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Items: 40

1.

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
2.

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
3.

Flavopiridol Hoechst AG.

Zvelebil MJ.

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

PMID:
18465538
4.

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.

5.

The application of 2D gel-based proteomics methods to the study of breast cancer.

Stein RC, Zvelebil MJ.

J Mammary Gland Biol Neoplasia. 2002 Oct;7(4):385-93. Review.

PMID:
12882523
6.
7.

Evaluation of two-dimensional differential gel electrophoresis for proteomic expression analysis of a model breast cancer cell system.

Gharbi S, Gaffney P, Yang A, Zvelebil MJ, Cramer R, Waterfield MD, Timms JF.

Mol Cell Proteomics. 2002 Feb;1(2):91-8.

8.

Cluster analysis of an extensive human breast cancer cell line protein expression map database.

Harris RA, Yang A, Stein RC, Lucy K, Brusten L, Herath A, Parekh R, Waterfield MD, O'Hare MJ, Neville MA, Page MJ, Zvelebil MJ.

Proteomics. 2002 Feb;2(2):212-23.

PMID:
11840567
9.

Activation loop sequences confer substrate specificity to phosphoinositide 3-kinase alpha (PI3Kalpha ). Functions of lipid kinase-deficient PI3Kalpha in signaling.

Pirola L, Zvelebil MJ, Bulgarelli-Leva G, Van Obberghen E, Waterfield MD, Wymann MP.

J Biol Chem. 2001 Jun 15;276(24):21544-54. Epub 2001 Feb 13.

10.

Class II phosphoinositide 3-kinases are downstream targets of activated polypeptide growth factor receptors.

Arcaro A, Zvelebil MJ, Wallasch C, Ullrich A, Waterfield MD, Domin J.

Mol Cell Biol. 2000 Jun;20(11):3817-30.

11.

Proteomic definition of normal human luminal and myoepithelial breast cells purified from reduction mammoplasties.

Page MJ, Amess B, Townsend RR, Parekh R, Herath A, Brusten L, Zvelebil MJ, Stein RC, Waterfield MD, Davies SC, O'Hare MJ.

Proc Natl Acad Sci U S A. 1999 Oct 26;96(22):12589-94.

12.

Identification of germline missense mutations and rare allelic variants in the ATM gene in early-onset breast cancer.

Izatt L, Greenman J, Hodgson S, Ellis D, Watts S, Scott G, Jacobs C, Liebmann R, Zvelebil MJ, Mathew C, Solomon E.

Genes Chromosomes Cancer. 1999 Dec;26(4):286-94.

PMID:
10534763
13.

Human phosphoinositide 3-kinase C2beta, the role of calcium and the C2 domain in enzyme activity.

Arcaro A, Volinia S, Zvelebil MJ, Stein R, Watton SJ, Layton MJ, Gout I, Ahmadi K, Downward J, Waterfield MD.

J Biol Chem. 1998 Dec 4;273(49):33082-90.

14.

1H NMR structure of an antifungal gamma-thionin protein SIalpha1: similarity to scorpion toxins.

Bloch C Jr, Patel SU, Baud F, Zvelebil MJ, Carr MD, Sadler PJ, Thornton JM.

Proteins. 1998 Aug 15;32(3):334-49.

PMID:
9715910
15.

Perforin is activated by a proteolytic cleavage during biosynthesis which reveals a phospholipid-binding C2 domain.

Uellner R, Zvelebil MJ, Hopkins J, Jones J, MacDougall LK, Morgan BP, Podack E, Waterfield MD, Griffiths GM.

EMBO J. 1997 Dec 15;16(24):7287-96.

16.

Cloning of a human phosphoinositide 3-kinase with a C2 domain that displays reduced sensitivity to the inhibitor wortmannin.

Domin J, Pages F, Volinia S, Rittenhouse SE, Zvelebil MJ, Stein RC, Waterfield MD.

Biochem J. 1997 Aug 15;326 ( Pt 1):139-47.

17.

P110delta, a novel phosphoinositide 3-kinase in leukocytes.

Vanhaesebroeck B, Welham MJ, Kotani K, Stein R, Warne PH, Zvelebil MJ, Higashi K, Volinia S, Downward J, Waterfield MD.

Proc Natl Acad Sci U S A. 1997 Apr 29;94(9):4330-5.

18.

Distinct specificity in the recognition of phosphoinositides by the pleckstrin homology domains of dynamin and Bruton's tyrosine kinase.

Salim K, Bottomley MJ, Querfurth E, Zvelebil MJ, Gout I, Scaife R, Margolis RL, Gigg R, Smith CI, Driscoll PC, Waterfield MD, Panayotou G.

EMBO J. 1996 Nov 15;15(22):6241-50.

19.

The C-terminal SH3 domain of p67phox binds its natural ligand in a reverse orientation.

Finan P, Koga H, Zvelebil MJ, Waterfield MD, Kellie S.

J Mol Biol. 1996 Aug 16;261(2):173-80.

PMID:
8757285
20.

Wortmannin inactivates phosphoinositide 3-kinase by covalent modification of Lys-802, a residue involved in the phosphate transfer reaction.

Wymann MP, Bulgarelli-Leva G, Zvelebil MJ, Pirola L, Vanhaesebroeck B, Waterfield MD, Panayotou G.

Mol Cell Biol. 1996 Apr;16(4):1722-33.

21.

Structural and functional diversity of phosphoinositide 3-kinases.

Zvelebil MJ, MacDougall L, Leevers S, Volinia S, Vanhaesebroeck B, Gout I, Panayotou G, Domin J, Stein R, Pages F, et al.

Philos Trans R Soc Lond B Biol Sci. 1996 Feb 29;351(1336):217-23. Review.

PMID:
8650269
22.

Structural similarity between the pleckstrin homology domain and verotoxin: the problem of measuring and evaluating structural similarity.

Orengo CA, Swindells MB, Michie AD, Zvelebil MJ, Driscoll PC, Waterfield MD, Thornton JM.

Protein Sci. 1995 Oct;4(10):1977-83.

23.

A human phosphatidylinositol 3-kinase complex related to the yeast Vps34p-Vps15p protein sorting system.

Volinia S, Dhand R, Vanhaesebroeck B, MacDougall LK, Stein R, Zvelebil MJ, Domin J, Panaretou C, Waterfield MD.

EMBO J. 1995 Jul 17;14(14):3339-48.

24.

Prediction and analysis of SH2 domain-phosphopeptide interactions.

Zvelebil MJ, Panayotou G, Linacre J, Waterfield MD.

Protein Eng. 1995 Jun;8(6):527-33.

PMID:
8532676
25.

Structural basis for pleckstrin homology domain mutations in X-linked agammaglobulinemia.

Vihinen M, Zvelebil MJ, Zhu Q, Brooimans RA, Ochs HD, Zegers BJ, Nilsson L, Waterfield MD, Smith CI.

Biochemistry. 1995 Feb 7;34(5):1475-81.

PMID:
7849006
26.

A novel point mutation in the tyrosine kinase domain of the RET proto-oncogene in sporadic medullary thyroid carcinoma and in a family with FMTC.

Eng C, Smith DP, Mulligan LM, Healey CS, Zvelebil MJ, Stonehouse TJ, Ponder MA, Jackson CE, Waterfield MD, Ponder BA.

Oncogene. 1995 Feb 2;10(3):509-13.

PMID:
7845675
27.

Three-dimensional solution structure of the pleckstrin homology domain from dynamin.

Downing AK, Driscoll PC, Gout I, Salim K, Zvelebil MJ, Waterfield MD.

Curr Biol. 1994 Oct 1;4(10):884-91.

PMID:
7850421
28.

Mechanism of inhibition of trypanothione reductase and glutathione reductase by trivalent organic arsenicals.

Cunningham ML, Zvelebil MJ, Fairlamb AH.

Eur J Biochem. 1994 Apr 1;221(1):285-95.

29.

Peptide-protein interactions: an overview.

Zvelebil MJ, Thornton JM.

Q Rev Biophys. 1993 Aug;26(3):333-63. Review. No abstract available.

PMID:
8022970
30.

A detailed molecular model for human aromatase.

Laughton CA, Zvelebil MJ, Neidle S.

J Steroid Biochem Mol Biol. 1993 Mar;44(4-6):399-407.

PMID:
8476753
31.

Molecular modelling and epitope prediction of gp29 from lymphatic filariae.

Zvelebil MJ, Tang L, Cookson E, Selkirk ME, Thornton JM.

Mol Biochem Parasitol. 1993 Mar;58(1):145-53.

PMID:
7681545
32.

A pyruvate-stimulated adenylate cyclase has a sequence related to the fes/fps oncogenes and to eukaryotic cyclases.

Peters EP, Wilderspin AF, Wood SP, Zvelebil MJ, Sezer O, Danchin A.

Mol Microbiol. 1991 May;5(5):1175-81.

PMID:
1683468
33.

A predicted three-dimensional structure of human cytochrome P450: implications for substrate specificity.

Zvelebil MJ, Wolf CR, Sternberg MJ.

Protein Eng. 1991 Feb;4(3):271-82.

PMID:
1857713
34.

A molecular model for the enzyme cytochrome P450(17 alpha), a major target for the chemotherapy of prostatic cancer.

Laughton CA, Neidle S, Zvelebil MJ, Sternberg MJ.

Biochem Biophys Res Commun. 1990 Sep 28;171(3):1160-7.

PMID:
2222435
35.

Prediction of protein structure from sequence.

Sternberg MJ, Zvelebil MJ.

Eur J Cancer. 1990;26(11-12):1163-6.

PMID:
2149999
36.
37.

Analysis and prediction of the location of catalytic residues in enzymes.

Zvelebil MJ, Sternberg MJ.

Protein Eng. 1988 Jul;2(2):127-38.

PMID:
3244695
38.

Prediction of antigenic determinants and secondary structures of the major AIDS virus proteins.

Sternberg MJ, Barton GJ, Zvelebil MJ, Cookson J, Coates AR.

FEBS Lett. 1987 Jun 29;218(2):231-7.

39.

Prediction of protein secondary structure and active sites using the alignment of homologous sequences.

Zvelebil MJ, Barton GJ, Taylor WR, Sternberg MJ.

J Mol Biol. 1987 Jun 20;195(4):957-61.

PMID:
3656439
40.

AIDS vaccine predictions.

Coates AR, Cookson J, Barton GJ, Zvelebil MJ, Sternberg MJ.

Nature. 1987 Apr 9-15;326(6113):549-50. No abstract available.

PMID:
2436055

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