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HDAC Inhibitors - References

Posters & Presentations

  • Sriram Balasubramanian, Mint Sirisawad, Susanne Steggerd, Wangsen Cao, Charles Lowenstein and Joseph J. Buggy The histone deacetylase (HDAC) inhibitor PCI-24781 decreases pro-inflammatory cytokine secretion in vitro and in vivo, and protects against endotoxemia in a sepsis model [Poster Presentation] 2010 American Society of Hematology Annual Meeting, San Diego, CA, 10-13 December, 2010
  • AACR 2010 Annual Meeting, Washington, DC, April 2010. Poster: "Development and biological characterization of novel, potent and stable isoform-specific inhibitors of histone deacetylase-8 (HDAC8)."
  • ASH 2009 Annual Meeting, New Orleans, LA, December 2009. Poster: “Phase I Analysis of the Safety and Pharmacodynamics of the Broad Spectrum Histone Deacetylase Inhibitor (HDACi) PCI-24781 in Relapsed and Refractory Lymphoma."
  • 3rd Annual HDAC Inhibitors: Developing Molecules for Targeting Oncology and More, at CHI Discovery on Target 2009 Conference, Boston, MA, November 2009. Seminar: “Utility of Predictive Biomarkers in the Clinical Development of the HDAC inhibitor PCI-24781."
  • AACR 2009 Annual Meeting, Denver, CO, April 2009. Seminar: “Identification of microRNA markers of response to HDAC inhibitor PCI-24781 in primary colon tumors."
  • ASH 2008 Annual Meeting, San Francisco, CA, 6-9 December 2008. Poster: ”The histone deacetylase-8 (HDAC8) selective inhibitor PCI-34051 decreases interleukin-1 beta secretion in vitro and reduces inflammation in vivo."
  • 2nd Annual HDAC Inhibitors: Targeting Oncology and Beyond, at CHI Discovery on Target 2008 Conference, Boston, MA, October 2008. Seminar: “Novel Mechanisms of Action for HDAC Inhibitors Point the Way to Novel Indications."
  • AACR 2008 Annual Meeting, San Diego, CA, April 2008. Poster: “The histone deacetylase-8 (HDAC8) selective inhibitor PCI-34051 induces apoptosis in T-cell tumors and downregulates IL-1? by novel mechanisms."
  • ASH 2007 Annual Meeting, Atlanta, December 2007. Poster: “Development of RAD51 as Biomarker for Sensitivity to the Histone Deacetylase (HDAC) Inhibitor PCI-24781 in Lymphoma."
  • ASH 2007 Annual Meeting, Atlanta, December 2007. Poster: “Histone Deacetylase Inhibitor (HDACi) PCI-24781 and Bortezomib Result in Synergistic Apoptosis in Hodgkin Lymphoma (HL) and Non-Hodgkin’s Lymphoma (NHL) Cell Lines."
  • AACR-NCI-EORTC 2007 International Conference, San Francisco, October 2007. Poster: “Activity of a novel HDAC inhibitor PCI-24781 in colorectal cancer: Discovery and validation of biomarkers of sensitivity and resistance."
  • AACR 2007 Annual Meeting, Los Angeles, CA, April 2007. Poster: “Cross-validated functional biomarkers for PCI-24781 and selection of clinical indications."

 

Scientific Manuscripts

HDAC Inhibitors

  • Yang C, Choy E, Hornicek F, Wood KB, Schwab JH, Liu X, Mankin H, Duan Z. The histone deacetylase inhibitor (HDACI) PCI-24781 enhances chemotherapy induced apoptosis in multidrug resistant sarcoma cell lines. Cancer Chemother Pharmacol. 2010 May 12. [Epub ahead of print].
  • Rivera-Del Valle N, Gao S, Miller C, Gonzales C, Sirisawad M, Steggerda S, Wheler J, Balasubramanian S, Chandra J. PCI-24781, a novel hydroxamic acid HDAC inhibitor, exerts cytotoxicity and histone alterations via caspase-8 and FADD in leukemia cells. Int J Cell Biol. 2010;2010:207420. Epub 2010 Jan 18.
  • Bhalla S, Balasubramanian S, David K, Sirisawad M, Buggy JJ, Mauro L, Prachand S, Miller R, Gordon LI, Evens AM. The Histone Deacetylase Inhibitor PCI-24781 Induces Caspase and ROS-Dependent Apoptosis Through NF-?B and is Synergistic with Bortezomib in Lymphoma Cells. Clin Cancer Res. (2009) May 15;15(10):3354-65. Epub 2009 May 5.
  • Lopez G, Liu J, Ren W, Wei W, Wang S, Lahat G, Zhu QS, Bornmann WG, McConkey DJ, Pollock RE, Lev DC. Combining PCI-24781, a novel histone deacetylase inhibitor, with chemotherapy for the treatment of soft tissue sarcoma. Clin Cancer Res. 2009 May 15;15(10):3472-83. Epub 2009 May 5.
  • Balasubramanian S, Verner E, Buggy JJ. Isoform-specific histone deacetylase inhibitors: The next step? Cancer Lett. (2009) Aug 8;280(2):211-21. Epub 2009 Mar 16.
  • Balasubramanian S, Ramos J, Sirisawad M, Luo W, Verner E, Buggy JJ. A novel histone deacetylase 8 (HDAC8) specific inhibitor PCI-34051 induces apoptosis in T-cell lymphomas. Leukemia. (2008) May;22(5):1026-34. Epub 2008 Feb 7.
  • Adimoolam S, Sirisawad M, Chen J, Thiemann P, Ford JM, Buggy JJ. HDAC inhibitor PCI-24781 decreases RAD51 expression and inhibits homologous recombination. Proc Natl Acad Sci USA (2007) Dec 4;104(49):19482-7.
  • Banuelos CA, Banáth JP, MacPhail SH, Zhao J, Reitsema T, Olive PL. Radiosensitization by the histone deacetylase inhibitor PCI-24781. Clin Cancer Res. (2007) Nov 15;13(22 Pt 1):6816-26.
  • Buggy JJ, Cao ZA, Bass KE, Verner E, Balasubramanian S, Liu L, et al. CRA-024781: a novel synthetic inhibitor of histone deacetylase enzymes with antitumor activity in vitro and in vivo. Mol Cancer Ther (2006) May;5(5):1309-17.
  • Cao ZA, Bass KE, Balasubramanian S, Liu L, Schultz B, Verner E, et al. CRA-026440: a potent, broad-spectrum, hydroxamic histone deacetylase inhibitor with antiproliferative and antiangiogenic activity in vitro and in vivo. Mol Cancer Ther (2006) Jul;5(7):1693-701.
  • Schultz BE, Misialek S, Wu J, Tang J, Conn MT, Tahilramani R, Wong L. Kinetics and comparative reactivity of human class I and class IIb histone deacetylases. Biochemistry. (2004) Aug 31;43(34):11083-91.
  • Somoza JR, Skene RJ, Katz BA, Mol C, Ho JD, Jennings AJ, et al. Structural snapshots of human HDAC8 provide insights into the class I histone deacetylases. Structure (2004) Jul;12(7):1325-34.
  • Buggy JJ, Sideris ML, Mak P, Lorimer DD, McIntosh B, Clark JM. Cloning and characterization of a novel human histone deacetylase, HDAC8. Biochem J (2000) Aug 15;350 Pt 1:199-205.:199-205.

Background

  • Tan J, Cang S, Ma Y, Petrillo RL, Liu D. Novel histone deacetylase inhibitors in clinical trials as anti-cancer agents. J Hematol Oncol. 2010 Feb 4;3:5.
  • Oehme I, Deubzer H, Wegener D, et al. Histone deacetylase 8 in neuroblastoma tumorigenesis. Clin Cancer Res. Jan 2009;15(1):91-99.
  • Gallinari P, Di Marco S, Jones P, Pallaoro M, Steinkühler C. HDACs, histone deacetylation and gene transcription: from molecular biology to cancer therapeutics. Cell Research (2007) 17:195-211.
  • Bieliauskas AV, Pflum MK. Isoform-selective histone deacetylase inhibitors. Chem Soc Rev. 2008 Jul;37(7):1402-13. Epub 2008 May 8.
  • Elaut G, Rogiers V, Vanhaecke T. The pharmaceutical potential of histone deacetylase inhibitors. Curr Pharm Des. 2007;13(25):2584-2620.
  • Farasat S, Aksentijevich I, Toro J. Autoinflammatory diseases: clinical and genetic advances. Arch Dermatol. Mar 2008;144(3):392-402.
  • Blanchard F, Chipoy C. Histone deacetylase inhibitors: new drugs for the treatment of inflammatory diseases? Drug Discov Today. Feb 2005;10(3):197-204.
  • Gray S, Dangond F. Rationale for the use of histone deacetylase inhibitors as a dual therapeutic modality in multiple sclerosis. Epigenetics.1(2):67-75.
  • Kazantsev A, Thompson L. Therapeutic application of histone deacetylase inhibitors for central nervous system disorders. Nat Rev Drug Discov. Oct 2008;7(10):854-868.
  • LequerrÈ T, Quartier P, Rosellini D, et al. Interleukin-1 receptor antagonist (anakinra) treatment in patients with systemic-onset juvenile idiopathic arthritis or adult onset Still disease: preliminary experience in France. Ann Rheum Dis. Mar 2008;67(3):302-308.
  • Pascual V, Allantaz F, Arce E, Punaro M, Banchereau J. Role of interleukin-1 (IL-1) in the pathogenesis of systemic onset juvenile idiopathic arthritis and clinical response to IL-1 blockade. J Exp Med. May 2005;201(9):1479-1486.
  • Steffan J, Bodai L, Pallos J, et al. Histone deacetylase inhibitors arrest polyglutamine-dependent neurodegeneration in Drosophila. Nature. Oct 2001;413(6857):739-743.
  • Susick L, Senanayake T, Veluthakal R, Woster P, Kowluru A. A novel histone deacetylase inhibitor prevents IL-1beta-induced metabolic dysfunction in pancreatic beta-cells. J Cell Mol Med. Jan 2009.