Scientific publications

Belinostat

Review papers 2011

• Molife LR, de Bono JS. Belinostat: clinical applications in solid tumors and lymphoma. Expert Opin Investig Drugs. 2011 Dec;20(12):1723-32.

• Howman RA, Prince HM. New drug therapies in peripheral T-cell lymphoma. Expert Rev Anticancer Ther. 2011 Mar;11(3):457-72.

• Hideshima T, Richardson PG, Anderson KC. Mechanism of action of proteasome inhibitors and deacetylase inhibitors and the biological basis of synergy in multiple myeloma.Mol Cancer Ther. 2011 Nov;10(11):2034-42.
  
  

• Atadja PW. HDAC inhibitors and cancer therapy. Prog Drug Res. 2011;67:175-95.
  

• Roncolato F, Gazzola A, Zinzani PL, Pileri SA, Piccaluga PP. Targeted molecular therapy in peripheral T-cell lymphomas.Expert Rev Hematol. 2011 Oct;4(5):551-62.

• Wong HK, Mishra A, Hake T, Porcu P. Evolving insights in the pathogenesis and therapy of cutaneous T-cell lymphoma (mycosis fungoides and Sezary syndrome).Br J Haematol. 2011 Oct;155(2):150-66.
  

• Tse E, Kwong YL. Treatment algorithms for mature T-cell and natural killer-cell neoplasms. Future Oncol. 2011 Sep;7(9):1101-12.

• Kwa FA, Balcerczyk A, Licciardi P, El-Osta A, Karagiannis TC. Chromatin modifying agents - the cutting edge of anticancer therapy.Drug Discov Today. 2011 Jul;16(13-14):543-7.
  

• Sawas A, Diefenbach C, O'Connor OA. New therapeutic targets and drugs in non-Hodgkin's lymphoma. Curr Opin Hematol. 2011 Jul;18(4):280-7.

• Stintzing S, Kemmerling R, Kiesslich T, Alinger B, Ocker M, Neureiter D. Myelodysplastic syndrome and histone deacetylase inhibitors: "to be or not to be acetylated"?J Biomed Biotechnol. 2011;2011:214143.

• Gisselbrecht C. Peripheral T-cell lymphoma: Tailoring of new drugs to the histology? Oncologie 2011;13:9 (565-70).

• Foss FM, Zinzani PL, Vose JM, Gascoyne RD, Rosen ST, Tobinai K. Peripheral T-cell lymphoma. Blood. 2011 Jun 23;117(25):6756-67.

• Martinet N, Bertrand P. Interpreting clinical assays for histone deacetylase inhibitors. Cancer Manag Res. 2011;3:117-41.

• Petrella A, Fontanella B, Carratù A, Bizzarro V, Rodriquez M, Parente L. Histone deacetylase inhibitors in the treatment of hematological malignancies.Mini Rev Med Chem. 2011 Jun;11(6):519-27.

• Mahadevan D, Fisher RI. Novel therapeutics for aggressive non-Hodgkin's lymphoma.J Clin Oncol. 2011 May 10;29(14):1876-84.

• Venugopal B, Evans TR. Developing histone deacetylase inhibitors as anti-cancer therapeutics. Curr Med Chem. 2011;18(11):1658-71.

• Thaler F. and Minucci S. Next generation histone deacetylase inhibitors: the answer to the search for optimized epigenetic therapies? Expert Opinion on Drug Discovery 2011 6:4 (393-404).

• Horwitz SM. The emerging role of histone deacetylase inhibitors in treating T-cell lymphomas. Curr Hematol Malig Rep. 2011 Mar;6(1):67-72.

• Federico M, Bagella L. Histone deacetylase inhibitors in the treatment of hematological malignancies and solid tumors. J Biomed Biotechnol. 2011;2011:475641.

• Quintás-Cardama A, Santos FP, Garcia-Manero G. Histone deacetylase inhibitors for the treatment of myelodysplastic syndrome and acute myeloid leukemia.Leukemia. 2011 Feb;25(2):226-35.

• Detchokul S, Frauman AG. Recent developments in prostate cancer biomarker research: therapeutic implications.Br J Clin Pharmacol. 2011 Feb;71(2):157-74.

• Thurn KT, Thomas S, Moore A, Munster PN. Rational therapeutic combinations with histone deacetylase inhibitors for the treatment of cancer. Future Oncol. 2011 Feb;7(2):263-83.

• Carafa V, Nebbioso A, Altucci L. Histone deacetylase inhibitors: recent insights from basic to clinical knowledge & patenting of anti-cancer actions. Recent Pat Anticancer Drug Discov. 2011 Jan;6(1):131-45.

Clinical research 2011

• Cashen A, Juckett M, Jumonville A, Litzow M, Flynn PJ, Eckardt J, Laplant B, Laumann K, Erlichman C, Dipersio J. Phase II study of the histone deacetylase inhibitor belinostat (PXD101) for the treatment of myelodysplastic syndrome (MDS).Ann Hematol. 2012 Jan;91(1):33-8. [Epub 2011 May 3]

• Giaccone G, Rajan A, Berman A, Kelly RJ, Szabo E, Lopez-Chavez A, Trepel J, Lee MJ, Cao L, Espinoza-Delgado I, Spittler J, Loehrer PJ Sr. Phase II study of belinostat in patients with recurrent or refractory advanced thymic epithelial tumors.J Clin Oncol. 2011 May 20;29(15):2052-9.

• Steele NL, Plumb JA, Vidal L, Tjørnelund J, Knoblauch P, Buhl-Jensen P, Molife R, Brown R, de Bono JS, Evans TR. Pharmacokinetic and pharmacodynamic properties of an oral formulation of the histone deacetylase inhibitor Belinostat (PXD101).Cancer Chemother Pharmacol. 2011 Jun;67(6):1273-9.

• Force J, Rajan A, Dombi E, Steinberg SM, Giaccone G. Assessment of objective responses using volumetric evaluation in advanced thymic malignancies and metastatic non-small cell lung cancer.J Thorac Oncol. 2011 Jul;6(7):1267-73.

Pre-clinical research 2011

• Beloueche-Babari M, Arunan V, Troy H, Te Poele RH, Wong Te Fong AC, Jackson LE, Payne GS, Griffiths JR, Judson IR, Workman P, Leach MO, Chung YL. Histone deacetylase inhibition increases levels of choline kinase alpha and phosphocholine facilitating non-invasive imaging in human cancers.Cancer Res. 2012 Jan 30 [Epub 2011 Dec 22]

• Ghosh SK, Perrine SP, Williams RM, Faller DV. Histone deacetylase inhibitors are potent inducers of gene expression in latent EBV and sensitize lymphoma cells to nucleoside anti-viral agents.Blood.2012 Jan;119(4):1008-17 [Epub 2011 Dec 7]

• Gravina GL, Marampon F, Giusti I, Carosa E, Di Sante S, Ricevuto E, Dolo V,Tombolini V, Jannini EA, Festuccia C. Differential effects of PXD101 (belinostat) on androgen-dependent and androgen-independent prostate cancer models.Int J Oncol. 2012 Mar;40(3):711-20. doi: 10.3892/ijo.2011.1270 [Epub 2011 Nov 23]

• Luchenko VL, Salcido CD, Zhang Y, Agama K, Komlodi-Pasztor E, Murphy RF, Giaccone G, Pommier Y, Bates SE, Varticovski L. Schedule-dependent synergy of histone deacetylase inhibitors with DNA damaging agents in small cell lung cancer.Cell Cycle. 2011 Sep 15;10(18):3119-28.

• Hwang JJ, Kim YS, Kim T, Kim MJ, Jeong IG, Lee JH, Choi J, Jang S, Ro S, Kim CS. A novel histone deacetylase inhibitor, CG200745, potentiates anticancer effect of docetaxel in prostate cancer via decreasing Mcl-1 and Bcl-(XL).Invest New Drugs. 2011 Jul 20.

• Li X. Epigenetics and autosomal dominant polycystic kidney disease.Biochim Biophys Acta. 2011 Oct;1812(10):1213-8

• Rikiishi H. Autophagic and apoptotic effects of HDAC inhibitors on cancer cells. J Biomed Biotechnol. 2011;2011:830260.

• Chowdhury S, Howell GM, Teggart CA, Chowdhury A, Person JJ, Bowers DM, Brattain MG. Histone deacetylase inhibitor belinostat represses survivin expression through reactivation of transforming growth factor beta (TGFbeta) receptor II leading to cancer cell death.J Biol Chem. 2011 Sep 2;286(35):30937-48.

• Spratlin JL, Pitts TM, Kulikowski GN, Morelli MP, Tentler JJ, Serkova NJ, Eckhardt SG. Synergistic activity of histone deacetylase and proteasome inhibition against pancreatic and hepatocellular cancer cell lines.Anticancer Res. 2011 Apr;31(4):1093-103.

• Dai Y, Chen S, Wang L, Pei XY, Kramer LB, Dent P, Grant S. Bortezomib interacts synergistically with belinostat in human acute myeloid leukaemia and acute lymphoblastic leukaemia cells in association with perturbation in NF-κB and Bim.Br J Haematol. 2011 Mar 6. doi: 10.1111/j.1365-2141.2011.08591.x. [Epub ahead of print]

• Na YS, Jung KA, Kim SM, Hong YS, Ryu MH, Jang SJ, Moon DH, Cho DH, Kim JC, Lee JS, Kim TW. The histone deacetylase inhibitor PXD101 increases the efficacy of irinotecan in in vitro and in vivo colon cancer models.Cancer Chemother Pharmacol. 2011 Aug;68(2):389-98.

• Matalon S, Rasmussen TA, Dinarello CA. Histone deacetylase inhibitors for purging HIV-1 from the latent reservoir.Mol Med. 2011 May-Jun;17(5-6):466-72.

Abstracts on belinostat presented at scientific meetings

Clinical research 2011

• Preliminary Results of An Ongoing Phase I Trial of Oral Belinostat a Novel Histone Deacetylase Inhibitor in Patients with Lymphoid Malignancies. Jasmine M. Zain, MD, Francine M. Foss, MD, Catherine S. Diefenbach, MD, Daniel Petrylak, MD^*, Ameet Narwal, Ellen Neylon, NP, RN, BSN, OCN, Poul Knoblauch and Owen A. O'Connor, MD, PhD^.. The American Society of Hematology 53rd annual 2011 meeting 10-13 December San Diego

• Phase I Trial of Belinostat and Bortezomib in Patients with Relapsed or Refractory Acute Leukemia, Myelodysplastic Syndrome, or Chronic Myelogenous Leukemia in Blast Crisis. Beata Holkova, MD, Mary Beth Tombes, RN, Ellen Shrader, Sheryl S. Cooke, RN, Wen Wan, PhD, Heidi Sankala, PhD, Maciej Kmieciak, PhD, John D. Roberts, MD, Guillermo Garcia-Manero and Steven Grant, MDPhD. The American Society of Hematology 53rd annual 2011 meeting 10-13 December San Diego.

• A phase II study of epigenetic therapy using belinostat for patients with unresectable hepatocellular carcinoma: a multicenter study of the Mayo Phase 2 Consortium (P2C) and the Cancer Therapeutics Research Group (CTRG). W. Yeo, H.C. Chung, S.L. Chan, L.Z. Wang, R. Lim, J. Picus, M. Boyer, C. Erlichman, A.T.C. Chan, B.C. Goh. Poster European Multidisciplinary Cancer Congress 2011, 23 - 27th September Stockholm.

• Belinostat in Combination With Carboplatin and Paclitaxel (BelCaP) for Treatment of Bladder Cancer - a Pharmacokinetic Study of Exposure to Belinostat and Its MetabolitesR.J. Jones, J. Tjørnelund, K.D. Erichsen, L. Sengeløv, J. De Bono^. European Multidisciplinary Cancer Congress 2011, 23 - 27th September Stockholm

• A phase I and pharmacodynamic (PD) study of the histone deacetylase (HDAC) inhibitor belinostat (BEL) plus azacitidine (AZC) in advanced myeloid malignancies. O. Odenike, L. A. Godley, J. Madzo, T. Karrison, M. Green, A. S. Artz, R. J. Mattison, K. W. L. Yee, M. Bennett, N. Fulton, G. Koval, G. Malnassy, R. A. Larson, M. J. Ratain, W. Stock Oral presentation at the Annual Meeting of the American Society of Clinical Oncology (ASCO) June 3-7, 2011, Chicago.

• Management of thymic epithelial tumors (TETs) at the National Cancer Institute (NCI). A. Rajan, R. J. Kelly, A. Lopez-Chavez, C. A. Carter, E. Szabo, B. Scepura, M. J. Manu, A. W. Berman, G. Giaccone. Annual Meeting of the American Society of Clinical Oncology (ASCO) June 3-7, 2011, Chicago.

Pre-clinical research 2011

• Combination of Epigenetic Agents Synergistically Reverse the Malignant Phenotype in Models of T-Cell Lymphoma. Enrica Marchi, MD, PhD. Matko Kalac, MD, PhD. Danielle C Bongero, Christine M McIntosh, Laura K Fogli, Luigi Scotto, PhD, Maura Rossi, PhD, Pier Luigi Zinzani, MD, PhD, Stefano Pileri, MD, Pier Paolo Piccaluga Sr., MD, PhD5 and Owen A. O'Connor, MD, PhD.The American Society of Hematology 53rd annual 2011 meeting 10-13 December San Diego.

• Therapeutic Targeting of the Bcl-6 : p53 Axis with Histone Deacetylase Inhibitors in Diffuse Large B-Cell Lymphoma . Jennifer E Amengual, MD, Matko Kalac, MD, PhD, Luigi Scotto, PhD, Patrick A Sleckman, Enrica Marchi, MD, PhD, Changchun Deng, MD, PhD, Danielle C Bongero, Salvia Jain, MD1, Jairo Baquero Buitrago1 and Owen A. O'Connor, MD, PhD. The American Society of Hematology 53rd annual 2011 meeting 10-13 December San Diego.

• Changes in [18]F-FLT and [18]F-FDG positron emission tomography following treatment with belinostat alone and in combination with paclitaxel/carboplatin in human ovary cancer xenografts in mice. Mette Munk Jensen, Kamille Dumong Erichsen, Camilla Bardram Johnbeck, Fredrik Björkling, Jacob Madsen, Peter Buhl Jensen, Maxwell Sehested, Liselotte Højgaard¹, Andreas Kjær. American Association for Cancer Research annual meeting 2011 April 2-6, 2011 Orlando.

• Treatment of human medullary thyroid carcinoma (MTC) with either proteasome (Pr) or histone deacetylase (HDAC) inhibitors leads to a fall in RET mRNA levels and, in turn, a decrease in RET protein expression providing alternate strategies to reduce RET expression in a tyrosine-kinase driven disease . Marianne S. Poruchynsky, Ann W. Gramza, Samuel A. Wells, Tito Fojo. NIH-NCI, Bethesda, MD American Association for Cancer Research annual meeting 2011 April 2-6, 2011 Orlando.

• Pre-treatment with histone deacetylase inhibitor HDACI) synergizes the anti-cancer effect of sorafenib in renal cell carcinoma cells. Dong Eun Kim, Mi Joung Kim, Sejin Jang, Je-Hwan Lee, Jene Choi, Seonggu Ro, Choung-Soo Kim, Jung Jin Hwang. American Association for Cancer Research annual meeting 2011 April 2-6, 2011 Orlando.

• Non-invasive metabolic biomarkers of histone deacetylase inhibition in human colon cancer cells and tumors. Mounia Beloueche-Babari, Vaitha Arunan, Helen Troy, L. Elizabeth Jackson, Anne-Christine Wong, Paul Workman, Ian Judson, John R. Griffiths, Martin O. Leach, Yuen-Li Chung. American Association for Cancer Research annual meeting 2011 April 2-6, 2011 Orlando.

• The cellular and genomic response to histone deacetylase inhibitors in diffuse large b-cell lymphoma. Ana A. Tula-Sanchez, Mary E. Klein, Catharine L. Smith, Lingling An. University of Arizona, Tucson, AZ. American Association for Cancer Research annual meeting 2011 April 2-6, 2011 Orlando.

• Histone deacetylase inhibitor potentiates sorafenib-induced cell death in renal cell carcinoma cell lines. Hong S., You D., Kim K.H., Jeong I.G., Kim M.J., Kim D., Hwang J.J., Jang S., Lee J.-H., Choi J., Ro S. and Kim C.-S.Annual Meeting of the American Urological Association 2011 May 14-19, 2011 Washington DC.

• Nanoparticle delivery of the histone deacetylase inhibitor PXD101 facilitates bladder cancer cell uptake and cytotoxicity. Kaimakliotis H.Z., Martin D.T., Hoimes C.J., Cheng C.C., Liu J., Kelly W.K., Tew G.N., Mark Saltzman and Weiss R.M. Annual Meeting of the American Urological Association 2011 May 14-19, 2011 Washington DC.

Belinostat publications 1999-2010:

1. Beck HC, Petersen J, Nielsen SJ, Morszeck C, Jensen PB, Sehested M, Grauslund M. Proteomic profiling of human colon cancer cells treated with the histone deacetylase inhibitor belinostat. Electrophoresis. 2010 Aug;31(16):2714-21. PMID: 20717991
2. Steele NL, Plumb JA, Vidal L, Tjørnelund J, Knoblauch P, Buhl-Jensen P, Molife R, Brown R, de Bono JS, Evans TR. Pharmacokinetic and pharmacodynamic properties of an oral formulation of the histone deacetylase inhibitor Belinostat (PXD101). Cancer Chemother Pharmacol. 2010 Aug 13. [Epub ahead of print]. PMID: 20706839
3. Gimsing P. Belinostat: a new broad acting antineoplastic histone deacetylase inhibitor. Expert Opin Investig Drugs. 2009 Apr;18(4):501-8. PMID: 19335278
4. Steele N, Finn P, Brown R, Plumb JA. Combined inhibition of DNA methylation and histone acetylation enhances gene re-expression and drug sensitivity in vivo. Br J Cancer. 2009 March 10; 100(5): 758-763. PMID: 19259094
5. Andrianov V, Gailite V, Lola D, Loza E, Semenikhina V, Kalvinsh I, Finn P, Petersen KD, Ritchie JW, Khan N, Tumber A, Collins LS, Vadlamudi SM, Björkling F, Sehested M. Novel amide derivatives as inhibitors of histone deacetylase: Design, synthesis and SAR. Eur J Med Chem. 2009 Mar;44(3):1067-85. PMID: 18672316
6. Marquard L, Gjerdrum LM, Christensen IJ, Jensen PB, Sehested M, Ralfkiaer E. Prognostic significance of the therapeutic targets histone deacetylase 1, 2, 6 and acetylated histone H4 in cutaneous T-cell lymphoma. Histopathology. 2008 Sep;53(3):267-77. PMID: 18671804
7. Dejligbjerg M, Grauslund M, Litman T, Collins L, Qian X, Jeffers M, Lichenstein H, Jensen PB, Sehested M. Differential effects of class I isoform histone deacetylase depletion and enzymatic inhibition by belinostat or valproic acid in HeLa cells. Mol Cancer. 2008 Sep 12;7:70. PMID: 18789133
8. Gimsing P, Hansen M, Knudsen LM, Knoblauch P, Christensen IJ, Ooi CE, Buhl Jensen P. A phase I clinical trial of the histone deacetylase inhibitor belinostat (PXD101) in patients with advanced haematological neoplasia. Eur J Haematol. 2008 Sep;81(3):170-6. Epub 2008 May 28. PMID: 18510700
9. Warren KE, McCully C, Dvinge H, Tjørnelund J, Sehested M, Lichenstein HS, Balis FM. Plasma and cerebrospinal fluid pharmacokinetics of the histone deacetylase inhibitor, belinostat (PXD101), in non-human primates. Cancer Chemother Pharmacol. 2008 Aug;62(3):433-7. PMID: 17960383
10. Marquard L, Petersen KD, Persson M, Hoff KD, Jensen PB, Sehested M. Monitoring the effect of belinostat in solid tumors by H4 acetylation. APMIS. 2008 May;116(5):382-92. PMID: 18452428
11. Qian X, Ara G, Mills E, LaRochelle WJ, Lichenstein HS, Jeffers M. Activity of the histone deacetylase inhibitor belinostat (PXD101) in preclinical models of prostate cancer. Int J Cancer. 2008 Mar 15;122(6):1400-10. PMID: 18027850
12. Steele NL, Plumb JA, Vidal L, Tjørnelund J, Knoblauch P, Rasmussen A, Ooi CE, Buhl Jensen P, Brown R, Evans TR, DeBono JS. A phase 1 pharmacokinetic and pharmacodynamic study of the histone deacetylase inhibitor belinostat in patients with advanced solid tumors. Clin Cancer Res. 2008 Feb 1;14(3):804-10. PMID: 18245542
13. Khan N, Jeffers M, Kumar S, Hackett C, Boldog F, Khramtsov N, Qian X, Mills E, Berghs SC, Carey N, Finn PW, Collins LS, Tumber A, Ritchie JW, Jensen PB, Lichenstein HS, Sehested M. Determination of the class and isoform selectivity of small-molecule histone deacetylase inhibitors. Biochem J. 2008 Jan 15;409(2):581-9. PMID: 17868033
14. Dai Y, Chen S, Kramer LB, Funk VL, Dent P, Grant S. Interactions between Bortezomib and Romidepsin and Belinostat in Chronic Lymphocytic Leukemia Cells. Clin Cancer Res. 2008 Jan 15;14(2):549-58. PMID: 18223231
15. Dejligbjerg M, Grauslund M, Christensen IJ, Tjørnelund J, Buhl Jensen P, Sehested M. Identification of predictive biomarkers for the histone deacetylase inhibitor belinostat in a panel of human cancer cell lines. Cancer Biomark. 2008;4(2):101-9. PMID: 18503161
16. Stapnes C, Ryningen A, Hatfield K, Øyan AM, Eide GE, Corbascio M, Kalland KH, Gjertsen BT, Bruserud Ø. Functional characteristics and gene expression profiles of primary acute myeloid leukaemia cells identify patient subgroups that differ in susceptibility to histone deacetylase inhibitors. Int J Oncol. 2007 Dec;31(6):1529-38. PMID: 17982680
17. Feng R, Oton A, Mapara MY, Anderson G, Belani C, Lentzsch S. The histone deacetylase inhibitor, PXD101, potentiates bortezomib-induced anti-multiple myeloma effect by induction of oxidative stress and DNA damage. Br J Haematol. 2007 Nov;139(3):385-97. PMID: 17910628
18. Buckley MT, Yoon J, Yee H, Chiriboga L, Liebes L, Ara G, Qian X, Bajorin DF, Sun TT, Wu XR, Osman I. The histone deacetylase inhibitor belinostat (PXD101) suppresses bladder cancer cell growth in vitro and in vivo. J Transl Med. 2007 Oct 12;5:49. PMID: 17935615
19. Tumber A, Collins LS, Petersen KD, Thougaard A, Christiansen SJ, Dejligbjerg M, Jensen PB, Sehested M, Ritchie JW. The histone deacetylase inhibitor PXD101 synergises with 5-fluorouracil to inhibit colon cancer cell growth in vitro and in vivo. Cancer Chemother Pharmacol. 2007 Jul;60(2):275-83. PMID: 17124594
20. Huh YH, Ryu JH, Chun JS. Regulation of type II collagen expression by histone deacetylase in articular chondrocytes. J Biol Chem. 2007 Jun;8;282(23):17123-31. PMID: 17428794
21. Zhang N, Goh BC, Khoo YM, Yeo W, Lee HS. A simple and sensitive high-performance liquid chromatographic method for quantification of PXD101, a histone deacetylase inhibitor in human plasma. Ther Drug Monit. 2007 Apr;29(2):231-5. PMID: 17417079
22. Duan J, Friedman J, Nottingham L, Chen Z, Ara G, Van Waes C. Nuclear factor-kappaB p65 small interfering RNA or proteasome inhibitor bortezomib sensitizes head and neck squamous cell carcinomas to classic histone deacetylase inhibitors and novel histone deacetylase inhibitor PXD101. Mol Cancer Ther. 2007 Jan;6(1):37-50. PMID: 17237265
23. Qian X, LaRochelle WJ, Ara G, Wu F, Petersen KD, Thougaard A, Sehested M, Lichenstein HS, Jeffers M. Activity of PXD101, a histone deacetylase inhibitor, in preclinical ovarian cancer studies. Mol Cancer Ther. 2006 Aug;5(8):2086-95. PMID: 16928830
24. Beck HC, Nielsen EC, Matthiesen R, Jensen LH, Sehested M, Finn P, Grauslund M, Hansen AM, Jensen ON. Quantitative Proteomic Analysis of Post-translational Modifications of Human Histones. Mol Cell Proteomics. 2006 Jul;5(7):1314-25. Epub 2006 Apr 20.
25. Finn PW, Bandara M, Butcher C, Finn A, Hollinshead R, Khan N, Law N, Murthy S, Romero R, Watkins C, Andrianov V,. Bokaldere RM, Dikovska K, Gailite V, Loza E, Piskunova I, Starchenkov I, Vorona M, Kalvinsh I. Novel Sulfonamide Derivatives as Inhibitors of Histone Deacetylase. Helvita Chemica Acta. 2005; 88(7); 1630-57
26. La Thangue NB. A mis-matched role for Bcl2. Nature Cell Biology 2005; 7:101-102.
27. Smith L, La Thangue NB. Signalling DNA damage by regulating p53 co-factor activity. Cell Cycle 2005 Jan;4(1):30-2. PMID: 15655373
28. Kerr DJ, La Thangue NB. Signal transduction blockade and cancer: combination therapy or multi-targeted inhibitors? Ann Oncol 2004 Dec; 15(12):1727-29. PMID: 15550576
29. Plumb JA, Steele N, Finn PW, Brown R. Epigenetic approaches to Cancer Therapy. Biochem Soc Trans 2004 Dec;32(Pt6):1095-97. PMID: 15506976
30. La Thangue NB. Histone deacetylase inhibitors and cancer therapy. J Chemother 2004 Nov; 16 Suppl 4:64-6. PMID: 15688613
31. Demonacos C, Krstic-Demonacos M., Smith L, Xu, D, O'Connor P, Jansson M, La Thangue, NB. A new effector pathway links ATM kinase with the DNA damage response. Nat Cell Biol 2004 Oct; 6 (10):968-76. PMID: 15448695
32. McLaughlin F, La Thangue NB. Histone deacetylase inhibitors open new doors in cancer. Biochem Pharmacol 2004 Sep 15; 68(6):1139-44. PMID: 15313411
33. Stevens C, La Thangue NB. The emerging role of E2F-1 in the DNA damage response and checkpoint control. DNA Repair (Amst.) 2004 Aug-Sep; 3(8-9):1071-79. PMID: 15279795
34. Logan N, Delavaine L, Reilly C, Wilson J, Brummelkamp TR, Hijmans EM, Bernards R, La Thangue NB. E2F-7: a distinctive E2F family member with an unusual organization of DNA binding domains. Oncogene 2004 Jul 1; 23(30):5138-50. PMID: 15133492
35. McLaughlin F, La Thangue NB. Histone deacetylase inhibitors in psoriasis therapy. Curr Drug Targets Inflamm Allergy 2004 Jun;3(2): 213-9. PMID: 15180476
36. Stevens C, La Thangue NB. A new role for E2F-1 in checkpoint control. Cell Cycle. 2003 Sep-Oct; 2(5):435-7. PMID: 12963836
37. McLaughlin F, Finn PW, La Thangue NB. The cell cycle, chromatin and cancer: mechanism-based therapeutics come of age. Drug Discov Today 2003 Sep 1; 8(17):793-802. PMID: 12946642
38. Plumb JA, Finn PW, Williams RJ, Bandara MW, Romero MR, Watkins CJ, La Thangue NB, Brown R. Pharmacodynamic response and inhibition of growth of human tumour xenografts by the novel histone deacetylase inhibitor PXD101. Mol Cancer Ther. 2003 Aug; 2:721-28. PMID: 12939461
39. La Thangue NB. The yin and yang of E2F-1: balancing life and death. Nat Cell Biol. 2003 Jul; 5:587-589. PMID: 12833056
40. Stevens C, Smith L, La Thangue NB. Chk2 activates E2F-1 in response to DNA damage. Natur Cell Biol 2003 May; 5:401-9. PMID: 12717439
41. Stevens C, La Thangue NB. E2F and cell cycle control: a double edged sword. Arch Biochem Biophys 2003 Apr 15;412(2):157-69. PMID: 12667479
42. La Thangue NB. Theoretical foundations in cancer chemotherapy. Enc Mol Cell Biol Mol Med. 2003;171-189.
43. Demonacos C, La Thangue NB. Drug discovery and the p53 family. Prog Cell Cycle Res. 2003; 5:375-82. PMID: 14593732
44. La Thangue NB. Chromatin control - a place for E2F and Myc to meet. Science 2002 May 10; 296(5570):1034-35. PMID: 12004105
45. Loughran Ö, La Thangue NB. E2F: a family of transcription factors implicated in cell cycle control. Curr Biol 2002; 12:R377.
46. Mason S, Loughran Ö, La Thangue NB. p14^ARF regulates E2F activity. Oncogene 2002 Jun 20;21(27):4220-30. PMID: 12082609
47. McLaughlin F, La Thangue NB. Tumour classification for tailored cancer therapy. Annual Reports in Med. Chem. 2002; 37:225-235.
48. Bandara LR, La Thangue NB. Targets for cancer chemotherapy: Transcription factors and other nuclear proteins. Humana Press Eds. 2002.
49. Chan HM, Smith L, La Thangue NB. Role of LXCXE motif-dependent interactions in the activity of the retinoblastoma protein. Oncogene 2001 Sep 27; 20(43):6152-63. PMID: 11593423
50. Demonacos C, Krstic-Demonacos M, La Thangue NB. A novel TPR-motif co-factor contributes to p300 activity in the p53 response. Mol Cell. 2001 Jul; 8(1):71-84. PMID: 11511361
51. Chan HM, Krstic-Demonacos M, Smith L, Demonacos C, La Thangue NB. Acetylation control of the retinoblastoma tumour suppressor protein. Nat Cell Biol. 2001 Jul; 3(7):667-74. PMID: 11433299
52. Chan H-M, La Thangue NB. p300/CBP proteins: HATs for transcriptional bridges and scaffolds. J Cell Sci. 2001 Jul;114(Pt13):2363-73. PMID: 11559745
53. Chan HM, Shikama N, La Thangue NB. Control of gene expression and the cell cycle. Essays Biochem 2001;37: 87-96. PMID: 11758459
54. Shikama N, Chan H-M, Smith L, Krstic-Demonacos M, Lee C-W, Cairns W, La Thangue NB. Functional interaction between nucleosome assembly proteins and p300/CBP co-activators. Mol Cell Biol 2000 Dec; 20(23):8933-43. PMID: 11073993
55. Clark W, Black EJ, MacLaren A, Kruse U, La Thangue NB, Vogt PK, Gillespie DAF. v-Jun overrides the mitogen dependence of S-phase entry by deregulating retinoblastoma protein phosphorylation and E2F-pocket protein interactions as a consequence of enhanced cyclinE-cdk2 catalytic activity. Mol Cell Biol. 2000 Apr; 20(7):2529-42. PMID: 10713176
56. Morris L, Allen KE, La Thangue NB. Regulation of E2F transcription by cyclinE/cdk2 kinase mediated through p300/CBP co-activators. Nat Cell Biol 2000 Apr; 2(4):232-9. PMID: 10783242
57. Loughran Ö, La Thangue NB. Apoptotic and growth-promoting activity of E2F modulated by MDM2. Mol Cell Biol 2000 Mar; 20(6):2186-97. PMID: 10688665
58. Chan H-M, La Thangue NB. Regulation of the retinoblastoma protein. Cancer Encyclopedia 2000, Springer Verlag.
59. La Valle SM, Finn PW, Kavraki LE, Latombe J-C. A Randomized Kinematics-Based Approach to Pharmacophore-Constrained Conformational Search and Database Screening. Journal of Computational Chemisty 2000; 21:731-747.
60. Brooks G, La Thangue NB. Drug discovery and the cell cycle: The promise and the hope. Drug Discov Today 1999 Oct; 4(10):455-64. PMID: 10481141
61. Delavaine L, La Thangue NB. Control of E2F activity by p21Waf1/Cip1. Oncogene 1999 Sep 23; 18(39):5381-92. PMID: 10498892
62. Shikama N, Lee C-W, Delavaine S, France J, Lyon W, Krstic-Demonacos M, La Thangue NB. A novel co-factor for p300 that regulates the p53 response. Mol Cell 1999 Sep; 4(3):365-76. PMID: 10518217
63. Lee C-W, La Thangue NB. Promoter specificity and stability control of the p53-related protein p73. Oncogene 1999 Jul 22; 18(29):4171-81. PMID: 10435630
64. De la Luna S, Allen KE, Mason SL, La Thangue NB. Integration of a growth-suppressing BTB/POZ domain protein with the DP component of the E2F transcription factor. EMBO J. 1999 Jan 4; 18(1):212-28. PMID: 9878064

Dexrazoxane

1. Langer SW. Extravasation of chemotherapy. Curr Oncol Rep. 2010 Jul;12(4):242-6. Review. PMID: 20480268
2. Thougaard AV, Langer SW, Hainau B, Grauslund M, Juhl BR, Jensen PB, Sehested M. A murine experimental anthracycline extravasation model: pathology and study of the involvement of topoisomerase II alpha and iron in the mechanism of tissue damage. Toxicology. 2010 Feb 28;269(1):67-72. PMID: 20079798
3. Langer SW, Sehested M, Jensen PB. Anthracycline extravasation: a comprehensive review of experimental and clinical treatments. Tumori. 2009 May-Jun;95(3):273-82. PMID: 19688963
4. Langer SW. Dexrazoxane for anthracycline extravasation. Expert Rev Anticancer Ther. 2007 Aug;7(8):1081-8. Review. PMID: 18028016
5. Mouridsen HT, Langer SW, Buter J, Eidtmann H, Rosti G, de Wit M, Knoblauch P, Rasmussen A, Dahlstrøm K, Jensen PB, Giaccone G. Treatment of anthracycline extravasation with Savene (dexrazoxane): results from two prospective clinical multicentre studies. Ann Oncol. 2007 Mar;18(3):546-50. PMID: 17185744
6. Grauslund M, Thougaard AV, Füchtbauer A, Hofland KF, Hjorth PH, Jensen PB, Sehested M, Füchtbauer EM, Jensen LH. A mouse model for studying the interaction of bisdioxopiperazines with topoisomerase IIalpha in vivo. Mol Pharmacol. 2007 Oct;72(4):1003-14. PMID: 17622580
7. Langer SW, Jensen PB, Sehested M. Other uses of dexrazoxane: Savene, the first proven antidote against anthracycline extravasation injuries. Cardiovasc Toxicol. 2007;7(2):151-3. Review. PMID: 17652821
8. Jensen LH, Liang H, Shoemaker R, Grauslund M, Sehested M, Hasinoff BB. A Three-Dimensional Quantitative Structure-Activity Relationship Study of the Inhibition of the ATPase Activity and the Strand Passing Catalytic Activity of Topoisomerase II{alpha} by Substituted Purine Analogs. Mol Pharmacol. 2006 Nov;70(5):1503-1513. PMID: 16880287
9. Langer SW, Thougaard AV, Sehested M, Jensen PB. Treatment of anthracycline extravasation in mice with dexrazoxane with or without DMSO and hydrocortisone. Cancer Chemother Pharmacol. 2006 Jan;57(1):125-8. PMID: 16001176
10. Hofland KF, Thougaard AV, Dejligbjerg M, Jensen LH, Kristjansen PEG, Rengtved P, Sehested M, Jensen PB. Combining Etoposide and Dexrazoxane synergizes with radiotherapy and improves survival in mice with central nervous system tumors. Clin Cancer Res 2005 Sep15; 11(18): 6722-29. PMID: 16166453
11. Jensen LH, Thougaard AV, Grauslund M, Sokilde B, Carstensen EV, Dvinge HK, Scudiero DA, Jensen PB, Shoemaker RH, Sehested M. Substituted purine analogues define a novel structural class of catalytic topoisomerase II inhibitors. Cancer Res. 2005 Aug 15;65(16):7470-7. PMID: 16103101
12. Hofland KF, Thougaard AV, Sehested M, Jensen PB. Dexrazoxane protects against myelosuppression from the DNA cleavage-enhancing drugs etoposide and daunorubicin but not doxorubicin. Clin Cancer Res. 2005 May 15;11(10):3915-24. PMID: 15897593
13. Vaughn J, Huang S, Wessel I, Sorensen TK, Hsieh T, Jensen LH, Jensen PB, Sehested M, Nitiss JL. Stability of the topoisomerase II closed clamp conformation may influence DNA stimulated ATP hydrolysis. J Biol Chem. 2005 Mar 25; 280(12): 11920-9. PMID: 15647268
14. Walker JV, Nitiss KC, Jensen LH, Mayne C, Hu T, Jensen PB, Sehested M, Hsieh T, Nitiss JL. A mutation in human topoisomerase II alpha whose expression is lethal in DNA repair-deficient yeast cells. J Biol Chem. 2004 Jun 18; 279(25):25947-54. PMID: 15037624
15. Schroeder PE, Hofland KF, Jensen PB, Sehested M, Langer SW, Hasinoff BB. Pharmacokinetics of etoposide in cancer patients treated with high-dose etoposide and with dexrazoxane (ICRF-187) as a rescue agent. Cancer Chemother Pharmacol. 2004 Jan;53(1):91-3. PMID: 14574459
16. Sorensen TK, Grauslund M, Jensen PB, Sehested M, Jensen LH. Separation of bisdioxopiperazine- and vanadate resistance in topoisomerase II. Biochem Biophys Res Commun. 2005 Sep 2;334(3):853-60. PMID: 16053917
17. Schroeder PE, Jensen PB, Sehested M, Hofland KF, Langer SW, Hasinoff BB. Metabolism of dexrazoxane (ICRF-187) used as a rescue agent in cancer patients treated with high-dose etoposide. Cancer Chemother Pharmacol. 2003 Aug;52(2):167-74. Epub 2003 May 15. PMID: 12750840
18. Renodon-Cornière A, Sørensen TK, Jensen PB, Nitiss JL, Søkilde B, Sehested M, Jensen LH. Probing the role of linker substituents in bisdioxopiperazine analogs for activity against wild type and mutant human topoisomerase II. Mol Pharmacol. 2003 May; 63(5):1159-68. PMID: 12695544
19. Jensen JN, Lock-Andersen J, Langer SW, Mejer J. Dexrazoxane - a promising antidote in the treatment of accidental extravasation of anthracyclines. Scand J Plast Reconstr Surg Hand Surg. 2003;37(3):174-5. PMID: 12841619
20. Jensen LH, Renodon-Cornière A, Nitiss KC, Hill BT, Nitiss JL, Jensen PB, Sehested M. A dual mechanism of action of the anticancer agent F 11782 on human topoisomerase. Biochem Pharmacol. 2003 Aug 15; 66(4):623-31. PMID: 12906927
21. Jensen LH, Renodon-Corniere A, Wessel I, Langer SW, Søkilde B, Carstensen EV, Sehested M, Jensen PB. Maleimide is a potent inhibitor of topoisomerase II in vitro and in vivo. - A new mode of catalytic inhibition. Mol Pharmacol 2002 May; 61(5):1235-43. PMID: 11961142
22. Kellner U, Sehested M, Jensen PB, Gieseler F, Rudolph P. Culprit and victim - DNA topoisomerase II. Lancet Oncology 2002 Apr; 3:325-43. PMID: 12067686 PMID: 12067686
23. Renodon-Corniere A, Jensen LH, Nitiss JL, Jensen PB, Sehested M. Interaction of Human DNA Topoisomerase II alpha with DNA: Quantification by Surface Plasmon Resonance. Biochem 2002 Nov 12; 41(45):13395-402. PMID: 12416984
24. Wessel I, Jensen LH, Renodon-Corniere A, Sorensen TK, Nitiss JL, Jensen PB, Sehested M. Human small cell lung cancer NYH cells resistant to the bisdioxopiperazine ICRF-187 exhibit a functional dominant Tyr165Ser mutation in the Walker A ATP binding site of topoisomerase ll. FEBS Lett 2002 Jun 5; 520(1-3):161-6. PMID: 12044890
25. Langer SW, Sehested M, Jensen PB. Dexrazoxane is a potent and specific inhibitor of anthracycline induced subcutaneous lesions in mice. Ann Oncol. 2001 Mar;12(3):405-10. PMID: 11332155
26. Langer SW, Sehested M, Jensen PB. Treatment of anthracycline extravasation with dexrazoxane. Clin Cancer Res. 2000 Sep;6(9):3680-6. PMID: 10999761
27. Langer SW, Sehested M, Jensen PB, Buter J, Giaccone G. Dexrazoxane in anthracycline extravasation. J Clin Oncol. 2000 Aug;18(16):3064. PMID: 10944144
28. Hofland K, Petersen BO, Falck J, Helin K, Jensen PB, Sehested M. Differential cytotoxic pathways of topoisomerase I and II anticancer agents following overexpression of the E2F-1/DP-1 transcription factor complex. Clin. Cancer Res. 2000 Apr; 6(4):1488-97. PMID: 10778981
29. Jensen LH, Nitiss KC, Rose A, Dong J, Zhou J, Hu T, Osheroff N, Jensen PB, Sehested M, Nitiss J. A novel mechanism of cell killing by anti-topoisomerase II bisdioxopiperazines. J. Biol Chem. 2000 Jan 21; 275(3):2137-46. PMID: 10636919
30. Jensen LH, Wessel I, Møller M, Nitiss JL, Sehested M, Jensen PB. N-terminal and core-domain random mutations in human topoisomerase II conferring bisdioxopiperazine resistance. FEBS Lett. 2000 Sep 1; 480(2-3):201-7. PMID: 11034329
31. Langer SW, Schmidt G, Sørensen M, Sehested M, Jensen PB. Inhibitors of topoisomerase II as pH-dependent modulators of etoposide-mediated cytotoxicity. Clin Cancer Res. 1999 Oct;5(10):2899-907. PMID: 10537359

Apoxis

1. Etter AL, Bassi I, Germain S, Delaloye JF, Tschopp J, Sordat B, Dupuis M. The combination of chemotherapy and intraperitoneal MegaFas Ligand improves treatment of ovarian carcinoma. Gynecol Oncol. 2007 Oct;107(1):14-21. Epub 2007 Jun 29. PMID: 17604087
2. Greaney P, Nahimana A, Lagopoulos L, Etter AL, Aubry D, Attinger A, Beltraminelli N, Huni B, Bassi I, Sordat B, Demotz S, Dupuis M, Duchosal MA. A Fas agonist induces high levels of apoptosis in haematological malignancies. Leuk Res. 2006 Apr;30(4):415-26. Epub 2005 Sep 21. PMID: 16181674

Zemab

1. von Minckwitz G, Harder S, Hövelmann S, Jäger E, Al-Batran SE, Loibl S, Atmaca A, Cimpoiasu C, Neumann A, Abera A, Knuth A, Kaufmann M, Jäger D, Maurer AB, Wels WS. Phase I clinical study of the recombinant antibody toxin scFv(FRP5)-ETA specific for the ErbB2/HER2 receptor in patients with advanced solid malignomas. Breast Cancer Res. 2005;7(5):R617-26. PMID: 16168106
2. Azemar M, Djahansouzi S, Jäger E, Solbach C, Schmidt M, Maurer AB, Mross K, Unger C, von Minckwitz G, Dall P, Groner B, Wels WS. Regression of cutaneous tumor lesions in patients intratumorally injected with a recombinant single-chain antibody-toxin targeted to ErbB2/HER2. Breast Cancer Res Treat. 2003 Dec;82(3):155-64. PMID: 14703062

NAD

1. Holen K, Saltz LB, Hollywood E, Burk K, Hanauske AR. The pharmacokinetics, toxicities, and biologic effects of FK866, a nicotinamide adenine dinucleotide biosynthesis inhibitor. Invest New Drugs. 2008 Feb;26(1):45-51. Epub 2007 Oct 9. PMID: 17924057
2. Pogrebniak A, Schemainda I, Azzam K, Pelka-Fleischer R, Nüssler V, Hasmann M. Chemopotentiating effects of a novel NAD biosynthesis inhibitor, FK866, in combination with antineoplastic agents. Eur J Med Res. 2006 Aug 30;11(8):313-21. PMID: 17052966
3. Drevs J, Löser R, Rattel B, Esser N. Antiangiogenic potency of FK866/K22.175, a new inhibitor of intracellular NAD biosynthesis, in murine renal cell carcinoma. Anticancer Res. 2003 Nov-Dec;23(6C):4853-8. PMID: 14981935
4. Hasmann M, Schemainda I. FK866, a highly specific noncompetitive inhibitor of nicotinamide phosphoribosyltransferase, represents a novel mechanism for induction of tumor cell apoptosis. Cancer Res. 2003 Nov 1;63(21):7436-42. PMID: 14612543
5. Olesen UH, Christensen MK, Björkling F, Jäättelä M, Jensen PB, Sehested M, Nielsen SJ. Anticancer agent CHS-828 inhibits cellular synthesis of NAD. Biochem Biophys Res Commun. 2008 Mar 21;367(4):799-804. Epub 2008 Jan 15. PMID: 18201551Cowland J, Soerensen OE, Sehested M, Borregaard N. Neutrophil Gelatinase-Associated Lipocalin (NGAL) is Upregulated in Human Epithelial Cells by IL-1 but not by TNF. J. Immunol. 2003; 171:6630-6639.

Other

1. La Cour J, Mollerup J, Winding P, Tarabykina S, Sehested M, Berchtold MW. Up-regulation of ALG-2 in hepatomas and lung cancer tissue. Am J Pathol 2003; 163:81-89.
2. Di Tullio RA, Mochan TA, Venere M, Bartkova J, Sehested M, Bartek J, Halazonetis TD. 53BP1 functions in an ATM-dependent checkpoint pathway that is constitutively activated in human cancer. Nature Cell Biol. 2002; 4:998-1002.
3. Rothenborg-Jensen L, Hansen HF, Wessel I, Nitiss JL, Schmidt G, Jensen PB, Sehested M, Jensen LH. Linker length in podophyllotoxin-acridine conjugates determines potency in vivo and in vitro as well as specificity against MDR cell lines. Anti-Cancer Drug Design 2002; 16:305-315.
4. Bergman AM, Munch-Petersen B, Jensen PB, Sehested M, Veerman G, Voorn DA, Smid K, Pinedo HM, Peters GJ. Collateral sensitivity to gemcitabine (2',2'-difluorodeoxycytidine) and cytosine arabinoside of daunorubicin- and VM-26-resistant variants of human small cell lung cancer cell lines. Biochem. Pharmacol. 2001; 61:1401-1408.
5. Lukas C, Bartkova J, Latella L, Falck J, Mailand N, Schroeder T, Sehested M, Lukas J, Bartek J. DNA damage-activated kinase Chk2 is independent of proliferation or differentiation yet correlates with tissue biology. Cancer Res. 2001; 61:4990-4993.
6. Nielsen BS, Sehested M, Duun S, Rank F, Timshel S, Rygard J, Johnsen M, Danø K. Urokinase plasminogen activator is localized in stromal cells in ductal breast cancer. Lab. Invest. 2001; 81:1485-501.