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Items: 1 to 50 of 99

1.

5-(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology.

Beaufils F, Cmiljanovic N, Cmiljanovic V, Bohnacker T, Melone A, Marone R, Jackson E, Zhang X, Sele A, Borsari C, Mestan J, Hebeisen P, Hillmann P, Giese B, Zvelebil M, Fabbro D, Williams RL, Rageot D, Wymann MP.

J Med Chem. 2017 Sep 14;60(17):7524-7538. doi: 10.1021/acs.jmedchem.7b00930. Epub 2017 Sep 1.

2.

Deconvolution of Buparlisib's mechanism of action defines specific PI3K and tubulin inhibitors for therapeutic intervention.

Bohnacker T, Prota AE, Beaufils F, Burke JE, Melone A, Inglis AJ, Rageot D, Sele AM, Cmiljanovic V, Cmiljanovic N, Bargsten K, Aher A, Akhmanova A, Díaz JF, Fabbro D, Zvelebil M, Williams RL, Steinmetz MO, Wymann MP.

Nat Commun. 2017 Mar 9;8:14683. doi: 10.1038/ncomms14683.

3.

Cholesterol biosynthesis pathway as a novel mechanism of resistance to estrogen deprivation in estrogen receptor-positive breast cancer.

Simigdala N, Gao Q, Pancholi S, Roberg-Larsen H, Zvelebil M, Ribas R, Folkerd E, Thompson A, Bhamra A, Dowsett M, Martin LA.

Breast Cancer Res. 2016 Jun 1;18(1):58. doi: 10.1186/s13058-016-0713-5.

4.

Mouse mammary stem cells express prognostic markers for triple-negative breast cancer.

Soady KJ, Kendrick H, Gao Q, Tutt A, Zvelebil M, Ordonez LD, Quist J, Tan DW, Isacke CM, Grigoriadis A, Smalley MJ.

Breast Cancer Res. 2015 Mar 4;17:31. doi: 10.1186/s13058-015-0539-6.

5.

Effect of aromatase inhibition on functional gene modules in estrogen receptor-positive breast cancer and their relationship with antiproliferative response.

Gao Q, Patani N, Dunbier AK, Ghazoui Z, Zvelebil M, Martin LA, Dowsett M.

Clin Cancer Res. 2014 May 1;20(9):2485-94. doi: 10.1158/1078-0432.CCR-13-2602. Epub 2014 Mar 14.

6.

An in vivo functional screen identifies ST6GalNAc2 sialyltransferase as a breast cancer metastasis suppressor.

Murugaesu N, Iravani M, van Weverwijk A, Ivetic A, Johnson DA, Antonopoulos A, Fearns A, Jamal-Hanjani M, Sims D, Fenwick K, Mitsopoulos C, Gao Q, Orr N, Zvelebil M, Haslam SM, Dell A, Yarwood H, Lord CJ, Ashworth A, Isacke CM.

Cancer Discov. 2014 Mar;4(3):304-17. doi: 10.1158/2159-8290.CD-13-0287. Epub 2014 Feb 11.

7.

Deriving a mutation index of carcinogenicity using protein structure and protein interfaces.

Espinosa O, Mitsopoulos K, Hakas J, Pearl F, Zvelebil M.

PLoS One. 2014 Jan 15;9(1):e84598. doi: 10.1371/journal.pone.0084598. eCollection 2014.

8.

ROCK: a resource for integrative breast cancer data analysis.

Ur-Rehman S, Gao Q, Mitsopoulos C, Zvelebil M.

Breast Cancer Res Treat. 2013 Jun;139(3):907-21. doi: 10.1007/s10549-013-2593-z. Epub 2013 Jun 12.

PMID:
23756628
9.

GDNF-RET signaling in ER-positive breast cancers is a key determinant of response and resistance to aromatase inhibitors.

Morandi A, Martin LA, Gao Q, Pancholi S, Mackay A, Robertson D, Zvelebil M, Dowsett M, Plaza-Menacho I, Isacke CM.

Cancer Res. 2013 Jun 15;73(12):3783-95. doi: 10.1158/0008-5472.CAN-12-4265. Epub 2013 May 6.

10.

Neuregulin 3 and erbb signalling networks in embryonic mammary gland development.

Kogata N, Zvelebil M, Howard BA.

J Mammary Gland Biol Neoplasia. 2013 Jun;18(2):149-54. doi: 10.1007/s10911-013-9286-4. Epub 2013 May 7. Review.

PMID:
23649700
11.

Chemical development of intracellular protein heterodimerizers.

Erhart D, Zimmermann M, Jacques O, Wittwer MB, Ernst B, Constable E, Zvelebil M, Beaufils F, Wymann MP.

Chem Biol. 2013 Apr 18;20(4):549-57. doi: 10.1016/j.chembiol.2013.03.010.

12.

Embryonic mammary signature subsets are activated in Brca1-/- and basal-like breast cancers.

Zvelebil M, Oliemuller E, Gao Q, Wansbury O, Mackay A, Kendrick H, Smalley MJ, Reis-Filho JS, Howard BA.

Breast Cancer Res. 2013 Mar 18;15(2):R25. doi: 10.1186/bcr3403.

13.

Normalized mean glandular dose computation from mammography using GATE: a validation study.

Myronakis ME, Zvelebil M, Darambara DG.

Phys Med Biol. 2013 Apr 7;58(7):2247-65. doi: 10.1088/0031-9155/58/7/2247. Epub 2013 Mar 11.

PMID:
23475310
14.

Genome-wide association study identifies a common variant in RAD51B associated with male breast cancer risk.

Orr N, Lemnrau A, Cooke R, Fletcher O, Tomczyk K, Jones M, Johnson N, Lord CJ, Mitsopoulos C, Zvelebil M, McDade SS, Buck G, Blancher C; KConFab Consortium, Trainer AH, James PA, Bojesen SE, Bokmand S, Nevanlinna H, Mattson J, Friedman E, Laitman Y, Palli D, Masala G, Zanna I, Ottini L, Giannini G, Hollestelle A, Ouweland AM, Novaković S, Krajc M, Gago-Dominguez M, Castelao JE, Olsson H, Hedenfalk I, Easton DF, Pharoah PD, Dunning AM, Bishop DT, Neuhausen SL, Steele L, Houlston RS, Garcia-Closas M, Ashworth A, Swerdlow AJ.

Nat Genet. 2012 Nov;44(11):1182-4. doi: 10.1038/ng.2417. Epub 2012 Sep 23.

15.

Functional proteomic analysis of long-term growth factor stimulation and receptor tyrosine kinase coactivation in Swiss 3T3 fibroblasts.

Nagano K, Akpan A, Warnasuriya G, Corless S, Totty N, Yang A, Stein R, Zvelebil M, Stensballe A, Burlingame A, Waterfield M, Cramer R, Timms JF, Naaby-Hansen S.

Mol Cell Proteomics. 2012 Dec;11(12):1690-708. doi: 10.1074/mcp.M112.019778. Epub 2012 Sep 6.

16.

A gene expression and systems pathway analysis of the effects of clozapine compared to haloperidol in the mouse brain implicates susceptibility genes for schizophrenia.

Rizig MA, McQuillin A, Ng A, Robinson M, Harrison A, Zvelebil M, Hunt SP, Gurling HM.

J Psychopharmacol. 2012 Sep;26(9):1218-30. doi: 10.1177/0269881112450780. Epub 2012 Jul 5.

PMID:
22767372
17.

Genomic characterisation of acral melanoma cell lines.

Furney SJ, Turajlic S, Fenwick K, Lambros MB, MacKay A, Ricken G, Mitsopoulos C, Kozarewa I, Hakas J, Zvelebil M, Lord CJ, Ashworth A, Reis-Filho JS, Herlyn M, Murata H, Marais R.

Pigment Cell Melanoma Res. 2012 Jul;25(4):488-92. doi: 10.1111/j.1755-148X.2012.01016.x.

PMID:
22578220
18.

Genome-wide analysis of p63 binding sites identifies AP-2 factors as co-regulators of epidermal differentiation.

McDade SS, Henry AE, Pivato GP, Kozarewa I, Mitsopoulos C, Fenwick K, Assiotis I, Hakas J, Zvelebil M, Orr N, Lord CJ, Patel D, Ashworth A, McCance DJ.

Nucleic Acids Res. 2012 Aug;40(15):7190-206. doi: 10.1093/nar/gks389. Epub 2012 May 9.

19.

Ubiquitylation of the initiator caspase DREDD is required for innate immune signalling.

Meinander A, Runchel C, Tenev T, Chen L, Kim CH, Ribeiro PS, Broemer M, Leulier F, Zvelebil M, Silverman N, Meier P.

EMBO J. 2012 Jun 13;31(12):2770-83. doi: 10.1038/emboj.2012.121. Epub 2012 May 1.

20.

Whole genome in vivo RNAi screening identifies the leukemia inhibitory factor receptor as a novel breast tumor suppressor.

Iorns E, Ward TM, Dean S, Jegg A, Thomas D, Murugaesu N, Sims D, Mitsopoulos C, Fenwick K, Kozarewa I, Naceur-Lombarelli C, Zvelebil M, Isacke CM, Lord CJ, Ashworth A, Hnatyszyn HJ, Pegram M, Lippman M.

Breast Cancer Res Treat. 2012 Aug;135(1):79-91. doi: 10.1007/s10549-012-2068-7. Epub 2012 Apr 26.

PMID:
22535017
21.

CYP3A variation, premenopausal estrone levels, and breast cancer risk.

Johnson N, Walker K, Gibson LJ, Orr N, Folkerd E, Haynes B, Palles C, Coupland B, Schoemaker M, Jones M, Broderick P, Sawyer E, Kerin M, Tomlinson IP, Zvelebil M, Chilcott-Burns S, Tomczyk K, Simpson G, Williamson J, Hillier SG, Ross G, Houlston RS, Swerdlow A, Ashworth A, Dowsett M, Peto J, Dos Santos Silva I, Fletcher O.

J Natl Cancer Inst. 2012 May 2;104(9):657-69. doi: 10.1093/jnci/djs156. Epub 2012 Apr 3.

PMID:
22472546
22.

A modified method for whole exome resequencing from minimal amounts of starting DNA.

Kozarewa I, Rosa-Rosa JM, Wardell CP, Walker BA, Fenwick K, Assiotis I, Mitsopoulos C, Zvelebil M, Morgan GJ, Ashworth A, Lord CJ.

PLoS One. 2012;7(3):e32617. doi: 10.1371/journal.pone.0032617. Epub 2012 Mar 5. Erratum in: PLoS One. 2012;7(4): doi/10.1371/annotation/5b071c93-9fa8-4be6-9cbd-95aead146305. J, Christopher [corrected Lord, Christopher J].

23.

Whole genome sequencing of matched primary and metastatic acral melanomas.

Turajlic S, Furney SJ, Lambros MB, Mitsopoulos C, Kozarewa I, Geyer FC, Mackay A, Hakas J, Zvelebil M, Lord CJ, Ashworth A, Thomas M, Stamp G, Larkin J, Reis-Filho JS, Marais R.

Genome Res. 2012 Feb;22(2):196-207. doi: 10.1101/gr.125591.111. Epub 2011 Dec 19.

24.

The transcription factor Erg regulates expression of histone deacetylase 6 and multiple pathways involved in endothelial cell migration and angiogenesis.

Birdsey GM, Dryden NH, Shah AV, Hannah R, Hall MD, Haskard DO, Parsons M, Mason JC, Zvelebil M, Gottgens B, Ridley AJ, Randi AM.

Blood. 2012 Jan 19;119(3):894-903. doi: 10.1182/blood-2011-04-350025. Epub 2011 Nov 23.

25.

High-throughput RNA interference screening using pooled shRNA libraries and next generation sequencing.

Sims D, Mendes-Pereira AM, Frankum J, Burgess D, Cerone MA, Lombardelli C, Mitsopoulos C, Hakas J, Murugaesu N, Isacke CM, Fenwick K, Assiotis I, Kozarewa I, Zvelebil M, Ashworth A, Lord CJ.

Genome Biol. 2011 Oct 21;12(10):R104. doi: 10.1186/gb-2011-12-10-r104.

26.

Identification of a disease-defining gene fusion in epithelioid hemangioendothelioma.

Tanas MR, Sboner A, Oliveira AM, Erickson-Johnson MR, Hespelt J, Hanwright PJ, Flanagan J, Luo Y, Fenwick K, Natrajan R, Mitsopoulos C, Zvelebil M, Hoch BL, Weiss SW, Debiec-Rychter M, Sciot R, West RB, Lazar AJ, Ashworth A, Reis-Filho JS, Lord CJ, Gerstein MB, Rubin MA, Rubin BP.

Sci Transl Med. 2011 Aug 31;3(98):98ra82. doi: 10.1126/scitranslmed.3002409.

27.

Transcriptome analysis of embryonic mammary cells reveals insights into mammary lineage establishment.

Wansbury O, Mackay A, Kogata N, Mitsopoulos C, Kendrick H, Davidson K, Ruhrberg C, Reis-Filho JS, Smalley MJ, Zvelebil M, Howard BA.

Breast Cancer Res. 2011 Aug 11;13(4):R79. doi: 10.1186/bcr2928.

28.

Comprehensive genomic analysis of a BRCA2 deficient human pancreatic cancer.

Barber LJ, Rosa Rosa JM, Kozarewa I, Fenwick K, Assiotis I, Mitsopoulos C, Sims D, Hakas J, Zvelebil M, Lord CJ, Ashworth A.

PLoS One. 2011;6(7):e21639. doi: 10.1371/journal.pone.0021639. Epub 2011 Jul 5.

29.

Genome-wide functional screen identifies a compendium of genes affecting sensitivity to tamoxifen.

Mendes-Pereira AM, Sims D, Dexter T, Fenwick K, Assiotis I, Kozarewa I, Mitsopoulos C, Hakas J, Zvelebil M, Lord CJ, Ashworth A.

Proc Natl Acad Sci U S A. 2012 Feb 21;109(8):2730-5. doi: 10.1073/pnas.1018872108. Epub 2011 Apr 11.

30.

The FLIGHT Drosophila RNAi database: 2010 update.

Sims D, Bursteinas B, Jain E, Gao Q, Baum B, Zvelebil M.

Fly (Austin). 2010 Oct-Dec;4(4):344-8. doi: 10.4161/fly.4.4.13303. Epub 2010 Oct 1.

31.

Genomic distance entrained clustering and regression modelling highlights interacting genomic regions contributing to proliferation in breast cancer.

Dexter TJ, Sims D, Mitsopoulos C, Mackay A, Grigoriadis A, Ahmad AS, Zvelebil M.

BMC Syst Biol. 2010 Sep 8;4:127. doi: 10.1186/1752-0509-4-127.

32.

ROCK: a breast cancer functional genomics resource.

Sims D, Bursteinas B, Gao Q, Jain E, MacKay A, Mitsopoulos C, Zvelebil M.

Breast Cancer Res Treat. 2010 Nov;124(2):567-72. doi: 10.1007/s10549-010-0945-5. Epub 2010 Jun 20.

PMID:
20563840
33.

The vascular endothelial growth factor receptor inhibitor PTK787/ZK222584 inhibits aromatase.

Banerjee S, Zvelebil M, Furet P, Mueller-Vieira U, Evans DB, Dowsett M, Martin LA.

Cancer Res. 2009 Jun 1;69(11):4716-23. doi: 10.1158/0008-5472.CAN-08-4711. Epub 2009 May 12.

34.

PPM1D is a potential therapeutic target in ovarian clear cell carcinomas.

Tan DS, Lambros MB, Rayter S, Natrajan R, Vatcheva R, Gao Q, Marchiò C, Geyer FC, Savage K, Parry S, Fenwick K, Tamber N, Mackay A, Dexter T, Jameson C, McCluggage WG, Williams A, Graham A, Faratian D, El-Bahrawy M, Paige AJ, Gabra H, Gore ME, Zvelebil M, Lord CJ, Kaye SB, Ashworth A, Reis-Filho JS.

Clin Cancer Res. 2009 Apr 1;15(7):2269-80. doi: 10.1158/1078-0432.CCR-08-2403. Epub 2009 Mar 17.

35.

In Vitro and in Vivo Characterization of Molecular Interactions between Calmodulin, Ezrin/Radixin/Moesin, and L-selectin.

Killock DJ, Parsons M, Zarrouk M, Ameer-Beg SM, Ridley AJ, Haskard DO, Zvelebil M, Ivetic A.

J Biol Chem. 2009 Mar 27;284(13):8833-45. doi: 10.1074/jbc.M806983200. Epub 2009 Jan 7.

36.

Transcriptome analysis of mammary epithelial subpopulations identifies novel determinants of lineage commitment and cell fate.

Kendrick H, Regan JL, Magnay FA, Grigoriadis A, Mitsopoulos C, Zvelebil M, Smalley MJ.

BMC Genomics. 2008 Dec 8;9:591. doi: 10.1186/1471-2164-9-591.

37.

A threonine to isoleucine missense mutation in the pericentriolar material 1 gene is strongly associated with schizophrenia.

Datta SR, McQuillin A, Rizig M, Blaveri E, Thirumalai S, Kalsi G, Lawrence J, Bass NJ, Puri V, Choudhury K, Pimm J, Crombie C, Fraser G, Walker N, Curtis D, Zvelebil M, Pereira A, Kandaswamy R, St Clair D, Gurling HM.

Mol Psychiatry. 2010 Jun;15(6):615-28. doi: 10.1038/mp.2008.128. Epub 2008 Dec 2.

PMID:
19048012
38.

Inactivation of effector caspases through nondegradative polyubiquitylation.

Ditzel M, Broemer M, Tenev T, Bolduc C, Lee TV, Rigbolt KT, Elliott R, Zvelebil M, Blagoev B, Bergmann A, Meier P.

Mol Cell. 2008 Nov 21;32(4):540-53. doi: 10.1016/j.molcel.2008.09.025.

39.

MoKCa database--mutations of kinases in cancer.

Richardson CJ, Gao Q, Mitsopoulous C, Zvelebil M, Pearl LH, Pearl FM.

Nucleic Acids Res. 2009 Jan;37(Database issue):D824-31. doi: 10.1093/nar/gkn832. Epub 2008 Nov 5.

40.

IAPs contain an evolutionarily conserved ubiquitin-binding domain that regulates NF-kappaB as well as cell survival and oncogenesis.

Gyrd-Hansen M, Darding M, Miasari M, Santoro MM, Zender L, Xue W, Tenev T, da Fonseca PC, Zvelebil M, Bujnicki JM, Lowe S, Silke J, Meier P.

Nat Cell Biol. 2008 Nov;10(11):1309-17. doi: 10.1038/ncb1789. Epub 2008 Oct 19.

41.

Recombinant human serine racemase: enzymologic characterization and comparison with its mouse ortholog.

Hoffman HE, Jirásková J, Ingr M, Zvelebil M, Konvalinka J.

Protein Expr Purif. 2009 Jan;63(1):62-7. doi: 10.1016/j.pep.2008.09.003. Epub 2008 Sep 11.

PMID:
18812225
42.

The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer .

Folkes AJ, Ahmadi K, Alderton WK, Alix S, Baker SJ, Box G, Chuckowree IS, Clarke PA, Depledge P, Eccles SA, Friedman LS, Hayes A, Hancox TC, Kugendradas A, Lensun L, Moore P, Olivero AG, Pang J, Patel S, Pergl-Wilson GH, Raynaud FI, Robson A, Saghir N, Salphati L, Sohal S, Ultsch MH, Valenti M, Wallweber HJ, Wan NC, Wiesmann C, Workman P, Zhyvoloup A, Zvelebil MJ, Shuttleworth SJ.

J Med Chem. 2008 Sep 25;51(18):5522-32. doi: 10.1021/jm800295d.

PMID:
18754654
43.

Structural analysis of PI3-kinase isoforms: identification of residues enabling selective inhibition by small molecule ATP-competitive inhibitors.

Zvelebil MJ, Waterfield MD, Shuttleworth SJ.

Arch Biochem Biophys. 2008 Sep 15;477(2):404-10. doi: 10.1016/j.abb.2008.06.024. Epub 2008 Jul 8.

PMID:
18647592
44.

Phosphorylation regulates tau interactions with Src homology 3 domains of phosphatidylinositol 3-kinase, phospholipase Cgamma1, Grb2, and Src family kinases.

Reynolds CH, Garwood CJ, Wray S, Price C, Kellie S, Perera T, Zvelebil M, Yang A, Sheppard PW, Varndell IM, Hanger DP, Anderton BH.

J Biol Chem. 2008 Jun 27;283(26):18177-86. doi: 10.1074/jbc.M709715200. Epub 2008 May 8.

45.

Flavopiridol Hoechst AG.

Zvelebil MJ.

IDrugs. 1998 Jun;1(2):241-6.

PMID:
18465538
46.

Mechanism of two classes of cancer mutations in the phosphoinositide 3-kinase catalytic subunit.

Miled N, Yan Y, Hon WC, Perisic O, Zvelebil M, Inbar Y, Schneidman-Duhovny D, Wolfson HJ, Backer JM, Williams RL.

Science. 2007 Jul 13;317(5835):239-42.

47.

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.

48.

Exploring the specificity of the PI3K family inhibitor LY294002.

Gharbi SI, Zvelebil MJ, Shuttleworth SJ, Hancox T, Saghir N, Timms JF, Waterfield MD.

Biochem J. 2007 May 15;404(1):15-21.

49.

A model of directional selection applied to the evolution of drug resistance in HIV-1.

Seoighe C, Ketwaroo F, Pillay V, Scheffler K, Wood N, Duffet R, Zvelebil M, Martinson N, McIntyre J, Morris L, Hide W.

Mol Biol Evol. 2007 Apr;24(4):1025-31. Epub 2007 Feb 1.

PMID:
17272680
50.

Resources for integrative systems biology: from data through databases to networks and dynamic system models.

Ng A, Bursteinas B, Gao Q, Mollison E, Zvelebil M.

Brief Bioinform. 2006 Dec;7(4):318-30. Epub 2006 Oct 13. Review.

PMID:
17040977

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