brd4770 and Breast-Neoplasms

brd4770 has been researched along with Breast-Neoplasms* in 1 studies

Other Studies

1 other study(ies) available for brd4770 and Breast-Neoplasms

Article	Year
Synthesis and biological evaluation of benzimidazole derivatives as the G9a Histone Methyltransferase inhibitors that induce autophagy and apoptosis of breast cancer cells. Bioorganic chemistry, 2017, Volume: 72 G9a (also known as KMT1C or EHMT2) is initially identified as a H3K9 methyltransferase that specifically mono- and dimethylates 'Lys-9' of histone H3 (H3K9me1 and H3K9me2, respectively) in euchromatin. It is overexpressed in various human cancers and employed as a promising target in cancer therapy. We discovered a benzoxazole scaffold through virtual high-throughput screening, and designed, synthesized 24 derivatives and investigated for inhibition of G9a. After several rounds of kinase and anti-proliferative activity screening, we discovered a potent G9a antagonist (GA001) with an IC Topics: Antineoplastic Agents; Autophagy; Benzimidazoles; Breast Neoplasms; Cell Survival; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; Enzyme Inhibitors; Female; Histocompatibility Antigens; Histone-Lysine N-Methyltransferase; Humans; MCF-7 Cells; Models, Molecular; Molecular Structure; Structure-Activity Relationship	2017

Article

Year

Synthesis and biological evaluation of benzimidazole derivatives as the G9a Histone Methyltransferase inhibitors that induce autophagy and apoptosis of breast cancer cells.

Bioorganic chemistry, 2017, Volume: 72

G9a (also known as KMT1C or EHMT2) is initially identified as a H3K9 methyltransferase that specifically mono- and dimethylates 'Lys-9' of histone H3 (H3K9me1 and H3K9me2, respectively) in euchromatin. It is overexpressed in various human cancers and employed as a promising target in cancer therapy. We discovered a benzoxazole scaffold through virtual high-throughput screening, and designed, synthesized 24 derivatives and investigated for inhibition of G9a. After several rounds of kinase and anti-proliferative activity screening, we discovered a potent G9a antagonist (GA001) with an IC

Topics: Antineoplastic Agents; Autophagy; Benzimidazoles; Breast Neoplasms; Cell Survival; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; Enzyme Inhibitors; Female; Histocompatibility Antigens; Histone-Lysine N-Methyltransferase; Humans; MCF-7 Cells; Models, Molecular; Molecular Structure; Structure-Activity Relationship

2017