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Items: 48

1.

A phase Ib dose-finding, pharmacokinetic study of the focal adhesion kinase inhibitor GSK2256098 and trametinib in patients with advanced solid tumours.

Mak G, Soria JC, Blagden SP, Plummer R, Fleming RA, Nebot N, Zhang J, Mazumdar J, Rogan D, Gazzah A, Rizzuto I, Greystoke A, Yan L, Tolson J, Auger KR, Arkenau HT.

Br J Cancer. 2019 May;120(10):975-981. doi: 10.1038/s41416-019-0452-3. Epub 2019 Apr 17.

2.

A study of the focal adhesion kinase inhibitor GSK2256098 in patients with recurrent glioblastoma with evaluation of tumor penetration of [11C]GSK2256098.

Brown NF, Williams M, Arkenau HT, Fleming RA, Tolson J, Yan L, Zhang J, Swartz L, Singh R, Auger KR, Lenox L, Cox D, Lewis Y, Plisson C, Searle G, Saleem A, Blagden S, Mulholland P.

Neuro Oncol. 2018 Nov 12;20(12):1634-1642. doi: 10.1093/neuonc/noy078.

PMID:
29788497
3.

A phase I, pharmacokinetic and pharmacodynamic study of GSK2256098, a focal adhesion kinase inhibitor, in patients with advanced solid tumors.

Soria JC, Gan HK, Blagden SP, Plummer R, Arkenau HT, Ranson M, Evans TR, Zalcman G, Bahleda R, Hollebecque A, Lemech C, Dean E, Brown J, Gibson D, Peddareddigari V, Murray S, Nebot N, Mazumdar J, Swartz L, Auger KR, Fleming RA, Singh R, Millward M.

Ann Oncol. 2016 Dec;27(12):2268-2274. doi: 10.1093/annonc/mdw427. Epub 2016 Oct 11.

PMID:
27733373
4.

Discovery of a Potent Class of PI3Kα Inhibitors with Unique Binding Mode via Encoded Library Technology (ELT).

Yang H, Medeiros PF, Raha K, Elkins P, Lind KE, Lehr R, Adams ND, Burgess JL, Schmidt SJ, Knight SD, Auger KR, Schaber MD, Franklin GJ, Ding Y, DeLorey JL, Centrella PA, Mataruse S, Skinner SR, Clark MA, Cuozzo JW, Evindar G.

ACS Med Chem Lett. 2015 Mar 20;6(5):531-6. doi: 10.1021/acsmedchemlett.5b00025. eCollection 2015 May 14.

5.

BET inhibition silences expression of MYCN and BCL2 and induces cytotoxicity in neuroblastoma tumor models.

Wyce A, Ganji G, Smitheman KN, Chung CW, Korenchuk S, Bai Y, Barbash O, Le B, Craggs PD, McCabe MT, Kennedy-Wilson KM, Sanchez LV, Gosmini RL, Parr N, McHugh CF, Dhanak D, Prinjha RK, Auger KR, Tummino PJ.

PLoS One. 2013 Aug 23;8(8):e72967. doi: 10.1371/journal.pone.0072967. eCollection 2013.

6.

Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia.

Dawson MA, Prinjha RK, Dittmann A, Giotopoulos G, Bantscheff M, Chan WI, Robson SC, Chung CW, Hopf C, Savitski MM, Huthmacher C, Gudgin E, Lugo D, Beinke S, Chapman TD, Roberts EJ, Soden PE, Auger KR, Mirguet O, Doehner K, Delwel R, Burnett AK, Jeffrey P, Drewes G, Lee K, Huntly BJ, Kouzarides T.

Nature. 2011 Oct 2;478(7370):529-33. doi: 10.1038/nature10509.

7.
8.

Baculovirus production of fully-active phosphoinositide 3-kinase alpha as a p85alpha-p110alpha fusion for X-ray crystallographic analysis with ATP competitive enzyme inhibitors.

Sinnamon RH, McDevitt P, Pietrak BL, Leydon VR, Xue Y, Lehr R, Qi H, Burns M, Elkins P, Ward P, Vincentini G, Fisher D, Grimes M, Brandt M, Auger KR, Ho T, Johanson K, Jones CS, Schwartz B, Sweitzer TD, Kirkpatrick RB.

Protein Expr Purif. 2010 Oct;73(2):167-76. doi: 10.1016/j.pep.2010.05.002. Epub 2010 May 10.

PMID:
20457255
9.

Discovery of GSK2126458, a Highly Potent Inhibitor of PI3K and the Mammalian Target of Rapamycin.

Knight SD, Adams ND, Burgess JL, Chaudhari AM, Darcy MG, Donatelli CA, Luengo JI, Newlander KA, Parrish CA, Ridgers LH, Sarpong MA, Schmidt SJ, Van Aller GS, Carson JD, Diamond MA, Elkins PA, Gardiner CM, Garver E, Gilbert SA, Gontarek RR, Jackson JR, Kershner KL, Luo L, Raha K, Sherk CS, Sung CM, Sutton D, Tummino PJ, Wegrzyn RJ, Auger KR, Dhanak D.

ACS Med Chem Lett. 2010 Jan 19;1(1):39-43. doi: 10.1021/ml900028r. eCollection 2010 Apr 8.

10.

Discovery of the First Potent and Selective Inhibitor of Centromere-Associated Protein E: GSK923295.

Qian X, McDonald A, Zhou HJ, Adams ND, Parrish CA, Duffy KJ, Fitch DM, Tedesco R, Ashcraft LW, Yao B, Jiang H, Huang JK, Marin MV, Aroyan CE, Wang J, Ahmed S, Burgess JL, Chaudhari AM, Donatelli CA, Darcy MG, Ridgers LH, Newlander KA, Schmidt SJ, Chai D, Colón M, Zimmerman MN, Lad L, Sakowicz R, Schauer S, Belmont L, Baliga R, Pierce DW, Finer JT, Wang Z, Morgan BP, Morgans DJ Jr, Auger KR, Sung CM, Carson JD, Luo L, Hugger ED, Copeland RA, Sutton D, Elliott JD, Jackson JR, Wood KW, Dhanak D, Bergnes G, Knight SD.

ACS Med Chem Lett. 2010 Jan 19;1(1):30-4. doi: 10.1021/ml900018m. eCollection 2010 Apr 8.

11.

Molecular evolutionary analysis of cancer cell lines.

Zhang Y, Italia MJ, Auger KR, Halsey WS, Van Horn SF, Sathe GM, Magid-Slav M, Brown JR, Holbrook JD.

Mol Cancer Ther. 2010 Feb;9(2):279-91. doi: 10.1158/1535-7163.MCT-09-0508. Epub 2010 Feb 2.

12.

Conformation-dependent ligand regulation of ATP hydrolysis by human KSP: activation of basal hydrolysis and inhibition of microtubule-stimulated hydrolysis by a single, small molecule modulator.

Luo L, Carson JD, Molnar KS, Tuske SJ, Coales SJ, Hamuro Y, Sung CM, Sudakin V, Auger KR, Dhanak D, Jackson JR, Huang PS, Tummino PJ, Copeland RA.

J Am Chem Soc. 2008 Jun 18;130(24):7584-91. doi: 10.1021/ja710889h. Epub 2008 May 21.

PMID:
18491908
13.

ATP-competitive inhibitors of the mitotic kinesin KSP that function via an allosteric mechanism.

Luo L, Parrish CA, Nevins N, McNulty DE, Chaudhari AM, Carson JD, Sudakin V, Shaw AN, Lehr R, Zhao H, Sweitzer S, Lad L, Wood KW, Sakowicz R, Annan RS, Huang PS, Jackson JR, Dhanak D, Copeland RA, Auger KR.

Nat Chem Biol. 2007 Nov;3(11):722-6. Epub 2007 Oct 7.

PMID:
17922005
14.

Effects of oncogenic p110alpha subunit mutations on the lipid kinase activity of phosphoinositide 3-kinase.

Carson JD, Van Aller G, Lehr R, Sinnamon RH, Kirkpatrick RB, Auger KR, Dhanak D, Copeland RA, Gontarek RR, Tummino PJ, Luo L.

Biochem J. 2008 Jan 15;409(2):519-24.

PMID:
17877460
15.

Novel ATP-competitive kinesin spindle protein inhibitors.

Parrish CA, Adams ND, Auger KR, Burgess JL, Carson JD, Chaudhari AM, Copeland RA, Diamond MA, Donatelli CA, Duffy KJ, Faucette LF, Finer JT, Huffman WF, Hugger ED, Jackson JR, Knight SD, Luo L, Moore ML, Newlander KA, Ridgers LH, Sakowicz R, Shaw AN, Sung CM, Sutton D, Wood KW, Zhang SY, Zimmerman MN, Dhanak D.

J Med Chem. 2007 Oct 4;50(20):4939-52. Epub 2007 Aug 29.

PMID:
17725339
16.

A second p53 binding site in the central domain of Mdm2 is essential for p53 ubiquitination.

Ma J, Martin JD, Zhang H, Auger KR, Ho TF, Kirkpatrick RB, Grooms MH, Johanson KO, Tummino PJ, Copeland RA, Lai Z.

Biochemistry. 2006 Aug 1;45(30):9238-45.

PMID:
16866370
17.
18.

A method for determining intracellular concentrations of enzyme substrates from a combination of competitive inhibition and mutagenesis studies.

Copeland RA, Luo L, Auger KR, Huang PS.

Anal Biochem. 2005 Feb 15;337(2):351-3. No abstract available.

PMID:
15691518
19.

Differentiation of Hdm2-mediated p53 ubiquitination and Hdm2 autoubiquitination activity by small molecular weight inhibitors.

Lai Z, Yang T, Kim YB, Sielecki TM, Diamond MA, Strack P, Rolfe M, Caligiuri M, Benfield PA, Auger KR, Copeland RA.

Proc Natl Acad Sci U S A. 2002 Nov 12;99(23):14734-9. Epub 2002 Oct 29.

20.

Human mdm2 mediates multiple mono-ubiquitination of p53 by a mechanism requiring enzyme isomerization.

Lai Z, Ferry KV, Diamond MA, Wee KE, Kim YB, Ma J, Yang T, Benfield PA, Copeland RA, Auger KR.

J Biol Chem. 2001 Aug 17;276(33):31357-67. Epub 2001 Jun 7.

21.

Steady-state kinetic analysis of human ubiquitin-activating enzyme (E1) using a fluorescently labeled ubiquitin substrate.

Wee KE, Lai Z, Auger KR, Ma J, Horiuchi KY, Dowling RL, Dougherty CS, Corman JI, Wynn R, Copeland RA.

J Protein Chem. 2000 Aug;19(6):489-98.

PMID:
11195973
22.

Thermodynamics of p53 binding to hdm2(1-126): effects of phosphorylation and p53 peptide length.

Lai Z, Auger KR, Manubay CM, Copeland RA.

Arch Biochem Biophys. 2000 Sep 15;381(2):278-84.

PMID:
11032416
23.

SCF(beta-TRCP) and phosphorylation dependent ubiquitinationof I kappa B alpha catalyzed by Ubc3 and Ubc4.

Strack P, Caligiuri M, Pelletier M, Boisclair M, Theodoras A, Beer-Romero P, Glass S, Parsons T, Copeland RA, Auger KR, Benfield P, Brizuela L, Rolfe M.

Oncogene. 2000 Jul 20;19(31):3529-36.

24.

Constitutive cellular expression of PI 3-kinase is distinct from transient expression.

Auger KR, Wang J, Narsimhan RP, Holcombe T, Roberts TM.

Biochem Biophys Res Commun. 2000 Jun 16;272(3):822-9.

PMID:
10860837
25.

Platelet-derived growth factor stimulation of monocyte chemoattractant protein-1 gene expression is mediated by transient activation of the phosphoinositide 3-kinase signal transduction pathway.

Alberta JA, Auger KR, Batt D, Iannarelli P, Hwang G, Elliott HL, Duke R, Roberts TM, Stiles CD.

J Biol Chem. 1999 Oct 22;274(43):31062-7.

26.

Transformation of chicken cells by the gene encoding the catalytic subunit of PI 3-kinase.

Chang HW, Aoki M, Fruman D, Auger KR, Bellacosa A, Tsichlis PN, Cantley LC, Roberts TM, Vogt PK.

Science. 1997 Jun 20;276(5320):1848-50.

27.

Platelet-derived growth factor-induced formation of tensin and phosphoinositide 3-kinase complexes.

Auger KR, Songyang Z, Lo SH, Roberts TM, Chen LB.

J Biol Chem. 1996 Sep 20;271(38):23452-7.

28.
29.

Direct association of Grb2 with the p85 subunit of phosphatidylinositol 3-kinase.

Wang J, Auger KR, Jarvis L, Shi Y, Roberts TM.

J Biol Chem. 1995 May 26;270(21):12774-80.

30.

Polyoma middle tumor antigen interacts with SHC protein via the NPTY (Asn-Pro-Thr-Tyr) motif in middle tumor antigen.

Campbell KS, Ogris E, Burke B, Su W, Auger KR, Druker BJ, Schaffhausen BS, Roberts TM, Pallas DC.

Proc Natl Acad Sci U S A. 1994 Jul 5;91(14):6344-8.

31.

Phosphoinositide 3-kinase is activated by phosphopeptides that bind to the SH2 domains of the 85-kDa subunit.

Carpenter CL, Auger KR, Chanudhuri M, Yoakim M, Schaffhausen B, Shoelson S, Cantley LC.

J Biol Chem. 1993 May 5;268(13):9478-83.

32.

A tightly associated serine/threonine protein kinase regulates phosphoinositide 3-kinase activity.

Carpenter CL, Auger KR, Duckworth BC, Hou WM, Schaffhausen B, Cantley LC.

Mol Cell Biol. 1993 Mar;13(3):1657-65.

33.

Inhibition of SH2 domain/phosphoprotein association by a nonhydrolyzable phosphonopeptide.

Domchek SM, Auger KR, Chatterjee S, Burke TR Jr, Shoelson SE.

Biochemistry. 1992 Oct 20;31(41):9865-70.

PMID:
1382595
34.

Polyoma virus middle T antigen-pp60c-src complex associates with purified phosphatidylinositol 3-kinase in vitro.

Auger KR, Carpenter CL, Shoelson SE, Piwnica-Worms H, Cantley LC.

J Biol Chem. 1992 Mar 15;267(8):5408-15.

35.

Phosphatidylinositol-3 kinase and growth regulation.

Soltoff SP, Carpenter CL, Auger KR, Kapeller R, Schaffhausen B, Cantley LC.

Cold Spring Harb Symp Quant Biol. 1992;57:75-80. Review. No abstract available.

PMID:
1339706
36.

Novel polyphosphoinositides in cell growth and activation.

Auger KR, Cantley LC.

Cancer Cells. 1991 Jul;3(7):263-70. Review.

PMID:
1654970
37.

Oncogenes and signal transduction.

Cantley LC, Auger KR, Carpenter C, Duckworth B, Graziani A, Kapeller R, Soltoff S.

Cell. 1991 Jan 25;64(2):281-302. Review. No abstract available. Erratum in: Cell 1991 May 31;65(5):following 914.

PMID:
1846320
38.

Identification and quantification of polyphosphoinositides produced in response to platelet-derived growth factor stimulation.

Serunian LA, Auger KR, Cantley LC.

Methods Enzymol. 1991;198:78-87. No abstract available.

PMID:
1649958
39.

Purification and characterization of phosphoinositide 3-kinase from rat liver.

Carpenter CL, Duckworth BC, Auger KR, Cohen B, Schaffhausen BS, Cantley LC.

J Biol Chem. 1990 Nov 15;265(32):19704-11.

40.
41.

Phosphatidylinositol 3-kinase and its novel product, phosphatidylinositol 3-phosphate, are present in Saccharomyces cerevisiae.

Auger KR, Carpenter CL, Cantley LC, Varticovski L.

J Biol Chem. 1989 Dec 5;264(34):20181-4.

42.

PDGF-dependent tyrosine phosphorylation stimulates production of novel polyphosphoinositides in intact cells.

Auger KR, Serunian LA, Soltoff SP, Libby P, Cantley LC.

Cell. 1989 Apr 7;57(1):167-75.

PMID:
2467744
44.
45.

Inducible interleukin-1 gene expression in human vascular smooth muscle cells.

Libby P, Ordovas JM, Birinyi LK, Auger KR, Dinarello CA.

J Clin Invest. 1986 Dec;78(6):1432-8.

46.

Endotoxin and tumor necrosis factor induce interleukin-1 gene expression in adult human vascular endothelial cells.

Libby P, Ordovas JM, Auger KR, Robbins AH, Birinyi LK, Dinarello CA.

Am J Pathol. 1986 Aug;124(2):179-85.

47.
48.

Endothelial cell seeding of small-caliber synthetic grafts in the baboon.

Shepard AD, Eldrup-Jorgensen J, Keough EM, Foxall TF, Ramberg K, Connolly RJ, Mackey WC, Gavris V, Auger KR, Libby P, et al.

Surgery. 1986 Mar;99(3):318-26.

PMID:
2937170

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