Workman P.

Cancer Res. 2007 Apr 1;67(7):3239-53.

26.

The phosphoinositide-specific phospholipase C inhibitor U73122 (1-(6-((17beta-3-methoxyestra-1,3,5(10)-trien-17-yl)amino)hexyl)-1H-pyrrole-2,5-dione) spontaneously forms conjugates with common components of cell culture medium.

Wilsher NE, Court WJ, Ruddle R, Newbatt YM, Aherne W, Sheldrake PW, Jones NP, Katan M, Eccles SA, Raynaud FI.

Drug Metab Dispos. 2007 Jul;35(7):1017-22. Epub 2007 Apr 2.

PMID:
17403917
27.

A duplexed phenotypic screen for the simultaneous detection of inhibitors of the molecular chaperone heat shock protein 90 and modulators of cellular acetylation.

Hardcastle A, Tomlin P, Norris C, Richards J, Cordwell M, Boxall K, Rowlands M, Jones K, Collins I, McDonald E, Workman P, Aherne W.

Mol Cancer Ther. 2007 Mar;6(3):1112-22.

28.

In vitro biological characterization of a novel, synthetic diaryl pyrazole resorcinol class of heat shock protein 90 inhibitors.

Sharp SY, Boxall K, Rowlands M, Prodromou C, Roe SM, Maloney A, Powers M, Clarke PA, Box G, Sanderson S, Patterson L, Matthews TP, Cheung KM, Ball K, Hayes A, Raynaud F, Marais R, Pearl L, Eccles S, Aherne W, McDonald E, Workman P.

Cancer Res. 2007 Mar 1;67(5):2206-16. Erratum in: Cancer Res. 2019 Jan 1;79(1):287.

29.

Identification of novel keratinocyte differentiation modulating compounds by high-throughput screening.

Honma M, Stubbs M, Collins I, Workman P, Aherne W, Watt FM.

J Biomol Screen. 2006 Dec;11(8):977-84. Epub 2006 Nov 7.

PMID:
17092913
30.

A prospective, blinded analysis of thymidylate synthase and p53 expression as prognostic markers in the adjuvant treatment of colorectal cancer.

Popat S, Chen Z, Zhao D, Pan H, Hearle N, Chandler I, Shao Y, Aherne W, Houlston R.

Ann Oncol. 2006 Dec;17(12):1810-7. Epub 2006 Sep 13.

PMID:
16971666
31.

Identification of small-molecule inhibitors of protein kinase B (PKB/AKT) in an AlphaScreenTM high-throughput screen.

Burns S, Travers J, Collins I, Rowlands MG, Newbatt Y, Thompson N, Garrett MD, Workman P, Aherne W.

J Biomol Screen. 2006 Oct;11(7):822-7. Epub 2006 Aug 10.

PMID:
16902245
32.

Identification of inhibitors of the kinase activity of oncogenic V600E BRAF in an enzyme cascade high-throughput screen.

Newbatt Y, Burns S, Hayward R, Whittaker S, Kirk R, Marshall C, Springer C, McDonald E; Cancer Genome Project, Marais R, Workman P, Aherne W.

J Biomol Screen. 2006 Mar;11(2):145-54. Epub 2005 Dec 16.

PMID:
16361694
33.

A Phase I study of the angiogenesis inhibitor SU5416 (semaxanib) in solid tumours, incorporating dynamic contrast MR pharmacodynamic end points.

O'Donnell A, Padhani A, Hayes C, Kakkar AJ, Leach M, Trigo JM, Scurr M, Raynaud F, Phillips S, Aherne W, Hardcastle A, Workman P, Hannah A, Judson I.

Br J Cancer. 2005 Oct 17;93(8):876-83.

34.

A phase I pharmacokinetic and pharmacodynamic study of BGC9331 and carboplatin in relapsed gynaecological malignancies.

Benepal T, Jackman A, Pyle L, Bate S, Hardcastle A, Aherne W, Mitchell F, Simmons L, Ruddle R, Raynaud F, Gore M.

Br J Cancer. 2005 Oct 17;93(8):868-75.

35.

Solid-phase immunoassays in mechanism-based drug discovery: their application in the development of inhibitors of the molecular chaperone heat-shock protein 90.

Hardcastle A, Boxall K, Richards J, Tomlin P, Sharp S, Clarke P, Workman P, Aherne W.

Assay Drug Dev Technol. 2005 Jun;3(3):273-85.

PMID:
15971989
37.

High-throughput screening assay for identification of small molecule inhibitors of Aurora2/STK15 kinase.

Sun C, Newbatt Y, Douglas L, Workman P, Aherne W, Linardopoulos S.

J Biomol Screen. 2004 Aug;9(5):391-7.

PMID:
15296638
38.

Structure-activity relationships in purine-based inhibitor binding to HSP90 isoforms.

Wright L, Barril X, Dymock B, Sheridan L, Surgenor A, Beswick M, Drysdale M, Collier A, Massey A, Davies N, Fink A, Fromont C, Aherne W, Boxall K, Sharp S, Workman P, Hubbard RE.

Chem Biol. 2004 Jun;11(6):775-85.

39.

Histone modification enzymes: novel targets for cancer drugs.

Kristeleit R, Stimson L, Workman P, Aherne W.

Expert Opin Emerg Drugs. 2004 May;9(1):135-54. Review.

PMID:
15155140
40.

High-throughput screening assay for inhibitors of heat-shock protein 90 ATPase activity.

Rowlands MG, Newbatt YM, Prodromou C, Pearl LH, Workman P, Aherne W.

Anal Biochem. 2004 Apr 15;327(2):176-83.

PMID:
15051534
41.

High-throughput screening for the identification of small-molecule inhibitors of retinoblastoma protein phosphorylation in cells.

Barrie SE, Eno-Amooquaye E, Hardcastle A, Platt G, Richards J, Bedford D, Workman P, Aherne W, Mittnacht S, Garrett MD.

Anal Biochem. 2003 Sep 1;320(1):66-74.

PMID:
12895470
42.

Assays for HSP90 and inhibitors.

Aherne W, Maloney A, Prodromou C, Rowlands MG, Hardcastle A, Boxall K, Clarke P, Walton MI, Pearl L, Workman P.

Methods Mol Med. 2003;85:149-61. Review. No abstract available.

PMID:
12710206
43.

A human capecitabine excretion balance and pharmacokinetic study after administration of a single oral dose of 14C-labelled drug.

Judson IR, Beale PJ, Trigo JM, Aherne W, Crompton T, Jones D, Bush E, Reigner B.

Invest New Drugs. 1999;17(1):49-56.

PMID:
10555122
44.

Vinblastine pharmacokinetics in patients with non-small cell lung cancer given cisplatin.

Links M, Watson S, Lethlean K, Aherne W, Kirsten F, Clarke S, Law M, Friedlander M, Galettis P, McKeage MJ.

Cancer Invest. 1999;17(7):479-85.

PMID:
10518192
45.

Metabolism, excretion and pharmacokinetics of a single dose of [14C]-raltitrexed in cancer patients.

Beale P, Judson I, Hanwell J, Berry C, Aherne W, Hickish T, Martin P, Walker M.

Cancer Chemother Pharmacol. 1998;42(1):71-6.

PMID:
9619761
46.

Interference by antifolate drugs in a folate competitive protein-binding assay.

Hardcastle A, Clarke S, Aherne W.

Cancer Chemother Pharmacol. 1997;39(6):552-3. No abstract available.

PMID:
9118469
47.

2'-Deoxycytidine kinase deficiency is a major determinant of 2-chloro-2'-deoxyadenosine resistance in lymphoid cell lines

Orr RM, Talbot DC, Aherne WG, Fisher TC, Serafinowski P, Harrap KR.

Clin Cancer Res. 1995 Apr;1(4):391-8.

48.

Development of an enzyme-linked immunosorbent assay for isoproturon in water.

Katmeh MF, Frost G, Aherne W, Stevenson D.

Analyst. 1994 Mar;119(3):431-5.

PMID:
8192230
49.

The measurement of deoxynucleotide (dNTP) pools by radioimmunoassay (RIA).

Aherne W, Hardcastle A, Kelland L, Jackman A.

Adv Exp Med Biol. 1994;370:801-4.

PMID:
7661027
50.

Histologic, pharmacologic, and immunocytochemical effects of injection of bleomycin into viral warts.

James MP, Collier PM, Aherne W, Hardcastle A, Lovegrove S.

J Am Acad Dermatol. 1993 Jun;28(6):933-7.

PMID:
7684410

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