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Items: 46

1.

Translational Framework Predicting Tumour Response in Gemcitabine-Treated Patients with Advanced Pancreatic and Ovarian Cancer from Xenograft Studies.

Garcia-Cremades M, Pitou C, Iversen PW, Troconiz IF.

AAPS J. 2019 Jan 31;21(2):23. doi: 10.1208/s12248-018-0291-9.

PMID:
30706160
2.

Broad Spectrum Activity of the Checkpoint Kinase 1 Inhibitor Prexasertib as a Single Agent or Chemopotentiator Across a Range of Preclinical Pediatric Tumor Models.

Lowery CD, Dowless M, Renschler M, Blosser W, VanWye AB, Stephens JR, Iversen PW, Lin AB, Beckmann RP, Krytska K, Cole KA, Maris JM, Hawkins DS, Rubin BP, Kurmasheva RT, Houghton PJ, Gorlick R, Kolb EA, Kang MH, Reynolds CP, Erickson SW, Teicher BA, Smith MA, Stancato LF.

Clin Cancer Res. 2019 Apr 1;25(7):2278-2289. doi: 10.1158/1078-0432.CCR-18-2728. Epub 2018 Dec 18.

PMID:
30563935
3.

Aurora A Kinase Inhibition Is Synthetic Lethal with Loss of the RB1 Tumor Suppressor Gene.

Gong X, Du J, Parsons SH, Merzoug FF, Webster Y, Iversen PW, Chio LC, Van Horn RD, Lin X, Blosser W, Han B, Jin S, Yao S, Bian H, Ficklin C, Fan L, Kapoor A, Antonysamy S, Mc Nulty AM, Froning K, Manglicmot D, Pustilnik A, Weichert K, Wasserman SR, Dowless M, Marugán C, Baquero C, Lallena MJ, Eastman SW, Hui YH, Dieter MZ, Doman T, Chu S, Qian HR, Ye XS, Barda DA, Plowman GD, Reinhard C, Campbell RM, Henry JR, Buchanan SG.

Cancer Discov. 2019 Feb;9(2):248-263. doi: 10.1158/2159-8290.CD-18-0469. Epub 2018 Oct 29.

PMID:
30373917
4.

Characterization of a novel AICARFT inhibitor which potently elevates ZMP and has anti-tumor activity in murine models.

Brooks HB, Meier TI, Geeganage S, Fales KR, Thrasher KJ, Konicek SA, Spencer CD, Thibodeaux S, Foreman RT, Hui YH, Roth KD, Qian YW, Wang T, Luo S, Torrado A, Si C, Toth JL, Mc Cowan JR, Frimpong K, Lee MR, Dally RD, Shepherd TA, Durham TB, Wang Y, Wu Z, Iversen PW, Njoroge FG.

Sci Rep. 2018 Oct 18;8(1):15458. doi: 10.1038/s41598-018-33453-4.

5.

Assay Guidance Manual: Quantitative Biology and Pharmacology in Preclinical Drug Discovery.

Coussens NP, Sittampalam GS, Guha R, Brimacombe K, Grossman A, Chung TDY, Weidner JR, Riss T, Trask OJ, Auld D, Dahlin JL, Devanaryan V, Foley TL, McGee J, Kahl SD, Kales SC, Arkin M, Baell J, Bejcek B, Gal-Edd N, Glicksman M, Haas JV, Iversen PW, Hoeppner M, Lathrop S, Sayers E, Liu H, Trawick B, McVey J, Lemmon VP, Li Z, McManus O, Minor L, Napper A, Wildey MJ, Pacifici R, Chin WW, Xia M, Xu X, Lal-Nag M, Hall MD, Michael S, Inglese J, Simeonov A, Austin CP.

Clin Transl Sci. 2018 Sep;11(5):461-470. doi: 10.1111/cts.12570. Epub 2018 Jul 24.

6.

Targeting the TGFβ pathway with galunisertib, a TGFβRI small molecule inhibitor, promotes anti-tumor immunity leading to durable, complete responses, as monotherapy and in combination with checkpoint blockade.

Holmgaard RB, Schaer DA, Li Y, Castaneda SP, Murphy MY, Xu X, Inigo I, Dobkin J, Manro JR, Iversen PW, Surguladze D, Hall GE, Novosiadly RD, Benhadji KA, Plowman GD, Kalos M, Driscoll KE.

J Immunother Cancer. 2018 Jun 4;6(1):47. doi: 10.1186/s40425-018-0356-4.

7.

Systematic Modeling and Design Evaluation of Unperturbed Tumor Dynamics in Xenografts.

Parra-Guillen ZP, Mangas-Sanjuan V, Garcia-Cremades M, Troconiz IF, Mo G, Pitou C, Iversen PW, Wallin JE.

J Pharmacol Exp Ther. 2018 Jul;366(1):96-104. doi: 10.1124/jpet.118.248286. Epub 2018 Apr 24.

PMID:
29691287
8.

The CDK4/6 Inhibitor Abemaciclib Induces a T Cell Inflamed Tumor Microenvironment and Enhances the Efficacy of PD-L1 Checkpoint Blockade.

Schaer DA, Beckmann RP, Dempsey JA, Huber L, Forest A, Amaladas N, Li Y, Wang YC, Rasmussen ER, Chin D, Capen A, Carpenito C, Staschke KA, Chung LA, Litchfield LM, Merzoug FF, Gong X, Iversen PW, Buchanan S, de Dios A, Novosiadly RD, Kalos M.

Cell Rep. 2018 Mar 13;22(11):2978-2994. doi: 10.1016/j.celrep.2018.02.053.

9.

Preclinical assessment of galunisertib (LY2157299 monohydrate), a first-in-class transforming growth factor-β receptor type I inhibitor.

Yingling JM, McMillen WT, Yan L, Huang H, Sawyer JS, Graff J, Clawson DK, Britt KS, Anderson BD, Beight DW, Desaiah D, Lahn MM, Benhadji KA, Lallena MJ, Holmgaard RB, Xu X, Zhang F, Manro JR, Iversen PW, Iyer CV, Brekken RA, Kalos MD, Driscoll KE.

Oncotarget. 2017 Dec 31;9(6):6659-6677. doi: 10.18632/oncotarget.23795. eCollection 2018 Jan 23.

10.

Predicting tumour growth and its impact on survival in gemcitabine-treated patients with advanced pancreatic cancer.

Garcia-Cremades M, Pitou C, Iversen PW, Troconiz IF.

Eur J Pharm Sci. 2018 Mar 30;115:296-303. doi: 10.1016/j.ejps.2018.01.033. Epub 2018 Jan 31.

PMID:
29366960
11.

Genomic Aberrations that Activate D-type Cyclins Are Associated with Enhanced Sensitivity to the CDK4 and CDK6 Inhibitor Abemaciclib.

Gong X, Litchfield LM, Webster Y, Chio LC, Wong SS, Stewart TR, Dowless M, Dempsey J, Zeng Y, Torres R, Boehnke K, Mur C, Marugán C, Baquero C, Yu C, Bray SM, Wulur IH, Bi C, Chu S, Qian HR, Iversen PW, Merzoug FF, Ye XS, Reinhard C, De Dios A, Du J, Caldwell CW, Lallena MJ, Beckmann RP, Buchanan SG.

Cancer Cell. 2017 Dec 11;32(6):761-776.e6. doi: 10.1016/j.ccell.2017.11.006.

12.

Minimum Significant Ratio – A Statistic to Assess Assay Variability.

Haas JV, Eastwood BJ, Iversen PW, Devanarayan V, Weidner JR.

In: Sittampalam GS, Coussens NP, Brimacombe K, Grossman A, Arkin M, Auld D, Austin C, Baell J, Bejcek B, Caaveiro JMM, Chung TDY, Dahlin JL, Devanaryan V, Foley TL, Glicksman M, Hall MD, Haas JV, Inglese J, Iversen PW, Kahl SD, Kales SC, Lal-Nag M, Li Z, McGee J, McManus O, Riss T, Trask OJ Jr., Weidner JR, Wildey MJ, Xia M, Xu X, editors. Assay Guidance Manual [Internet]. Bethesda (MD): Eli Lilly & Company and the National Center for Advancing Translational Sciences; 2004-.
2013 Nov 1 [updated 2017 Nov 20].

13.

Assay Operations for SAR Support.

Beck B, Chen YF, Dere W, Devanarayan V, Eastwood BJ, Farmen MW, Iturria SJ, Iversen PW, Kahl SD, Moore RA, Sawyer BD, Weidner J.

In: Sittampalam GS, Coussens NP, Brimacombe K, Grossman A, Arkin M, Auld D, Austin C, Baell J, Bejcek B, Caaveiro JMM, Chung TDY, Dahlin JL, Devanaryan V, Foley TL, Glicksman M, Hall MD, Haas JV, Inglese J, Iversen PW, Kahl SD, Kales SC, Lal-Nag M, Li Z, McGee J, McManus O, Riss T, Trask OJ Jr., Weidner JR, Wildey MJ, Xia M, Xu X, editors. Assay Guidance Manual [Internet]. Bethesda (MD): Eli Lilly & Company and the National Center for Advancing Translational Sciences; 2004-.
2012 May 1 [updated 2017 Nov 20].

14.

RAF inhibitor LY3009120 sensitizes RAS or BRAF mutant cancer to CDK4/6 inhibition by abemaciclib via superior inhibition of phospho-RB and suppression of cyclin D1.

Chen SH, Gong X, Zhang Y, Van Horn RD, Yin T, Huber L, Burke TF, Manro J, Iversen PW, Wu W, Bhagwat SV, Beckmann RP, Tiu RV, Buchanan SG, Peng SB.

Oncogene. 2018 Feb 8;37(6):821-832. doi: 10.1038/onc.2017.384. Epub 2017 Oct 23.

PMID:
29059158
15.

Mouse PDX Trial Suggests Synergy of Concurrent Inhibition of RAF and EGFR in Colorectal Cancer with BRAF or KRAS Mutations.

Yao YM, Donoho GP, Iversen PW, Zhang Y, Van Horn RD, Forest A, Novosiadly RD, Webster YW, Ebert P, Bray S, Ting JC, Aggarwal A, Henry JR, Tiu RV, Plowman GD, Peng SB.

Clin Cancer Res. 2017 Sep 15;23(18):5547-5560. doi: 10.1158/1078-0432.CCR-16-3250. Epub 2017 Jun 13.

16.

Characterizing Gemcitabine Effects Administered as Single Agent or Combined with Carboplatin in Mice Pancreatic and Ovarian Cancer Xenografts: A Semimechanistic Pharmacokinetic/Pharmacodynamics Tumor Growth-Response Model.

Garcia-Cremades M, Pitou C, Iversen PW, Troconiz IF.

J Pharmacol Exp Ther. 2017 Mar;360(3):445-456. doi: 10.1124/jpet.116.237610. Epub 2016 Dec 27.

PMID:
28028124
17.

Assay Establishment and Validation of a High-Throughput Screening Platform for Three-Dimensional Patient-Derived Colon Cancer Organoid Cultures.

Boehnke K, Iversen PW, Schumacher D, Lallena MJ, Haro R, Amat J, Haybaeck J, Liebs S, Lange M, Schäfer R, Regenbrecht CR, Reinhard C, Velasco JA.

J Biomol Screen. 2016 Oct;21(9):931-41. doi: 10.1177/1087057116650965. Epub 2016 May 27.

18.

A novel CDK9 inhibitor shows potent antitumor efficacy in preclinical hematologic tumor models.

Yin T, Lallena MJ, Kreklau EL, Fales KR, Carballares S, Torrres R, Wishart GN, Ajamie RT, Cronier DM, Iversen PW, Meier TI, Foreman RT, Zeckner D, Sissons SE, Halstead BW, Lin AB, Donoho GP, Qian Y, Li S, Wu S, Aggarwal A, Ye XS, Starling JJ, Gaynor RB, de Dios A, Du J.

Mol Cancer Ther. 2014 Jun;13(6):1442-56. doi: 10.1158/1535-7163.MCT-13-0849. Epub 2014 Mar 31.

19.

Selectivity data: assessment, predictions, concordance, and implications.

Gao C, Cahya S, Nicolaou CA, Wang J, Watson IA, Cummins DJ, Iversen PW, Vieth M.

J Med Chem. 2013 Sep 12;56(17):6991-7002. doi: 10.1021/jm400798j. Epub 2013 Aug 30.

PMID:
23937569
20.

Discovery and characterization of LY2784544, a small-molecule tyrosine kinase inhibitor of JAK2V617F.

Ma L, Clayton JR, Walgren RA, Zhao B, Evans RJ, Smith MC, Heinz-Taheny KM, Kreklau EL, Bloem L, Pitou C, Shen W, Strelow JM, Halstead C, Rempala ME, Parthasarathy S, Gillig JR, Heinz LJ, Pei H, Wang Y, Stancato LF, Dowless MS, Iversen PW, Burkholder TP.

Blood Cancer J. 2013 Apr 12;3:e109. doi: 10.1038/bcj.2013.6.

21.

Inhibition of Mnk kinase activity by cercosporamide and suppressive effects on acute myeloid leukemia precursors.

Altman JK, Szilard A, Konicek BW, Iversen PW, Kroczynska B, Glaser H, Sassano A, Vakana E, Graff JR, Platanias LC.

Blood. 2013 May 2;121(18):3675-81. doi: 10.1182/blood-2013-01-477216. Epub 2013 Mar 18.

22.

Human carboxylesterase-2 hydrolyzes the prodrug of gemcitabine (LY2334737) and confers prodrug sensitivity to cancer cells.

Pratt SE, Durland-Busbice S, Shepard RL, Heinz-Taheny K, Iversen PW, Dantzig AH.

Clin Cancer Res. 2013 Mar 1;19(5):1159-68. doi: 10.1158/1078-0432.CCR-12-1184. Epub 2013 Jan 16.

23.

Mechanism of Action Assays for Enzymes.

Strelow J, Dewe W, Iversen PW, Brooks HB, Radding JA, McGee J, Weidner J.

In: Sittampalam GS, Coussens NP, Brimacombe K, Grossman A, Arkin M, Auld D, Austin C, Baell J, Bejcek B, Caaveiro JMM, Chung TDY, Dahlin JL, Devanaryan V, Foley TL, Glicksman M, Hall MD, Haas JV, Inglese J, Iversen PW, Kahl SD, Kales SC, Lal-Nag M, Li Z, McGee J, McManus O, Riss T, Trask OJ Jr., Weidner JR, Wildey MJ, Xia M, Xu X, editors. Assay Guidance Manual [Internet]. Bethesda (MD): Eli Lilly & Company and the National Center for Advancing Translational Sciences; 2004-.
2012 May 1 [updated 2012 Oct 1].

24.

HTS Assay Validation.

Iversen PW, Beck B, Chen YF, Dere W, Devanarayan V, Eastwood BJ, Farmen MW, Iturria SJ, Montrose C, Moore RA, Weidner JR, Sittampalam GS.

In: Sittampalam GS, Coussens NP, Brimacombe K, Grossman A, Arkin M, Auld D, Austin C, Baell J, Bejcek B, Caaveiro JMM, Chung TDY, Dahlin JL, Devanaryan V, Foley TL, Glicksman M, Hall MD, Haas JV, Inglese J, Iversen PW, Kahl SD, Kales SC, Lal-Nag M, Li Z, McGee J, McManus O, Riss T, Trask OJ Jr., Weidner JR, Wildey MJ, Xia M, Xu X, editors. Assay Guidance Manual [Internet]. Bethesda (MD): Eli Lilly & Company and the National Center for Advancing Translational Sciences; 2004-.
2012 May 1 [updated 2012 Oct 1].

25.

Nonclinical assessment of carcinogenic risk and tumor growth enhancement potential of prasugrel, a platelet-inhibiting therapeutic agent.

Buckley LA, Sanbuissho A, Starling JJ, Knadler MP, Iversen PW, Jakubowski JA.

Int J Toxicol. 2012 Jul-Aug;31(4):317-25. doi: 10.1177/1091581812445073. Epub 2012 Jun 12.

PMID:
22692976
26.

Therapeutic inhibition of MAP kinase interacting kinase blocks eukaryotic initiation factor 4E phosphorylation and suppresses outgrowth of experimental lung metastases.

Konicek BW, Stephens JR, McNulty AM, Robichaud N, Peery RB, Dumstorf CA, Dowless MS, Iversen PW, Parsons S, Ellis KE, McCann DJ, Pelletier J, Furic L, Yingling JM, Stancato LF, Sonenberg N, Graff JR.

Cancer Res. 2011 Mar 1;71(5):1849-57. doi: 10.1158/0008-5472.CAN-10-3298. Epub 2011 Jan 13.

27.

A comparison of assay performance measures in screening assays: signal window, Z' factor, and assay variability ratio.

Iversen PW, Eastwood BJ, Sittampalam GS, Cox KL.

J Biomol Screen. 2006 Apr;11(3):247-52. Epub 2006 Feb 20.

PMID:
16490779
28.

The minimum significant ratio: a statistical parameter to characterize the reproducibility of potency estimates from concentration-response assays and estimation by replicate-experiment studies.

Eastwood BJ, Farmen MW, Iversen PW, Craft TJ, Smallwood JK, Garbison KE, Delapp NW, Smith GF.

J Biomol Screen. 2006 Apr;11(3):253-61. Epub 2006 Feb 20.

PMID:
16490778
29.

Elevated expression of angiogenin in prostate cancer and its precursors.

Katona TM, Neubauer BL, Iversen PW, Zhang S, Baldridge LA, Cheng L.

Clin Cancer Res. 2005 Dec 1;11(23):8358-63.

30.

The protein kinase Cbeta-selective inhibitor, Enzastaurin (LY317615.HCl), suppresses signaling through the AKT pathway, induces apoptosis, and suppresses growth of human colon cancer and glioblastoma xenografts.

Graff JR, McNulty AM, Hanna KR, Konicek BW, Lynch RL, Bailey SN, Banks C, Capen A, Goode R, Lewis JE, Sams L, Huss KL, Campbell RM, Iversen PW, Neubauer BL, Brown TJ, Musib L, Geeganage S, Thornton D.

Cancer Res. 2005 Aug 15;65(16):7462-9.

31.

Human splicing factor SPF45 (RBM17) confers broad multidrug resistance to anticancer drugs when overexpressed--a phenotype partially reversed by selective estrogen receptor modulators.

Perry WL 3rd, Shepard RL, Sampath J, Yaden B, Chin WW, Iversen PW, Jin S, Lesoon A, O'Brien KA, Peek VL, Rolfe M, Shyjan A, Tighe M, Williamson M, Krishnan V, Moore RE, Dantzig AH.

Cancer Res. 2005 Aug 1;65(15):6593-600.

32.

Acyl sulfonamide anti-proliferatives: benzene substituent structure-activity relationships for a novel class of antitumor agents.

Lobb KL, Hipskind PA, Aikins JA, Alvarez E, Cheung YY, Considine EL, De Dios A, Durst GL, Ferritto R, Grossman CS, Giera DD, Hollister BA, Huang Z, Iversen PW, Law KL, Li T, Lin HS, Lopez B, Lopez JE, Cabrejas LM, McCann DJ, Molero V, Reilly JE, Richett ME, Shih C, Teicher B, Wikel JH, White WT, Mader MM.

J Med Chem. 2004 Oct 21;47(22):5367-80.

PMID:
15481975
33.

Transgenic mice with cardiac-specific over-expression of MLK7 have increased mortality when exposed to chronic beta-adrenergic stimulation.

Christe M, Jin N, Wang X, Gould KE, Iversen PW, Yu X, Lorenz JN, Kadambi V, Zuckerman SH, Bloem LJ.

J Mol Cell Cardiol. 2004 Sep;37(3):705-15.

PMID:
15350844
34.

Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3.

Engler TA, Henry JR, Malhotra S, Cunningham B, Furness K, Brozinick J, Burkholder TP, Clay MP, Clayton J, Diefenbacher C, Hawkins E, Iversen PW, Li Y, Lindstrom TD, Marquart AL, McLean J, Mendel D, Misener E, Briere D, O'Toole JC, Porter WJ, Queener S, Reel JK, Owens RA, Brier RA, Eessalu TE, Wagner JR, Campbell RM, Vaughn R.

J Med Chem. 2004 Jul 29;47(16):3934-7.

PMID:
15267232
35.

Properties of bisphosphonates in the 13762 rat mammary carcinoma model of tumor-induced bone resorption.

Alvarez E, Westmore M, Galvin RJ, Clapp CL, Considine EL, Smith SJ, Keyes K, Iversen PW, Delafuente DM, Sulaimon S, Zambrano C, Ma L, Sato M, Martin TJ, Teicher BA, Galbreath EJ.

Clin Cancer Res. 2003 Nov 15;9(15):5705-13.

36.

Pharmacodynamics of oritavancin (LY333328) in a neutropenic-mouse thigh model of Staphylococcus aureus infection.

Boylan CJ, Campanale K, Iversen PW, Phillips DL, Zeckel ML, Parr TR Jr.

Antimicrob Agents Chemother. 2003 May;47(5):1700-6.

37.

Cloning and functional characterization of the multidrug resistance-associated protein (MRP1/ABCC1) from the cynomolgus monkey.

Godinot N, Iversen PW, Tabas L, Xia X, Williams DC, Dantzig AH, Perry WL 3rd.

Mol Cancer Ther. 2003 Mar;2(3):307-16.

38.

Protein kinase C betaII activation induces angiotensin converting enzyme expression in neonatal rat cardiomyocytes.

Zhang Y, Bloem LJ, Yu L, Estridge TB, Iversen PW, McDonald CE, Schrementi JP, Wang X, Vlahos CJ, Wang J.

Cardiovasc Res. 2003 Jan;57(1):139-46.

PMID:
12504823
39.

Validation of a noninvasive, real-time imaging technology using bioluminescent Escherichia coli in the neutropenic mouse thigh model of infection.

Rocchetta HL, Boylan CJ, Foley JW, Iversen PW, LeTourneau DL, McMillian CL, Contag PR, Jenkins DE, Parr TR Jr.

Antimicrob Agents Chemother. 2001 Jan;45(1):129-37.

40.

Aberrant methylation of the estrogen receptor and E-cadherin 5' CpG islands increases with malignant progression in human breast cancer.

Nass SJ, Herman JG, Gabrielson E, Iversen PW, Parl FF, Davidson NE, Graff JR.

Cancer Res. 2000 Aug 15;60(16):4346-8.

41.

An assessment of the antithymine and antipurine characteristics of MTA (LY231514) in CCRF-CEM cells.

Chen VJ, Bewley JR, Smith PG, Andis SL, Schultz RM, Iversen PW, Tonkinson JL, Shih C.

Adv Enzyme Regul. 2000;40:143-54. No abstract available.

PMID:
10828350
42.

Cellular pharmacology of MTA: a correlation of MTA-induced cellular toxicity and in vitro enzyme inhibition with its effect on intracellular folate and nucleoside triphosphate pools in CCRF-CEM cells.

Chen VJ, Bewley JR, Andis SL, Schultz RM, Iversen PW, Shih C, Mendelsohn LG, Seitz DE, Tonkinson JL.

Semin Oncol. 1999 Apr;26(2 Suppl 6):48-54.

PMID:
10598555
43.
45.

Application of automatic image segmentation to tibiae and vertebrae from ovariectomized rats.

Helterbrand JD, Higgs RE Jr, Iversen PW, Tysarczyk-Niemeyer G, Sato M.

Bone. 1997 Nov;21(5):401-9.

PMID:
9356733
46.

Protein kinase C isozymes differentially regulate promoters containing PEA-3/12-O-tetradecanoylphorbol-13-acetate response element motifs.

Reifel-Miller AE, Conarty DM, Valasek KM, Iversen PW, Burns DJ, Birch KA.

J Biol Chem. 1996 Aug 30;271(35):21666-71.

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