The SUV39H1 inhibitor chaetocin induces differentiation and shows synergistic cytotoxicity with other epigenetic drugs in acute myeloid leukemia cells

Identification of epipolythiodioxopiperazines HDN-1 and chaetocin as novel inhibitor of heat shock protein 90

(2015) Xiaoping Song et al.   Oncotarget

Small-molecule inhibition of BRD4 as a new potent approach to eliminate leukemic stem- and progenitor cells in acute myeloid leukemia (AML)

(2015) Harald Herrmann et al.   Oncotarget

The methyltransferase G9a regulates HoxA9-dependent transcription in AML

(2014) B. Lehnertz et al.   GENES & DEVELOPMENT

At the tipping point for epigenetic therapies in cancer

(2014) Peter A. Jones   JOURNAL OF CLINICAL INVESTIGATION

Polycomb Repressive Complex 2 and H3K27me3 Cooperate with H3K9 Methylation To Maintain Heterochromatin Protein 1  at Chromatin

(2014) J. Boros et al.   MOLECULAR AND CELLULAR BIOLOGY

BET Protein Antagonist JQ1 Is Synergistically Lethal with FLT3 Tyrosine Kinase Inhibitor (TKI) and Overcomes Resistance to FLT3-TKI in AML Cells Expressing FLT-ITD

(2014) W. Fiskus et al.   MOLECULAR CANCER THERAPEUTICS

Regulation of MYC Expression and Differential JQ1 Sensitivity in Cancer Cells

(2014) Trent Fowler et al.   PLoS One

Exploiting epigenetic vulnerabilities for cancer therapeutics

(2014) Barbara Mair et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Improved Therapeutic Effect against Leukemia by a Combination of the Histone Methyltransferase Inhibitor Chaetocin and the Histone Deacetylase Inhibitor Trichostatin A

(2013) Huong Thi Thanh Tran et al.   JOURNAL OF KOREAN MEDICAL SCIENCE

Gfi-1 is the transcriptional repressor of SOCS1 in acute myeloid leukemia cells

(2013) M.-C. Lee et al.   JOURNAL OF LEUKOCYTE BIOLOGY

On the Histone Lysine Methyltransferase Activity of Fungal Metabolite Chaetocin

(2013) Fanny L. Cherblanc et al.   JOURNAL OF MEDICINAL CHEMISTRY

Step-Wise Methylation of Histone H3K9 Positions Heterochromatin at the Nuclear Periphery

(2012) Benjamin D. Towbin et al.   CELL

G9a, a multipotent regulator of gene expression

(2012) Shilpa Rani Shankar et al.   Epigenetics

Epigenetic alterations in hematopoietic malignancies

(2012) Young Rock Chung et al.   INTERNATIONAL JOURNAL OF HEMATOLOGY

Recruitment of coregulator G9a by Runx2 for selective enhancement or suppression of transcription

(2012) Daniel J. Purcell et al.   JOURNAL OF CELLULAR BIOCHEMISTRY

G9a interacts with Snail and is critical for Snail-mediated E-cadherin repression in human breast cancer

(2012) Chenfang Dong et al.   JOURNAL OF CLINICAL INVESTIGATION

H3K9 methyltransferase G9a and the related molecule GLP

(2011) Y. Shinkai et al.   GENES & DEVELOPMENT

Anti-leukemia activity of chaetocin via death receptor-dependent apoptosis and dual modulation of the histone methyl-transferase SUV39H1

(2011) H Chaib et al.   LEUKEMIA

A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells

(2011) Masoud Vedadi et al.   Nature Chemical Biology

Targeting MYC dependence in cancer by inhibiting BET bromodomains

(2011) J. A. Mertz et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Unnatural enantiomer of chaetocin shows strong apoptosis-inducing activity through caspase-8/caspase-3 activation

(2010) Yuou Teng et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

H3K9 Histone Methyltransferase G9a Promotes Lung Cancer Invasion and Metastasis by Silencing the Cell Adhesion Molecule Ep-CAM

(2010) M.-W. Chen et al.   CANCER RESEARCH

Selective inhibition of BET bromodomains

(2010) Panagis Filippakopoulos et al.   NATURE

EVI-1 interacts with histone methyltransferases SUV39H1 and G9a for transcriptional repression and bone marrow immortalization

(2009) S Goyama et al.   LEUKEMIA

Reexpression of epigenetically silenced AML tumor suppressor genes by SUV39H1 inhibition

(2009) A Lakshmikuttyamma et al.   ONCOGENE

Lid2 Is Required for Coordinating H3K4 and H3K9 Methylation of Heterochromatin and Euchromatin

(2008) Fei Li et al.   CELL