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  • Chen CS, Wang YC, Yang HC, Huang PH et al., Histone deacetylase inhibitors sensitize prostate cancer cells to agents that produce DNA double-strand breaks by targeting Ku70 acetylation. Cancer Research, 67:5318-27, 2007.
  • *Chen CS, Weng SC, Tseng PH, Lin HP, and Chen CS. Nonepigenetic effects of histone deacetylase inhibitors on Akt through reshuffling protein phosphatase-1 complexes. J Biol Chem, 280:38879-38887, 2005.
  • *Chen CS, Weng SC, Tseng PH, Lin HP, and Chen CS, Histone Acetylation-independent Effect on Histone Deacetylase Inhibitors on Akt through the Reshuffling of Protein Phosphatase 1 Complexes. Journal of Biological Chemistry November 18, 2005: Volume 280: Number 46.
  • Chen CS, Weng SC, Tseng PH, Lin HP, Chen CS. Histone acetylation-independent effect of histone deacetylase inhibitors on Akt through the reshuffling of protein phosphatase 1 complexes. J Biol Chem. 2005 Nov 18;280(46):38879-87. Epub 2005 Sep 26.
  • Hassane DC, Balys M, Marcucci G, Byrd JC, Jordan CT, Guzman ML. Identification of the Histone Deacetylase Inhibitor (HDACi),AR-42, as a Novel Anti-Leukemia Stem Cell Agent in Acute Myeloid Leukemia (AML). ASH 2009 Abstract Poster Presentation.
  • Kisseberth WC, Murahari S, London CA, Kulp SK, Chen CS. Evaluation of the effects of histone deacetylase inhibitors on cells from canine cancer cell lines. Am J Vet Res. 2008 Jul;69(7):938-45.
  • Kulp SK, Chen CS, Wang D, Chen CY and Chen CS. Antitumor effects of a novel phenylbutyrate-based histone deacetylase inhibitor, (S)-HDAC-42, in prostate cancer. Clinical Cancer Research 12:5199-206, 2006.
  • Lin HY, Chen CS, Lin SP, Weng JR, Chen CS. Targeting histone deacetylase in cancer therapy. Med Res Rev. 2006 Jul;26(4):397-413.
  • Liu S, Wu LC, Pang J, Santhanam R, Schwind S, Wu YZ, Hickey CJ, Yu J, Becker H, Maharry K, Radmacher MD, Li C, Whitman SP, Mishra A, Stauffer N, Eiring AM, Briesewitz R, Baiocchi RA, Chan KK, Paschka P, Caligiuri MA, Byrd JC, Croce CM, Bloomfield CD, Perrotti D, Garzon R, Marcucci G. Sp1/NFkappaB/HDAC/miR-29b regulatory network in KIT-driven myeloid leukemia. Cancer Cell. 2010 Apr 13;17(4):333-47.
  • Lin TY, Fenger J, Murahari S, Bear MD, Kulp SK, Wang D, Chen CS, Kisseberth WC, London CA. AR-42, a novel HDAC inhibitor, exhibits biologic activity against malignant mast cell lines via downregulation of constitutively activated Kit. Blood. Prepublished online March 16, 2010.
  • Lu Q, Yang YT, Chen CS, Davis M, Byrd JC, Etherton MR, Umar A, Chen CS. Zn2+-chelating motif-tethered short-chain fatty acids as a novel class of histone deacetylase inhibitors. J Med Chem. 2004 Jan 15;47(2):467-74.
  • Lu YS, Kashida Y, Kulp SK, Wang YC et al., Efficacy of OSU-HDAC42, a Novel Histone Deacetylase Inhibitor, in Murine Models of Hepatocellular Carcinoma. Hepatology, Vol. 46, 2007.
  • Lucas DM, Alinari L, West DA, Davis ME, Edwards RB, et al. (2010) The Novel Deacetylase Inhibitor AR-42 Demonstrates Pre-Clinical Activity in B-Cell Malignancies In Vitro and In Vivo. PLoS ONE 5(6): e10941. doi:10.1371/journal.pone.0010941
  • Murahari S, Jalkanen A, Kulp S, Chen CS, Jubala C, Fosmire S, Modiano J, Fossey S, London C, Kisseberth W. OSU-HDAC42, a novel histone deacetylase inhibitor with potent antitumor effects on human and canine osteosarcoma cells. AACR Meeting Abstracts, Apr 2008; 2008: 2445.
  • Sargeant AM, Rengel RC, Kulp SK et al., OSU-HDAC42, a Histone Deacetylase Inhibitor, Blocks Prostate Tumor Progression in the Transgenic Adenocarcinoma of the Mouse Prostate Model. Cancer Res 2008; 68: (10).
  • Weng SC, Wu E, Kulp SK, Wang D, Wang YC, Chen CS, Yee LD. The antitumor effects of OSU-HDAC42, a histone deacetylase inhibitor, in HER2-positive breast cancer are mediated partly through Hsp90 modulation. AACR 2009 Abstract.
  • Yang YT, Balch C, Kulp SK, Mand MR, Nephew KP, Chen CS. A rationally designed histone deacetylase inhibitor with distinct antitumor activity against ovarian cancer. Neoplasia. 2009 Jun;11(6):552-63, 3 p following 563.


  • Abdulhameed MD, Hamza A, Zhan CG. Microscopic modes and free energies of 3-phosphoinositide-dependent kinase-1 (PDK1) binding with celecoxib and other inhibitors. J Phys Chem B. 2006 Dec 28;110(51):26365-74.
  • Alvarez FJ, Murahari S, Couto CG, Rosol TJ, Kulp SK, Chen CS, Kisseberth WC. 3-Phosphoinositide-dependent protein kinase-1/Akt signalling and inhibition in a canine prostate carcinoma cell line. Vet Comp Oncol. 2007 Mar;5(1):47-58.
  • Baryawno N, Sveinbjörnsson B, Eksborg S, Chen CS, Kogner P, Johnsen JI. Small-molecule inhibitors of phosphatidylinositol 3-kinase/Akt signaling inhibit Wnt/beta-catenin pathway cross-talk and suppress medulloblastoma growth. Cancer Res. 2010 Jan 1;70(1):266-76. Epub 2009 Dec 22.
  • Cen L, Hsieh FC, Lin HJ, Chen CS, Qualman SJ and Lin J, PDK-1/AKT pathway as a novel therapeutic target in rhabdomyosarcoma cells using OSU-03012 compound. British Journal of Cancer (2007).
  • Chiu HC, Kulp SK, Soni S, Wang D, Gunn JS, Schlesinger LS, Chen CS. Eradication of intracellular Salmonella enterica serovar Typhimurium with a small-molecule, host cell-directed agent. Antimicrob Agents Chemother. 2009 Dec;53(12):5236-44. Epub 2009 Oct 5.
  • Ding H, Han C, Guo D, Wang D, Chen CS, D'Ambrosio SM. OSU03012 activates Erk1/2 and Cdks leading to the accumulation of cells in the S-phase and apoptosis. Int J Cancer. 2008 Dec 15;123(12):2923-30.
  • Ding H, Han C, Guo D, Wang D, Duan W, Chen CS, D'Ambrosio SM. Sensitivity to the non-COX inhibiting celecoxib derivative, OSU03012, is p21(WAF1/CIP1) dependent. Int J Cancer. 2008 Dec 15;123(12):2931-8.
  • Gao M, Yeh PY, Lu YS, Hsu CH, Chen KF, Lee WC, Feng WC, Chen CS, Kuo ML, Cheng AL. OSU-03012, a novel celecoxib derivative, induces reactive oxygen species-related autophagy in hepatocellular carcinoma. Cancer Res. 2008 Nov 15;68(22):9348-57.
  • Hsu CH, Chao YW, Feng WC, Yeh PY, Chen CS, Cheng AL. Sorafenib, a multi-target inhibitor, and OSU-03012, a phosphoinositide- dependent kinase-1 inhibitor, are synergistic in cytotoxicity against nasopharyngeal carcinoma cells. AACR Meeting Abstracts, Apr 2008; 2008: 1331.
  • Johnson AJ, Smith LL, Zhu J, Heerema NA et al., A novel celecoxib derivative, OSU03012, induces cytotoxicity in primary CLL cells and transformed B-cell lymphoma cell line via a caspase- and Bcl-2-independent mechanism. Blood 2005 105: 2504-2509.
  • Lee TX, Packer MD, Huang J, Akhmametyeva EM, Kulp SK, Chen CS, Giovannini M, Jacob A, Welling DB, Chang LS. Growth inhibitory and anti-tumour activities of OSU-03012, a novel PDK-1 inhibitor, on vestibular schwannoma and malignant schwannoma cells. Eur J Cancer. 2009 Jun;45(9):1709-20. Epub 2009 Apr 7.
  • Li J, Zhu J, Melvin WS, Bekaii-Saab TS, Chen CS, Muscarella P. A structurally optimized celecoxib derivative inhibits human pancreatic cancer cell growth. J Gastrointest Surg. 2006 Feb;10(2):207-14.
  • McCubrey JA, LaHair MM, and Franklin RA, OSU-03012 in the Treatment of Glioblastoma. Molecular Pharmacology 70:437-439, 2006.
  • Park MA, Curiel DT, Koumenis C, Graf M, Chen CS, Fisher PB, Grant S, Dent P. PERK-dependent regulation of HSP70 expression and the regulation of autophagy. Autophagy. 2008 Apr 1;4(3):364-7. Epub 2008 Jan 17.
  • Park MA, Zhang G, Norris J, Hylemon PB, Fisher PB, Grant S, Dent P. Regulation of autophagy by ceramide-CD95-PERK signaling. Autophagy. 2008 Oct 1;4(7):929-31. Epub 2008 Oct 5.
  • Ping-Hui Tseng, Yu-Chieh Wang, Shu-Chuan Weng, et al., Overcoming Trastuzumab Resistance in HER2-Overexpressing Breast Cancer Cells by Using a Novel Celecoxib-Derived Phosphoinositide-Dependent Kinase-1 Inhibitor. Molecular Pharmacology 70:1534–1541, 2006.
  • Prochia LP. Guerra M, Wang YC, Zhang Y et al., OSU-03012, A Celecoxib Derivative, Directly Targets p21 Activated Kinase. Molecular Pharmacology Fast Forward 2007; doi:10.1121/mol.107.037556.
  • Sargeant AM, Klein RD, Rengel RC et al., Chemopreventive and Bioenergetic Signaling Effects of PDK1/Akt Pathway Inhibition in a Transgenic Mouse Model of Prostate Cancer. Toxicologic Pathology, 35:549-561, 2007.
  • Segerström L, Baryawno N, Sveinbjörnsson B, Johnsen JI, Kogner P. Effects of the PDK1-inhibitor OSU03012 and the PI3K inhibitor PI103 on neuroblastoma in vitro. 2009 AACR Poster Presentations.
  • Shah M, Kim H, Lopez-Bergmani P, Gaitonde S, De SK, Tcherpakov M, Dewing A, Yuan H, Riel-Mehan M, Krajewski S, Robertson G, Pellecchia M, Ronai Z. Targeting AKT and PDK1 in melanoma. Society for Melanoma Research: 2009 International Congress, Poster Abstracts.
  • To K, Zhao Y, Hu JK, Wang M et al., The Phosphoinositide-Dependent Kinase-1 Inhibitor 2-Amino-N-[4-[5-(2-phenanthrenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-acetamide (OSU-03012) Presents Y-Box Binding Portein-1 from Inducing Epidermal Growth Factor Receptor. Molecular Pharmacology 72:641-652, 2007.
  • To K, Zhao Y, Jiang H, Hu K, Wang M, Wu J, Lee C, Yokom DW, Stratford AL, Klinge U, Mertens PR, Chen CS, Bally M, Yapp D, Dunn SE. The phosphoinositide-dependent kinase-1 inhibitor 2-amino-N-[4-[5-(2-phenanthrenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-acetamide (OSU-03012) prevents Y-box binding protein-1 from inducing epidermal growth factor receptor. Mol Pharmacol. 2007 Sep;72(3):641-52. Epub 2007 Jun 26.
  • Tseng PH, Lin HP, Zhu J et al., Synergistic interactions between imatinib mesylate and the novel phosphoinositide-dependent kinase-1 inhibitor OSU-03012 in overcoming imatinib mesylate resistance. Blood, 15 May 2005 - Volume 105 - Number 10.
  • Wang et al., Targeting Endoplasmic Reticulum Stress and Akt with OSU-03012 and Gefitinib or Erlotinib to Overcome Resistance to Epidermal Growth Factor Receptor Inhibitors. Cancer Research 68, 2820-2830, April 2008. OSU-03012
  • Weng SC, Kashida Y, Kulp SK et al., Sensitizing estrogen-receptor - negative breast cancer cells to tamoxifen with OSU-03012, a novel celecoxib-derived phosphoinositide-dependent protein kinase - 1 /Akt signaling inhibitor. Mol Cancer Ther 2008; 7(4):800-8.
  • Yacoub A, Park MA, Hanna D et al., OSU-03012 Promotes Caspase-Independent but PERK-, Cathepsin B-, BID-, and AIF-Dependent Killing of Transformed Cells. Molecular Pharmacology 70:589-603, 2006.
  • Zhang S, Suvannasankha A, Crean C, White V et al., OSU-03012, a Novel Celecoxib Derivitave, Is Cytotoxic to Myeloma Cells and Acts through Multiple Mechanims. Clin Cancer Res 2007; 13(16).
  • Zhu J, Huang JW, Tseng PH et al., From the Cyclooxygenase-2 Inhibitor Celecoxib to a Novel Class of 3-Phosphoinositide-Dependent Protein Kinase-1 Inhibitors. Cancer Research 64, 4309-4318, June 15, 2004.

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