BioCentury | Dec 30, 2020
Distillery Therapeutics

Targeting the histone methyltransferase EHMT2 for breast cancer recurrence

...recurrent breast cancer. In murine recurrent breast cancer cell lines, EHMT2 knockout or treatment with an EHMT2...
...with improved recurrence-free survival in tumor samples from patients. In a mouse model of breast cancer, tumor-specific EHMT2 knockout...
...were injected with recurrent breast cancer cells, the inhibitor reduced tumor growth and burden.TARGET/MARKER/PATHWAY: Euchromatic histone-lysine N-methyltransferase 2 (EHMT2; G9A)EXPERIMENTAL...
BioCentury | Sep 12, 2019
Distillery Therapeutics

Inhibition of G9A and DNMT methyltransferases in bladder cancer

...DISEASE CATEGORY: Cancer INDICATION: Bladder cancer Dual inhibition of G9A and DNMT methyltransferases, in combination with...
...ligand 1 (PD-L1), could help to treat bladder cancer. A tool compound that inhibited both G9A...
...from Merck & Co. Inc. and Opdivo nivolumab from Bristol-Myers Squibb Co. TARGET/MARKER/PATHWAY: Euchromatic histone-lysine N-methyltransferase 2 (EHMT2; G9A...
BioCentury | Dec 6, 2018
Translation in Brief

Opening chromatin: long-term detriment?

...reduce chromatin accessibility, and whose inhibitors can increase it, include histone deacetylases (HDACs), euchromatic histone-lysine N-methyltransferase 2 (EHMT2; G9A...
...the IRB Barcelona team focused on EHMT2. Mouse models of chemical-induced skin cancer with epidermal-specific EHMT2...
...mice with normal EHMT2 expression, contradicting the hypothesis that chromatin accessibility affects TMB. In addition, EHMT2...
BioCentury | Dec 8, 2017
Targets & Mechanisms

Pathways emerging from ASH

...including the translation initiators EWSR1 and eIF4F and the ribosome binding protein nucleolin; epigenetic modulators EHMT2...
...1 BRDT - Bromodomain testis-specific CCR2 (CD192) - CC chemokine receptor 2 EHMT2 (G9A) - Euchromatic histone-lysine N-methyltransferase 2...
...2 (CCR2) (CD192) DEAD box polypeptide 58 (RIG-I) (DDX58) DNA ligase 4 (LIG4) DNA mismatch repair protein Mlh1 (MLH1) Euchromatic histone-lysine N-methyltransferase 2 (EHMT2) (G9A) Eukaryotic...
BioCentury | Dec 8, 2017
Targets & Mechanisms

Epiphenomena at ASH

...5, 2017 Target 2017 Abstracts 2016 Abstracts BRCA1-associated protein 1 (BAP1) 4 1 Euchromatic histone-lysine N-methyltransferase 2 (EHMT2; G9A...
...feature outside of cancer too, with abstracts pointing to inhibition of the methyltransferases EHMT1 and EHMT2...
...DNMT1 - DNA (cytosine-5-)-methyltransferase 1 EHMT1 (GLP) - Euchromatic histone-lysine N-methyltransferase 1 EHMT2 (G9A) - Euchromatic histone-lysine N-methyltransferase 2...
BioCentury | Jul 10, 2017
Distillery Techniques

Biomarkers

...KGFR ; FGFR2 ; CD332) -- that are regulated by Euchromatic histone-lysine N-methyltransferase 2 ( EHMT2 ; G9A...
...Institute, Herston, Australia email: jason.lee@qimrberghofer.edu.au Hongjiang Li QIMR Berghofer Medical Research Institute Aryl hydrocarbon receptor nuclear translocator-like (ARNTL) (BMAL1) CD1C Euchromatic histone-lysine N-methyltransferase 2 (EHMT2) (G9A) GATA...
BioCentury | Jun 7, 2017
Distillery Therapeutics

Cancer

...AML); B cell lymphoma Cell culture and mouse studies identified an aminoquinoline-based dual DNMT1 / EHMT2...
...of 4-aminoquinoline analogs, followed by optimization of hits, yielded a compound that inhibited DMNT1 and EHMT2...
...and Phase I testing for B cell lymphoma. TARGET/MARKER/PATHWAY: DNA (cytosine-5-)-methyltransferase 1 (DNMT1); euchromatic histone-lysine N-methyltransferase 2 (EHMT2; G9A...
BioCentury | Apr 11, 2017
Distillery Therapeutics

Endocrine / Metabolic

...INDICATION: Growth failure Cell culture, patent sample and mouse studies suggest inhibiting EHMT2 could help treat...
...repressed. Screening of about 9,000 small molecules in cell-based gene expression assays identified three selective EHMT2...
...penetration (see "Pushing for Progress in Prader-Willi." BioCentury Innovations (April 6, 2017)). TARGET/MARKER/PATHWAY: Euchromatic histone-lysine N-methyltransferase 2 (EHMT2; G9A...
BioCentury | Apr 7, 2017
Strategy

Pushing for progress in Prader-Willi

...lethality and poor growth in Prader-Willi, treatment with a selective inhibitor of the histone methyltransferase EHMT2...
...will help his group move forward with the approach described in the paper, where the EHMT2...
...Euchromatic histone-lysine N-methyltransferase 2 MetAP2 - Methionine aminopeptidase 2 References Kim, Y., et al. “Targeting the histone methyltransferase G9a...
BioCentury | Sep 15, 2016
Distillery Therapeutics

Therapeutics: Euchromatic histone-lysine N-methyltransferase 2 (EHMT2; G9a)

...Cancer INDICATION: Colorectal cancer Patient sample, cell culture and mouse studies suggest inhibiting EHMT2 could help...
...EHMT2 were associated with large tumor size, high levels of invasiveness and poor survival, and EHMT2...
...liver metastasis. Next steps include developing therapeutic compounds that degrade EHMT2 protein. TARGET/MARKER/PATHWAY: Euchromatic histone-lysine N-methyltransferase 2 (EHMT2; G9a...
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