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research Résumés scientifiques

111. Heath, E. et al., 2010 ASCO Annual Meeting, juin 2010
A phase I study of oral administration of MGCD265 in patients with advanced malignancies (study 265-102)

110. Drouin, M. et al., 2010 ASCO Annual Meeting, juin2010
Daily administration of MGCD265 to patients with solid tumors in a dose-escalation phase I study (study 265-101)

109. Martell, R. et al., 2010 ASCO Annual Meeting, juin2010
Phase II study of MGCD0103 in patients with relapsed follicular lymphoma: Study re-initiation and update of clinical efficacy and safety

108. Besterman, J. et al., 2010 ASCO Annual Meeting, juin2010
Potent preclinical anti-tumor activity of MGCD265, an oral Met/VEGFR kinase inhibitor in phase II clinical development, in combination with taxanes or erlotinib

107. Fournel, M. et al., 2010 AACR Annual Meeting, avril 2010
Potent preclinical anti-tumor activity of MGCD265, an orally active Met/VEGFR multi-targeted kinase inhibitor in phase II clinical development, in combination with an EGFR inhibitor

106. Beaulieu, N. et al., 2010 AACR Annual Meeting, avril 2010
MGCD265, an orally active Met/VEGFR multi-targeted kinase inhibitor in phase II clinical development, potently inhibits clinically relevant met mutants

105. Martell, R. E. et al., 2009 ASH Annual Meeting, décembre 2009
Clinical development of MGCD0103, an isotype-selective HDAC inhibitor: pericarditis/pericardial effusion in the context of overall safety and efficacy

104. LoRusso, P. et al., 2009 AACR-NCI-EORTC International Conference, novembre 2009
A phase I dose-escalation study of MGCD265 in patients with advanced malignancies (study 265-102)

103. Nguyen, T. D., et al., 49th Annual ICAAC Meeting, septembre 2009
A novel small molecule antifungal agent, MGCD290, modulates azole activity in yeast through specific inhibition of the histone deacetylase Hos2

102. Martell, L. et al. , 49th Annual ICAAC Meeting, septembre 2009
A novel beta-lactmase inhibitor potentiates and extends the antibacterial activity of imipenem against beta-lactam-resistant P. aeruginosa and K. pneumoniae

101. Martell, L. et al., 49th Annual ICCAC Meeting, septembre 2009
Multiple phase I studies in healthy subjects demonstrate safety and pharmacokinetics of MGCD290, an oral fungal Hos2 inhibitor +/- fluconazole

100. Conn K.L. et al., American Phytopathology Society (APS) Annual Meeting, août 2009
A new compound class synergizes with fungicides to inhibit plant pathogenic fungi

99. Conn K.L. et al., Canadian Phytopathological Society (CPS) Annual Meeting, juin 2009
Synergy between histone deacetylase inhibitors and azole fungicides to inhibit plant pathogenic fungi

98. Hong, D. et al., ASCO Annual Meeting, mai 2009
Phase I study of MGCD265 administered intermittently to patients with advanced malignancies (Study 265-102) 

97. Kollmannsberger, C.K. et al., ASCO Annual Meeting, mai 2009
Phase I study of daily administration of MGCD265 to patients with advanced malignancies (Study 265-101)

96. Maroun, C. et al. AACR Annual Meeting, avril 2009
Preclinical development of a novel oral multi-targeted kinase inhibitor with potent in vivo antitumor activity

95. Diekema, D. et al. ICAAC/IDSA Annual Meeting, octobre 2008
Combination testing of MGCD290, a fungal histone deacetylase inhibitor, with azole antifungals against a large collection of clinical fungal isolates

94. Nguyen, D. T. et al. ICAAC/IDSA Annual Meeting, octobre 2008
In vivo properties of MGCD290, an antifungal Hos2 histone deacetylase (HDAC) enzyme inhibitor

93. Beaulieu, N. et al. 20th EORTC-NCI-AACR Symposium, octobre 2008
Preclinical pharmacodynamic markers of MGCD265, a potent orally active c-Met/VEGFR multi-targeted kinase inhibitor in phase I clinical trials

92. Crump, M. et al. 2008 ASCO Annual Meeting, juin 2008
Treatment of relapsed or refractory lymphoma with the oral, isotype-selective HDAC inhibitor MGCD0103: Interim results from a phase II study (étude 008)

91. Hurwitz, H. et al. 2008 ASCO Annual Meeting, juin 2008
Phase I/II: The oral isotype-selective HDAC inhibitor MGCD0103 in combination with gemcitabine in patients with solid tumors (étude 006)

90. Bociek, R. et al. 2008 ASCO Annual Meeting, juin 2008
Isotype-selective histone deacetylase (HDAC) inhibitor MGCD0103 demonstrates clinical activity and safety in patients wiht relapsed/refractory classical Hodgkin lymphoma (HL) in a phase II study (étude 010)

89. Beaulieu, N. et al. 2008 AACR Annual Meeting, avril 2008
Preclinical development of MGCD265, a potent orally active c-Met/VEGFR multi-targeted kinase inhibitor

88. Fujita, H. et al. 2008 AACR Annual Meeting, avril 2008 (présentation orale)
MGCD0103, an oral HDAC inhibitor, significantly enhances the anti-tumor efficacy of taxanes via the unique modulation of angiogenesis gene expressions

87. Bonfils, C. et al. 2008 AACR Annual Meeting, avril 2008
Induction of an anti-angiogenesis factor TSP-1 by a novel HDAC inhibitor, MGCD0103 in human cancer cells in vitro and in vivo

86. Kacchap, S. et al. 2008 AACR Annual Meeting, avril 2008
Elucidating the role of class I and class II histone deacetylases in regulation of NDRG1 in prostate cancer

85. Chan, E. et al., ASCO 2008 GI Cancer Symposium, janvier 2008
Phase I/II trial of the oral isotype-selective histone deacetylase inhibitor MGCD0103 in combination with gemcitabine in patients with solid tumors (Trial 006)


84. Garica-Manero, G. et al., ASH Annual Meeting, décembre 2007 (présentation orale)
A Phase I/II study of 5-azacitidine in combination with MGCD0103 in AML or MDS

83. Younes, A. et al., ASH Annual Meeting, décembre 2007
Isotype-selective HDAC inhibitor MGCD0103 decreases serum TARC concentrations and produces clinical responses in heavily pretreated patients with relapsed classical Hodgkin lymphoma (Trial 010)

82. Younes, A. et al., ASH Annual Meeting, décembre 2007
Treatment of relapsed or refractory lymphoma with the oral isotype-selective histone deacetylase inhibitor MGCD0103: Interim results from a Phase II study (Trial 008)

81. Patzke, H. et al., The Inaugural Huntington's Disease Clinical Research Symposium, décembre 2007
Discovery and development of novel HDAC inhibitors for Huntington's Disease

80. Hurwitz, H. et al., AACR-EORTC-NCI International Conference, octobre 2007
Phase I/II: the oral isotype-selective HDAC inhibitor MGCD0103 in combination with gemcitabine in patients with refractory solid tumors

79. Li, Zuomei, et al., SMA Summit on Drug Development, septembre 2007
Brain-penetrant, isotype-selective HDAC inhibitors as novel therapeutic agents for spinal muscular atrophy

78. Diekema, D.J. et al., 47e Forum Annuel de l'ICAAC, septembre 2007
Synergy of MGCD290 with azole antifungals tested against clinical isolates of Candida and Aspergillus

77. Saavedra, O. et al., Gordon Research Conference, août 2007
A new series of Thieno[3,2-b] pyridines, inhibitors of the HGF and VEGF receptor family

76. Moradei, O. et al., Gordon Research Conference on Medicinal Chemistry, août 2007
Discovery of potent orally bioavailable benzamide-type histone deacetylase inhibitors

75. Raeppel, S. et al., 43rd International Conference on Medicinal Chemistry, juillet 2007
Inhibitors targeting multiple receptor tyrosine kinases for anticancer therapies

74. Vaisburg, A. CHI's 5th Annual Protein Kinase Targets Conference, juin 2007
Thienopyridine-Based Multi-Targeted Kinase Inhibitors

73. Guo, J. et al., 55th ASMS Conference on Mass Spec. juin 2007
Rapid detection and characterization of metabolites of potential histone deacetylase inhibitor MG89911 using a multiple information dependent acquisition strategy 

72. Lancet, et al., 43rd ASCO Annual Meeting, juin 2007
A Phase I Study of MGCD0103 Given as a Twice Weekly Oral Dose in Patients with Advanced Leukemias or Myelodysplastic Syndromes (MDS)

71. Younes, A. et al., 43rd ASCO Annual Meeting, juin 2007
A Phase I/II study of a novel oral isotype-selective histone deacetylase (HDAC) inhibitor MGCD0103 in patients with relapsed or refractory Hodgkin's lymphoma

70. Garcia-Manero, G. et al., 43rd ASCO Annual Meeting, juin 2007
Phase I/II study of novel oral isotype-selective histone deacetylase (HDAC) inhibitor MGCD0103 in combination with azacitidine in patients with high-risk myelodysplastic syndrome (MDS) or acute myelogenous leukemia (AML)

69. Akache, B. et al., ASM General Meeting, mai 2007
MG3290, a selective HDAC inhibitor, potentiates the anticandidal activity of ergosterol synthesis inhibitors, but not of compounds with other mechanisms of action

68. Nguyen, D. et al., ASM General Meeting, mai 2007
MG3290, a selective HDAC inhibitor, increases the post-antifungal effect and cidal potential of azoles in Candida species and decreases the frequenecy of azole resistance in Candida glabrata

67. Maroun, C. et al., AACR Annual Meeting, avril 2007
Induction of Interleukin-6 expression by the HDAC inhibitor, MGCD0103, in leukemia patients in vivo correlates with clinical efficacy

66. Liu, J. et al., AACR Annual Meeting, avril 2007
Induction of MT3 transcription as a pharmacodynamic biomarker for histone deacetylase inhibitor MGCD0103 in vitro and in vivo


65. Yeung, B. et al., 17th ECCMID, mars 2007
Effects of MG3290, a selective histone deacetylase inhibitor, on azole-resistance in Candida glabrata
VOIR AFFICHE

64. Garcia-Manero, G. et al., 48th Annual ASH Meeting, décembre 2006
Phase I/II study of the oral isotype-selective HDAC inhibitor MGCD0103 in combination with azaciticine in patients with high-risk Myelodysplastic Syndrome (MDS) or Acute Myelogenous Leukemia (AML)
VOIR AFFICHE

63. Lancet, J. et al., 48th Annual ASH Meeting,décembre 2006
Phase I study of MGCD0103 given as twice weekly oral dose in patients with leukemia (AML, ALL or CML) or Myelodysplastic Syndromes (MDS)
VOIR AFFICHE

62. Siu, L. et al., 18e Symposium de l'EORTC-NCI-AACR, novembre 2006
Phase I study of isotype-selective histone deacetylase (HDAC) inhibitor MGCD0103 given as a three-times weekly oral dose in patients with advanced solid tumors
VOIR AFFICHE

61. Beaulieu, N. et al., 18e Symposium de l'EORTC-NCI-AACR, novembre 2006
Identification and Characterization of Novel, Orally Active Inhibitors of c-MET and Ron Receptor Tyrosine Kinases
VOIR AFFICHE

60. Patzke, H. et al., 36th Society for Neuroscience Conference, octobre 2006
Development of Histone Deacetylase (HDAC) Inhibitors as Therapeutics for Huntington's Disease
VOIR AFFICHE

59. Campeol, N., 46th ICAAC Annual Meeting, septembre 2006
Potentiation of Azole Antifungal Activity by MG3290, a Selective Histone Deacetylase (HDAC) Inhibitor, in Candida glabrata
VOIR AFFICHE

58. Yeung, B. et al., 3rd Annual North American Genetic ABC Workshop, septembre 2006
Potentiation of Azole Antifungal Activity by MG3290, a Selective Histone Deacetylase (HDAC) Inhibitor, in Azole-Resistant Mutants of Candida glabrata
VOIR AFFICHE

57. Claridge, S., 232nd ACS National Meeting, septembre 2006
Novel Thieno[3,2-b]pyridine Scaffold Based Inhibitors of the c-Met and VEGFR Receptor Family
VOIR AFFICHE

56. Zhou, N., 232nd ACS National Meeting, septembre 2006
Design and Synthesis of Arylamino-(2-aminophenyl)-Benzamides or Cinnamides (A) and Heteroaryl-N-(2-aminophenyl)-Benzamides (B) as a Novel Class of Histone Deacetylase Inhibitors
VOIR AFFICHE

55. Vaisburg, A., XIXth International Symposium on Medicinal Chemisty, août 2006
Discovery and Development of MGCD0103 - an orally active HDAC inhibitor in human clinical trials
VOIR AFFICHE

54. Garcia-Manero, G. et al, ASCO 2006, juin 2006
Clinical Activity and Safety of the Histone Deacetylase Inhibitor MGCD0103. Results of a Phase I Study in Patients with Leukemia or Myelodysplastic Syndromes (MDS)
VOIR AFFICHE

53. Carducci, M. et al., ASCO 2006, juin 2006
Phase I Study of Isotype-selective Histone Deacetylase (HDAC) Inhibitor MGCD0103 Give as Three-times Weekly Oral Dose in Patients with Advanced Solid Tumors
VOIR AFFICHE

52. Amato, R. et al. ASCO 2006, juin 2006
A Dose and Schedule Optimizing Evaluation of MG98 Given as Either a 2-hour IV Infusion Twice Weekly or as a 7-day Continuous Infusion in Combination with Interferon Alpha (INF) in Nephrectomized Patients with Advanced Renal Cell Carcinoma (aRCC)

51. Nguyen, D.T. et al. ASM General Meeting, mai 2006
Synergy of MG3290, a Histone Deacetylase Inhibitor (HDAC1), with Azole Antifungals in Candida species and Aspergillus fumigatus. Effects on HDAC activity and ERG11 and CDR1/2 gene expression
VOIR AFFICHE

50. Nguyen, H. et al. AACR 97th Annual Meeting, avril 2006
Evaluation of Antitumor Activity, Anti-Angiogenic Activity and Pharmacodynamic End Points for Orally Active Multi-Targeted Anti-Angiogenic Kinase Inhibitors Targeting c-MET, Ron, VEGF and Tie-2 Receptors
VOIR AFFICHE

49. Fournel, M. et al. AACR 97th Annual Meeting, avril 2006
Enhanced Isotype-Selectivity and Antiproliferative Activity of Thiophenyl Derivatives of Benzamide HDAC Inhibitors in Human Cancer Cells
VOIR AFFICHE

48. Bedard, J. et al. 45th ICCAC Annual Meeting, décembre 2005
Synergism of Histone Deacetylase (HDC) Inhibitors with Ketoconazole in Candida albicnas and Candida glabrata. Relationship to their Effects on HDAC Activity in Protoplasts
VOIR AFFICHE

47. Hu, Wenqi et al. 45th ICCAC Annual Meeting, décembre 2005
Synergism of Histone Deacetylase (HDAC) inhibitors with Ketoconazole in Aspergillus fumigatus. Relationship to Inhibitory Effects on HDAC Activity in Protoplasts
VOIR AFFICHE

46. Garcia-Manero, G. et al. ASH 47th Annual Meeting, décembre 2005
A Phase I Study of the Histone Deacetylase Inhibitor MGCD0103 (MG-0103) Given as a Three-times Weekly Oral Dose in Patients with Leukemia or Myelodysplastic Syndromes (MDS)

45. Siu, L.L. et al., ASH 47th Annual Meeting, décembre 2005
Phase I Study of Isotype-Selective Histone Deacetylase (HDAC) Inhibitor MGCD0103 Given as Three-times Weekly Oral Dose in Patients with Advanced Solid Tumours
VOIR AFFICHE

44. Nguyen, Hannah et al
Synergistic Antitumour Activity of the Isotype-Selective Histone Deacetylase Inhibitor MGCD0103 in Combination with Gemcitabine
VOIR AFFICHE

43. Kalita, Ann et al
Pharmacodynamic Assessment of MGCD0103, a Novel Isotype-Specific HDAC Inhibitor, in Preclinical Evaluations and in Phase I Trials
VOIR AFFICHE

42. Cheriyath, Venugopalan et al
Epigenetic Regulation of IFN Activity in Multiple Myeloma by the Isotype-Selective HDAC Inhibitor MGCD0103
VOIR AFFICHE

41. Beaulieu, N. et al
Novel, Orally Active Multi-Kinase Inhibitors of c-MET and the VEGF Receptor Family Exhibit Potent Antiangiogenic Activity and Antitumour Efficacy in Preclinical Models
VOIR AFFICHE

40. Martell, R.
Epigenetic Mechanisms and Therapeutic Strategies in Disease

39. Reid, G.
Development of Novel Anticancer Therapeutics that Target Epigenetic Mechanisms of Gene Regulation

38. Besterman J.
Epigenetic Silencing of Tumor Suppressor Genes Through Aberrant Acetylation of Associated Histones Plays an Important Role in the Etiology of Cancer

37. Besterman, Jeffrey
Epigenetic Regulaton by MG98 and MGCD0103: From Bench to Clinic

36. Zhou, N. et al
Design and Synthesis of Arylamino-(2-aminophenyl)-Benzamides or Cinnamides (A) and Heteroaryl-N-(2-aminophenyl)-Benzamides (B) as a Novel Class of Histone Deacetylase Inhibitors

35. Peng, X. et al
Elucidation of In Vivo Rat Metabolic Pathways of Histone Deacetylase Inhibitor MS-275 by LC-MS/MS
VOIR AFFICHE

34. Peng, X. et al
Evaluation of Cytochrome P450 3A4 Inhibition by Test Compound HDAC Inhibitor MS-275 Using LC-MS/MS
VOIR AFFICHE

33. Reu., F. J. et al
Reactivation of the Tumor Suppressor RASSF1A by Selective Depletion of DNA Methyltransferase 1 (DNMT1) by MG98 Sensitizes Renal Cancer Cells to Interferon (IFN)-Induced Apoptosis
VOIR AFFICHE

32. Vidal, L. et al
A Phase I and Pharmacodynamic Study of a 7-day Infusion Schedule of the DNMT1 Antisense Compound MG98
POSTER

31. Gelmon, K. et al
Phase I Trials of the Oral Histone Deacetylase (HDAC) Inhibitor MGCD0103 Given Either Daily or 3x Weekly for 14 Days Every 3 Weeks in Patients with Advanced Solid Tumors

30. Kalita, A. et al
Pharmacodynamic Effect of MGCD0103 on Histone Deacetylase (HDAC) Enzyme Inhibition and Histone Acetylation Induction in Phase I Clinical Trials in Patients with Advanced Solid Tumours or Non-Hodgkin's Lymphoma (NHL)

29. Bonfils, C. et al
Specific Inhibition of HDAC8 by Antisense Leads to Growth Arrest and Apoptosis of Human Cancer Cells
POSTER

28. Bonfils, C. et al
Development of Whole Cell HDAC Enzyme Assay to Analyze Inhibitory Activity of MGCD0103 In Vitro and In Vivo
POSTER


27. Coulthard, L. et al
Decreased Expressionof DNMT1 at the mRNA Level Following 7-Day Infusion of the Antisense Compound Mg98 in a Phase I Study.
POSTER

26. Reu, F.J. et al
Gene Expression Enhancement by Inhibitors of Methylation: Potential role in Augmentation of Apoptosis Induced by Interferons (IFNs) in Melanoma and Renal Cell Carcinoma (RCC)
POSTER

25. Li, Z. et al.
Antitumour Activities of MGCD0103, A Novel and Isotype-Selective Histone Deacetylase Inhibitor
POSTER

24. Fréchette S. et al.
4-(Heteroarylaminomethyl)-N-(2-aminophenyl)-benzamides and their Analogs as a Novel Class of Histone Deacetylase Inhibitors show Antiproliferative Activity against Human Cancer Cells

23. Vaisburg, A. et al.
"Design, Synthesis and Biological Evaluation of N-(2-Amino-Phenyl)-4-(Heteroarylmethyl)-Benzamides as Novel Histone Deacetylase Inhibitors"

22. Gillespie, J. et al.
"An HPLC-MS/MS Assay for Simultaneous Determination of MS-275 and its Metabolite in Rat Plasma"

21. Georgopapadakou, N.
"Beta-lactamase Inhibitors: Evolving Compounds for Evolving Resistance Targets"

20. Paquin, I. et al.
"N-(2-Amino-phenyl)-4-(oxo/dioxo-heteroarylmethyl)-benzamides: Novel Histone Deacetylase Inhibitors"

19. Bonfils, C. et al.
"Cellular Function of HDAC1 in Human Cancer Cells Revealed by Using Isotype-Specific Antisense and Small Molecule Inhibitors"
POSTER


18. Reu, F. J., et al.
"Genes Involved in Sensitization of Renal Cancer Cells to Interferon-Induced Apoptosis After Selective Depletion of DNA Methyltransferase-1 by Antisense Oligonucleotide (MG98)"
POSTER

17. Beaulieu, N. et al.
"Antitumour Activity of MG98, an Antisense Oligodeoxynucleotide Targeting DNA Methyltransferase-1 (DMNT1) in Gastric Carcinoma"

16. Reu, F.J. et al.
"Selective Depletion of DNA Methyltransferase-1 by Antisense (MG98) sensitizes Renal Cancer Cells to Interferon-Induced Apoptosis"
POSTER

15. Moradei, O. et al.
"Design and Synthesis of a Novel Class of Histone Deacetylase Inhibitors which are Antiproliferative Against Human Cancer Cells"

14. Siu, L. et al.
"A Phase I and Pharmacokinetic (PK) Study of the Human DNA Methyltransferase (MeTase) Antisense Oligodeoxynucleotide MG98 Given as a 21-Day Continuous Infusion Every 4 Weeks"

13. Eisenhauer, E.A. et al.
"A Phase I and Pharmacokinetic (PK) Study of MG98, A Human DNA Methyltransferase (MeTase) Antisense Oligonucleotide, Given as a 2-Hour Twice Weekly Infusion 3 out of Every 4 Weeks"

12. Stewart, D. et al.
"A Phase I and Pharmacokinetic (PK) Study of MG98, a Human DNA Methyltransferase (MeTase) Antisense Oligonucleotide, Given as a 2-hour Twice Weekly (BIW) Infusion 3 Out of Every 4 Weeks"

11. Winquist, E. et al.
"Phase II Study of the DNA Methyltransferase I (DNMT1) Inhibitor MG98 in Patients (PTS) with Renal Cell Carcinoma (RCC)"

10. Barsalou, A. et al.
"Isotype-selective Depletion of DNA Methyltransferase-1 (DNMT1) by siRNa Highlights its Central Role in Maintenance of CpG Methylation and Tumour Suppressor Silencing in Human Cancer Cells"

9. Amrein, P. et al.
"Effect of MG98 Treatment on DNA Gene Promoter CpG Island Methylation Patterns in Advanced Head and Neck Carcinoma Patients (pts.)"

8. Robert, M.-F. et al.
"DNA Methyltransferase DNMT1 is Required to Maintain Aberrant CpG Island Methylation in Human Cancer Cells"

7. Woo, S.H. et al.
"Structurally Simple TSA-like Straight Chain Hydroxamates as Potent Histone Deacetylase Inhibitors"

6. Lavoie, R. et al., Intl Symposium of Medicinal Chemistry, septembre 2002
"Sulfonamide Hydroxamic Acids, A Novel Class of Histone Deacetylase Inhibitors, are Antiproliferative Against Human Cancer Cells"

5. Vaisburg, A. et al., Intl Symposium of Medicinal Chemistry, septembre 2002
"(2-Amino-Phenyl)-Amides of w-substituted Alkanoic Acids as New Histone Deacetylase Inhibitors"

4. Morin, S. et al., AACR, mars 2001
"DNA Methyltransferase DNMT1 is the Molecular Target for MG98 and 5-aza-deoxycytidine (5-aza-dC) Mediated Tumour Suppressor Gene Reactivation"

3. Abou-Khalil, E. et al., ICAAC, décembre 2001
"Sulfonamidomethylphosphonates : Novel NON-Beta-Lactam Beta-Lactamase Inhibitors"

2. Beaulieu, N. et al.
"Synergistic Antitumour Activity of MG98 (Antisense Oligodeoxynucleotide Targeting DNMT1) in Combination with 5-aza-deoxycytosine"

1. Beaulieu, N. et al.
"Antitumour Activity of MG98, an Antisense Oligodeoxynucleotide Targeting DNA Methyltransferase 1 (DNMT1)"








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