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Items: 1 to 50 of 69

1.

A fragment-based approach applied to a highly flexible target: Insights and challenges towards the inhibition of HSP70 isoforms.

Jones AM, Westwood IM, Osborne JD, Matthews TP, Cheeseman MD, Rowlands MG, Jeganathan F, Burke R, Lee D, Kadi N, Liu M, Richards M, McAndrew C, Yahya N, Dobson SE, Jones K, Workman P, Collins I, van Montfort RL.

Sci Rep. 2016 Oct 6;6:34701. doi: 10.1038/srep34701.

2.

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
3.

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.

4.

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
5.

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
6.

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
7.

Synthesis of isothiazol-3-one derivatives as inhibitors of histone acetyltransferases (HATs).

Gorsuch S, Bavetsias V, Rowlands MG, Aherne GW, Workman P, Jarman M, McDonald E.

Bioorg Med Chem. 2009 Jan 15;17(2):467-74. doi: 10.1016/j.bmc.2008.11.079. Epub 2008 Dec 7.

PMID:
19101154
8.

Identification of 4-(4-aminopiperidin-1-yl)-7H-pyrrolo[2,3-d]pyrimidines as selective inhibitors of protein kinase B through fragment elaboration.

Caldwell JJ, Davies TG, Donald A, McHardy T, Rowlands MG, Aherne GW, Hunter LK, Taylor K, Ruddle R, Raynaud FI, Verdonk M, Workman P, Garrett MD, Collins I.

J Med Chem. 2008 Apr 10;51(7):2147-57. doi: 10.1021/jm701437d. Epub 2008 Mar 18.

PMID:
18345609
9.

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
10.

Rapid evolution of 6-phenylpurine inhibitors of protein kinase B through structure-based design.

Donald A, McHardy T, Rowlands MG, Hunter LJ, Davies TG, Berdini V, Boyle RG, Aherne GW, Garrett MD, Collins I.

J Med Chem. 2007 May 17;50(10):2289-92. Epub 2007 Apr 24.

PMID:
17451235
11.

Calmodulin-independent, agonistic properties of a peptide containing the calmodulin binding site of estrogen receptor alpha.

Gallo D, Jacquemotte F, Cleeren A, Laïos I, Hadiy S, Rowlands MG, Caille O, Nonclercq D, Laurent G, Jacquot Y, Leclercq G.

Mol Cell Endocrinol. 2007 Mar 30;268(1-2):37-49. Epub 2007 Jan 25.

PMID:
17316976
12.

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
13.

Structure-based design of isoquinoline-5-sulfonamide inhibitors of protein kinase B.

Collins I, Caldwell J, Fonseca T, Donald A, Bavetsias V, Hunter LJ, Garrett MD, Rowlands MG, Aherne GW, Davies TG, Berdini V, Woodhead SJ, Davis D, Seavers LC, Wyatt PG, Workman P, McDonald E.

Bioorg Med Chem. 2006 Feb 15;14(4):1255-73. Epub 2005 Oct 24.

PMID:
16249095
14.

Isothiazolones as inhibitors of PCAF and p300 histone acetyltransferase activity.

Stimson L, Rowlands MG, Newbatt YM, Smith NF, Raynaud FI, Rogers P, Bavetsias V, Gorsuch S, Jarman M, Bannister A, Kouzarides T, McDonald E, Workman P, Aherne GW.

Mol Cancer Ther. 2005 Oct;4(10):1521-32.

15.

The identification, synthesis, protein crystal structure and in vitro biochemical evaluation of a new 3,4-diarylpyrazole class of Hsp90 inhibitors.

Cheung KM, Matthews TP, James K, Rowlands MG, Boxall KJ, Sharp SY, Maloney A, Roe SM, Prodromou C, Pearl LH, Aherne GW, McDonald E, Workman P.

Bioorg Med Chem Lett. 2005 Jul 15;15(14):3338-43.

PMID:
15955698
16.

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
17.

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
18.
19.

Assays for the identification and evaluation of histone acetyltransferase inhibitors.

Wynne Aherne G, Rowlands MG, Stimson L, Workman P.

Methods. 2002 Mar;26(3):245-53.

PMID:
12054880
20.

Solid-phase synthesis of novel inhibitors of farnesyl transferase.

Barber AM, Hardcastle IR, Rowlands MG, Nutley BP, Marriott JH, Jarman M.

Bioorg Med Chem Lett. 1999 Feb 22;9(4):623-6.

PMID:
10098677
21.

Inhibition of protein prenylation by metabolites of limonene.

Hardcastle IR, Rowlands MG, Barber AM, Grimshaw RM, Mohan MK, Nutley BP, Jarman M.

Biochem Pharmacol. 1999 Apr 1;57(7):801-9.

PMID:
10075086
22.

Comparison of biochemical aromatase activity with aromatase immunohistochemistry in human breast carcinomas.

Shenton KC, Dowsett M, Lu Q, Brodie A, Sasano H, Sacks NP, Rowlands MG.

Breast Cancer Res Treat. 1998;49 Suppl 1:S101-7; discussion S109-19.

PMID:
9797024
23.

Antagonism of estrogen receptor and calmodulin association by antiestrogens is not dependent on an interaction with calmodulin.

Rowlands MG, Grimshaw R, Jarman M, Bouhoute A, Leclercq G.

Biochem Pharmacol. 1997 Jan 24;53(2):241-4.

PMID:
9037257
24.
25.

Identification and characterization of limonene metabolites in patients with advanced cancer by liquid chromatography/mass spectrometry.

Poon GK, Vigushin D, Griggs LJ, Rowlands MG, Coombes RC, Jarman M.

Drug Metab Dispos. 1996 May;24(5):565-71.

PMID:
8723738
26.

Homologs of idoxifene: variation of estrogen receptor binding and calmodulin antagonism with chain length.

Hardcastle IR, Rowlands MG, Grimshaw RM, Houghton J, Jarman M.

J Med Chem. 1996 Feb 16;39(4):999-1004.

PMID:
8632423
27.

Esters of 3-pyridylacetic acid that combine potent inhibition of 17 alpha-hydroxylase/C17,20-lyase (cytochrome P45017 alpha) with resistance to esterase hydrolysis.

Rowlands MG, Barrie SE, Chan F, Houghton J, Jarman M, McCague R, Potter GA.

J Med Chem. 1995 Oct 13;38(21):4191-7.

PMID:
7473546
28.

Inhibition of aromatase expression by a psoralen-linked triplex-forming oligonucleotide targeted to a coding sequence.

Macaulay VM, Bates PJ, McLean MJ, Rowlands MG, Jenkins TC, Ashworth A, Neidle S.

FEBS Lett. 1995 Sep 25;372(2-3):222-8.

29.

Comparison between inhibition of protein kinase C and antagonism of calmodulin by tamoxifen analogues.

Rowlands MG, Budworth J, Jarman M, Hardcastle IR, McCague R, Gescher A.

Biochem Pharmacol. 1995 Aug 25;50(5):723-6.

PMID:
7669076
30.
31.

The deuterium isotope effect for the alpha-hydroxylation of tamoxifen by rat liver microsomes accounts for the reduced genotoxicity of [D5-ethyl]tamoxifen.

Jarman M, Poon GK, Rowlands MG, Grimshaw RM, Horton MN, Potter GA, McCague R.

Carcinogenesis. 1995 Apr;16(4):683-8.

PMID:
7728943
32.

Rationally designed analogues of tamoxifen with improved calmodulin antagonism.

Hardcastle IR, Rowlands MG, Houghton J, Parr IB, Potter GA, Jarman M, Edwards KJ, Laughton CA, Trent JO, Neidle S.

J Med Chem. 1995 Jan 20;38(2):241-8.

PMID:
7830266
33.
34.
35.

Lack of inhibition of placental estrone sulfatase and aromatase enzymes by vitamin D3 and its analogs.

Evans TR, Rowlands MG, Sahota SS, Coombes RC.

J Steroid Biochem Mol Biol. 1994 Apr;48(5-6):563-6.

PMID:
8180120
36.

Intratumoral oestrone sulphatase activity as a prognostic marker in human breast carcinoma.

Evans TR, Rowlands MG, Law M, Coombes RC.

Br J Cancer. 1994 Mar;69(3):555-61.

37.

Biological effects of stable overexpression of aromatase in human hormone-dependent breast cancer cells.

Macaulay VM, Nicholls JE, Gledhill J, Rowlands MG, Dowsett M, Ashworth A.

Br J Cancer. 1994 Jan;69(1):77-83.

38.

Evaluation of some 4-fluoro- and 4-cyano derivatives of delta 4,3-ketosteroids as inhibitors of testosterone 5 alpha-reductase.

Jarman M, Barrie SE, Houghton J, Rowlands MG, Mann J, Haase-Held M, Hatzis M.

J Enzyme Inhib. 1994;8(1):17-23.

PMID:
7539066
39.

Analysis of phase I and phase II metabolites of tamoxifen in breast cancer patients.

Poon GK, Chui YC, McCague R, Lłnning PE, Feng R, Rowlands MG, Jarman M.

Drug Metab Dispos. 1993 Nov-Dec;21(6):1119-24.

PMID:
7905393
40.

Detection of breast cancer-associated estrone sulfatase in breast cancer biopsies and cell lines using polymerase chain reaction.

Evans TR, Rowlands MG, Luqmani YA, Chander SK, Coombes RC.

J Steroid Biochem Mol Biol. 1993 Aug;46(2):195-201.

PMID:
8664167
41.

Prognostic significance of aromatase and estrone sulfatase enzymes in human breast cancer.

Evans TR, Rowlands MG, Silva MC, Law M, Coombes RC.

J Steroid Biochem Mol Biol. 1993 Mar;44(4-6):583-7.

PMID:
8476770
42.

New endocrine agents for the treatment of breast cancer.

Coombes RC, Jarman M, Dowsett M, Chander SK, Rowlands MG, Di Salle E, Evans TJ.

Recent Results Cancer Res. 1993;127:267-75. Review. No abstract available.

PMID:
8502825
43.

Investigation of conjugated metabolites of 4-hydroxyandrost-4-ene-3,17-dione in patient urine by liquid chromatography-atmospheric pressure ionization mass spectrometry.

Poon GK, Chui YC, Jarman M, Rowlands MG, Kokkonen PS, Niessen WM, van der Greef J.

Drug Metab Dispos. 1992 Nov-Dec;20(6):941-7.

PMID:
1362950
45.

Oestrone sulphatase activity in mammary tumours and the liver of N-nitrosomethylurea treated rats.

Evans TR, Chander SK, Rowlands MG, Coombes RC.

Br J Cancer. 1992 Jan;65(1):72-6.

46.

Effects of 4-hydroxyandrost-4-ene-3,17-dione and its metabolites on 5 alpha-reductase activity and the androgen receptor.

Davies JH, Shearer RJ, Rowlands MG, Poon GK, Houghton J, Jarman M, Dowsett M.

J Enzyme Inhib. 1992;6(2):141-7.

PMID:
1284430
47.

Inhibition of estrone sulfatase enzyme in human placenta and human breast carcinoma.

Evans TR, Rowlands MG, Jarman M, Coombes RC.

J Steroid Biochem Mol Biol. 1991 Oct;39(4A):493-9.

PMID:
1911438
48.
49.

Comparison of aromatase activity in human prostatic, testicular and placental tissues.

Rowlands MG, Davies JH, Shearer RJ, Dowsett M.

J Enzyme Inhib. 1991;4(4):307-13.

PMID:
1727017
50.

Inhibition of enzymes of estrogen and androgen biosynthesis by esters of 4-pyridylacetic acid.

McCague R, Rowlands MG, Barrie SE, Houghton J.

J Med Chem. 1990 Nov;33(11):3050-5.

PMID:
2231604

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