Selected Publications 2004 – 2009

(selected from a total of 162 peer-reviewed original publications)

S. K. Kulp, Y.-T. Yang, C.-C. Hung, K.-F. Chen, P.-H. Tseng, Y.-T. Yang, X. Zhu, J.-W. Huang, J. Fowble, and C.-S. Chen (2004) “PDK-1/Akt Signaling Represents a Major COX-2-Independent Target for the Antiproliferative Effect of the Cyclooxygenase-2 Inhibitor Celecoxib in Prostate Cancer Cells” Cancer Res. 64, 1444-1451.

Q. Lu, Y.-T. Yang, C.-S. Chen, M. Davis, J. C. Byrd, M. R. Etherton, A. Umar, and C.-S. Chen (2004) “Zn2+-Chelating Motif-Tethered Short-Chain Fatty Acids as a Novel Class of Histone Deacetylase Inhibitors” J. Med. Chem. 47, 467-474.

J. Zhu, J.-W. Huang, J. Fowble, P.-H. Tseng, C.-W. Shiau, Y-J. Shaw, S. K. Kulp, and C.-S. Chen (2004) “From the cyclooxygenase-2 inhibitor celecoxib to a novel class of potent Akt-targeted antitumor agents” Cancer Res. 64, 4309-4318.

P.-H. Tseng, H.-P. Lin, W. M. Shieh, H. Hu, C. Wang, X. Zhu, and C.-S. Chen (2004) “Selective Activation of TRPC Channels by Phosphophatidylinositol 3,4,5-Trisphosphate” Biochemistry 43, 11701-11708.

Y.-J. Shaw, Y.-T. Yang, J. B. Garrison, N. Kyprianou, and C.-S. Chen (2004) “Pharmacological exploitation of the a1-adrenoreceptor antagonist doxazosin to develop a novel class of antitumor agents that block intracellular Akt activation” J. Med. Chem. 47, 4453-62.

H.-P. Lin, S. K. Kulp, P.-H. Tseng, Y.-T. Yang, C.-S. Chen, C.-C. Yang, and C.-S. Chen (2004) “Growth-inhibitory effects of celecoxib in human umbilical vein endothelial cells are mediated through G1 arrest via multiple signaling mechanisms” Mol. Cancer Ther. 3, 1671-80.

R. Roychowdhury, R.A., Baiocchi, S. Vourgant, D. Bhatt, B.W. Blaser, A.G. Freud, J. Chou, C.-S. Chen, J.J. Xiao, M. Parthun, K.K. Chan, C.F. Eisenbeis, A.K. Ferketich, M.R. Grever, C.-S. Chen, M.A. Caligiuri (2004) “Selective efficacy of depsipeptide in a xenograft model of Epstein-Barr virus-positive lymphoproliferative disorder” J. Natl. Cancer Inst. 96, 1447-1457.

S. K. Kulp, K.-F. Chen, and C.-S. Chen (2005) “Chemotherapy for prostate cancer” in Prostate Cancer.  Basic mechanisms and Therapeutic Approaches (Ed., C. Chang) World Scientific, New Jersey, pp. 365-82.

A. J. Johnson, L. L. Smith, J. Zhu, N. A., Heerema, S. Jefferson, M. R. Grever, C.-S. Chen, J. C. Byrd (2005) “A novel celecoxib derivative induces apoptosis in primary CLL cells and transformed B-cll lymphoma via a caspase- and Bcl-2-independent mechanism” Blood 105, 2504-2509.

H. Ding, C. Han, J. Zhu, C.-S. Chen, and S. M. D’Ambrosio (2005) “Celecoxib derivatives induce apoptosis via the disruption of mitochondrial membrane potential and activation of caspase 9” Int. J. Cancer 113, 803-810.

C.-W. Shiau, C.-C. Yang, K.-F. Chen, J.-W. Huang, and C.-S. Chen (2005) “Thiazolidenediones mediates apoptosis in prostate cancer cells, in part, via the inhibition of Bcl-xL/Bcl-2 functions independently of PPARg” Cancer Res. 65, 1561-1569.

P.-H. Tseng, H.-P. Lin, K.-F. Chen, J. Zhu, J.C C. Byrd, M. R. Grever, B. J. Druker, and C.-S. Chen (2005) “synergistic interactions between imatinib and the novel phosphoinositide-dependent kinase-1 inhibitor OSU-03012 in overcoming imatinib resistance” Blood 105, 4021-4027.

J.-W. Huang, C.-W. Shiau, Y.-T. Yang, K.-F. Chen, S. K. Kulp, R. W. Brueggemeier, C. L. Shapiro, and C.-S. Chen (2005) “Peroxisome Proliferator-Activated Receptor g-Independent Ablation of Cyclin D1 by Thiazolidenediones and Their Derivatives in Breast Cancer Cells” Mol. Pharmacol. 67, 1342-1348.

O.S. Gardner, C.-W. Shiau, C.-S. Chen, and L.M. Graves (2005) “PPARg-independent activation of p38 MAPK by thiazolidebediones involves calcium/calmodulin-dependent protein kinase II and protein kinase R: correlation with endoplasmic reticulum stress” J. Biol. Chem. 280, 10109-10118.

J.E. Kucab, C. Lee, C.-S. Chen, J. Zhu, C. B. Gilks, M. Cheang, D. Huntsman, E. Yorida, J. Emerman, M. Pollak, S. E. Dunn (2005) Celecoxib analogues disrupt Akt signaling, which is commonly activated in primary breast tumours. Breast Cancer Res. 2005, 7:R796-R807.

Z. Tong, X. Wu, D. Ovcharenko, J. Zhu, C.-S. Chen, J. P. Kehrer (2005) Neutrophil gelatinase associated lipocalin as a survival factor.  Biochem. J. 391, 441-448.

C.-S, Chen, S.-C. Weng, P.-H. Tseng, H.-P. Lin, and C.-S. Chen (2005) “Nonepigenetic effects of histone deacetylase inhibitors on Akt through reshuffling protein phosphatae-1 complexes” J. Biol. Chem. 280, 38879-38887.

Q. Lu, D.-S. Wang, C.-S. Chen, Y.D. Hu, and C.-S. Chen (2005) “Structure-based optimization of phenylbutyrate-derived histone deacetylase inhibitors” J. Med. Chem. 48, 5530-5535.

C.-W. Shiau, J.-W. Huang, D.-S. Wang, J.-R. Weng, C.-C. Yang C. Li, and C.-S. Chen (2006) “a-Tocopheryl Succinate Induces Apoptosis in Prostate Cancer Cells in part through Inhibition of Bcl-xL/Bcl-2 Function”, J. Biol. Chem. 281, 11819-11825.

R. E. Teresi, C.-W. Shiau, C.-S. Chen, V. K. Chatterjee, K. A. Waite, and C. Eng (2006) “Increased PTEN expression due to transcriptional activation of PPARg by Lovastatin and Rosiglitazone” Int. J. Cancer 118, 2390-2398.

C.-C. Yang, C.-Y. Ku, S. Wei, C.-W. Shiau, C.-S. Chen, J. Pinzone, M.D. Ringel, and C.-S. Chen  (2006) “Peroxisome Proliferator-Activated Receptor g-Independent Repression of Prostate-Specific Antigen Expression by Thiazolidinediones in Prostate Cancer Cells”, Mol. Pharmacol. 69, 1564-1579.

J. Li, J. Zhu, W. S. Melvin, T. S., Bekaii-Saab, C.-S. Chen, P. Muscarella (2006) “A structurally optimized celecoxib derivative inhibits human pancreatic cancer cell growth” J. Gastrointest. Surg. 10, 207-214.

H.-Y. Lin, C.-S. Chen, S.-P. Lin, J.-R. Weng, and C.-S. Chen (2006) ²Targeting Histone Deacetylase in Cancer Therapy² Med. Res. Rev., 26, 397-413.

J.-R. Weng, C.-Y. Chen, J. Pinzone, M.D. Ringel, and C.-S. Chen (2006) ²Beyond PPARg Signaling. The Multi-Facets of the Antitumor Effect of Thiazolidinediones² Endocrine-Related Cancer 13, 401-413.

J. W. Huang, C.-W. Shiau, J. Yang, D.-S. Wang, C.-Y. Chen, and C.-S. Chen (2006) Development of Small-Molecule Cyclin D1-Ablative Agents” J. Med. Chem. 49, 4684-4689.

S. K. Kulp, C.-S. Chen, D.-S. Wang, C.-Y. Chen, and C.-S. Chen (2006) “Antitumor effects of a novel phenyl-butyrate-based histone deacetylase inhibitor, (S)-HDAC-42, in prostate cancer” Clin. Cancer Res., 12, 5199-5206.

A. Yacoub, M. A. Park, D. Hanna, Y. Hong, C. Mitchell, A. P. Pandya, H. Harada, G. Powis, C.-S. Chen, C. Koumenis, S. Grant, and P. Dent (2006) “OSU-03012 promotes caspase-independent, PWEK-, cathepsin B-, BID- and AIF-dependent killing of transformed cells” Mol. Pharmacol. 70, 589-603
P.-H. Tseng, S.-C. Weng, J.-R. Weng, R. W. Brueggemeier, C. L. Shapiro, S. E. Dunn, M. Pollak, and C.-S. Chen (2006) “Inhibition of PDK-1/Akt Signaling overcomes Trastuzumab Resistance in HER2-Overexpressing Breast Cancer Cells” Mol. Pharmacol. 70, 1534-1541.

Z. Tong, X. Wu, C.-S. Chen, and J. P. Kehrer (2006) “Cytotoxicity of a non-cyclooxygenase-2 inhibitor derivative of celecoxib in non-small-cell lung cancer A549 cells” Lung Cancer 52, 117-124
P. Pyrko, N. Soriano, A. Kardosh, Y.-T. Liu, J. Uddin, N. A. Petasis, F. M. Hofman, C.-S. Chen, T. C Chen and A. H. Schönthal (2006) “Downregulation of survivin expression and concomitant induction of apoptosis by celecoxib and its non-cyclooxygenase-2-inhibitory analog, dimethyl-celecoxib (DMC), in tumor cells in vitro and in vivo” Mol. Cancer 5:19.

C.-C. Yang, Y.-C. Wang, S. Wei, L.-F. Lin, C.-S. Chen, C.-C. Lee, C.-C. Lin, and C.-S. Chen (2007) “Peroxisome Proliferator-Activated Receptor g-Independent Suppression of Androgen Receptor Expression by Troglitazone.  Mechanism and Pharmacological Exploitation” Cancer Res, 67, 3229-3238.

C.-S. Chen, Y.-C. Wang, H.-C. Yang, P.-H. Huang, S.K. Kulp, C.-C. Yang, Y.-S. Lu, S. Matsuyama, C.-Y. Chen, and C.-S. Chen (2007) “Histone Deacetylase Inhibitors Sensitize Prostate Cancer Cells to Agents That Produce DNA Double-Strand Breaks by Targeting Ku70 Acetylation” Cancer Res. 67, 5318-5327.

Y.-S. Lu, Y. Kashida, S.K. Kulp, J.-H. Hung, D. Wang, Z.-Z. Lin, T.-J. Chen, A.-L. Cheng, and C.-S. Chen (2007) “Efficacy of OSU-HDAC42, a novel phenylbutyrate-based histone deacetylase inhibitor, in murine models of hepatocellular carcinoma” Hepatology 46, 1119-1130.

A. M. Sargeant, R.D. Klein, R.C. Rengel, S.K. Clinton, S.K. Kulp, Y. Kashida, M. Yamaguchi, and C.-S. Chen (2007) “Chemopreventive and bioenergetic signaling effects of PDK1/Akt pathway inhibition in a transgenic mouse model of prostate cancer” Toxicol. Pathol. 35, 549-561.

J.-R. Weng, C.-H. Tsai, S. K. Kulp. D. Wang, C.-H. Lin, H.-C. Yang, Y. Ma, A. Sargeant, C.-F. Chiu, M.-H. Tsai, and C.-S. Chen (2007) “A potent indole-3-carbinol-derived antitumor agent with pleotropic effects on multiple signaling pathways in prostate cancer cells” Cancer Res. 67, 67, 7815-7824.

S. Wei, L.-F. Lin, C.-C. Yang, C.-H. Tsai, Y.-C. Wang, G.-D. Chang, H. Chen, and C.-S. Chen (2007) “Thiazolidineiones modulate the expression of b-catenin and other cell-cycle regulatory proteins by targeting the F-box proteins of SCF E3 ubiquitin ligase independently of PPARg” Mol. Pharmacol. 72, 725-733.

L. M. Porchia, M. Guerra, Y. C. Wang, Y. Zhang, A. V. Espinosa, M. Shinohara, S. K. Kulp, L. S. Kirschner, M. Saji, C.-S. Chen, and M. D. Ringel (2007) 2-amino-N-{4-[5-(2-phenanthrenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]-phenyl}acetamide (OSU-03012), a celecoxib derivative, directly targets p21-activated kinase. Mol. Pharmacol. 72(5):1124-1131.

B. J. Dewar, O. S. Gardner, C.-S. Chen, H. D. Earp, J. M. Samet, and L. M. Graves (2007) Capacitative calcium entry contributes to the differential transactivation of the epidermal growth factor receptor in response to thiazolidinediones. Mol. Pharmacol. 72:1146-1156.

P. Neviani, R. Santhanam, J. J. Oaks, A. M. Eiring, M. Notari, B. W. Blaser, S. Liu, R. Trotta, N. Muthusamy, C. Gambacorti-Passerini, B. J. Druker , J. Cortes, G. Marcucci, C.-S. Chen, N. M. Verrills , D. C. Roy, M. A. Caligiuri, C. D. Bloomfield, J. C. Byrd, and D. Perrotti (2007) FTY720, a new alternative for treating blast crisis chronic myelogenous leukemia and Philadelphia chromosome-positive acute lymphocytic leukemia. J. Clin. Invest. 117(9):2408-2421.

Y.-C. Wang, S. K. Kulp, D. Wang, C.-C Yang, A. M. Sargeant, Y. Kashida, M. Yamaguchi, G.-D. Chang, and C.-S. Chen (2008) “Targeting ER-stress and Akt signaling with OSU-03012 and gefitinib or erlotinib to overcome epidermal growth factor receptor inhibitor-resistance in non-small cell lung cancer cells with activated Akt” Cancer Res. 68, 2820-2830.

J.-H. Hung, Y.-S. Lu, Y.-C. Wang, Y.-H. Ma, D. Wang, S. K. Kulp, N. Muthusamy, J. C. Byrd, A.-L. Cheng, and C.-S. Chen (2008) “FTY720 induces apoptosis in hepatocellular carcinoma cells in part through activation of reactive oxygen species-protein kinase C-delta signaling” Cancer Res. 68, 1204-1212.

J. Yang, S. Wei, D.-S. Wang, Y.-C. Wang, S. K. Kulp, and C.-S. Chen (2008) “Pharmacological exploitation of the peroxisome proliferator-activated receptor g agonist ciglitazone to develop a novel class of androgen receptor-ablative agents” J. Med. Chem. 51, 2100-2107.

J.-R. Weng, C.-H. Tsai, S. K. Kulp, and C.-S. Chen (2008) “Indole-3-carbinol as a chemopreventive and anti-cancer agent” Cancer Lett. 262, 153-163 (Invited review).

Q. Liu, X. Zhao, F. Frissora, Y. Ma, R. Santhanam, D. Jarjoura, A. Lehman, D. Perrotti, C.-S. Chen, J. T. Dalton, N. Muthusamy, and J.C. Byrd (2008) FTY720 demonstrates promising preclinical activity for chronic lymphocytic leukemia and lymphoblastic leukemia/lymphoma. Blood 111(1):275-284.

M.A. Park, A. Yacoub, M. Rahmani, G. Zhang, L. Hart, M. P. Hagan, S. K. Calderwood, M. Y. Sherman, C. Koumenis, S. Spiegel, C.-S. Chen, M. Graf, D. T. Curiel, P. B. Fisher, S. Grant and P. Dent (2008) OSU-03012 stimulates PKR-like endoplasmic reticulum-dependent increases in 70-kDa heat shock protein expression, attenuating its lethal actions in transformed cells. Mol. Pharmacol. 73(4):1168-1184.

S.-C. Weng, Y. Kashida, S. K. Kulp. D. Wang, R. W. Brueggemeier, C. L. Shapiro, and C.-S. Chen (2008) “Sensitizing estrogen receptor-negative cancer cells to tamoxifen with OSU-03012, a novel celecoxib-derived PDK-1/Akt signaling inhibitor” Mol. Cancer Ther. 7, 800-808.

A. M. Sargeant, R. C. Ringel, S. K. Kulp, R. D. Klein, S. K. Clinton, Y.-C. Wang, and C.-S. Chen (2008) “Dietary Intake of OSU-HDAC42, a histone deacetylase inhibitor, blocks prostate tumor progression in the TRAMP model” Cancer Res. 68, 3999-4009.

S. Wei, H.-C. Yang, H.-C. Chuang, J. Yang, S. K. Kulp, P.-J. Lu. M.-D. Lai, and C.-S. Chen (2008) “A novel mechanism by which thiazolidinediones facilitate the proteasomal degradation of cyclin D1 in cancer cells” J. Biol. Chem. 283, 26759-26770

S. Wei. J. Yang, S.-L. Lee, S. K. Kulp, and C.-S. Chen (2009) “PPARg-independent antitumor effects of thiazolidinediones” Cancer Lett. 276, 119-24 (invited review)

P.-H. Huang, D. Wang. H.-C. Chuang, S. Wei, S. K. Kulp, and C.-S. Chen (2009) “á-Tocopheryl succinate and derivatives mediate the transcriptional repression of androgen receptor in prostate cancer cells by targeting the PP2A-JNK-Sp1 signaling axis” Carcinogenesis 30, 1125-1131

S. Wei, H.-C. Chuang, W.-C. Tsai. H.-C. Yang. S.-R. Ho, A. J. Paterson, S. K. Kulp, and C.-S. Chen (2009) “Thiazolidinediones mimic glucose starvation in facilitating Sp1 degradation through the upregulation of b-TrCP’ Mol. Pharmacol. 76, 47-57

Y. Yang, C. Bulch, S. K. Kulp, M. Mand, K. Nephew, and C.-S. Chen (2009) “A rationally designed histone deacetylase inhibitor with unique antitumor activity against ovarian cancer” Neoplasia 11, 552-583

J.-R. Weng, C.-H. Tsai, H. Omar, A. M. Sargeant, D. Wang, S. K. Kulp, C. L. Shapiro, and C.-S. Chen (2009) “OSU-A9, a Potent Indole-3-Carbinol Derivative, Suppresses Breast Tumor Growth by Targeting the Akt-NF-kB Pathway and Stress Response Signaling” Carcinogenesis 30,in press

D. Wang, H.-C. Chuang, S.-C. Weng, P.-H. Huang, H.-Y. Hsieh, S. K. Kulp, and C.-S. Chen (2009) “a-Tocopheryl Succinate as a Scaffold to Develop Potent Inhibitors of Breast Cancer Cell Adhesion” J. Med. Chem. 52, in press

H. A. Omar, A. M. Sargeant, J.-R. Weng, D. Wang, S. K. Kulp, T. Patel, C.-S. Chen (2009) “Targeting of the Akt-NF-kB Signaling Network by OSU-A9, a Novel Indole-3-Carbinol Derivative, in a Mouse Model of Hepatocellular Carcinoma” Mol. Pharmacol. 76, in press

H.-C. Chiu, J. Yang, S. Soni, S. K. Kulp, J. S. Gunn, L. S. Schlesinger, C.-S. Chen (2009) “Pharmacological Exploitation of an Off-Target Antibacterial Effect of the Cyclooxygenase-2 Inhibitor Celecoxib against Francisella tularensis” Antimicrob. Agents Chemother. Accepted for publication. AAC.00048-09 [pii] 10.1128/AAC.00048-09

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