期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 34, 期 -, 页码 -出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2020.127763
关键词
Lysine-specific demethylase 1 (LSD1); Histone deacetylase 6 (HDAC6), Multiple; Myeloma (MM), Immunomodulatory imide; Drugs (IMiDs)
资金
- Jubilant Life Sciences
The article introduces a novel LSD1 and HDAC6 dual inhibitor, which has shown good efficacy in multiple myeloma in experiments, providing a new treatment strategy for various cancers.
Lysine specific demethylase 1 (LSD1) and HDAC6 are epigenetic proteins associated with several diseases, including cancer and combined inhibition of these proteins could be highly beneficial in treating some cancers such as AML, MM and solid tumors. Multiple myeloma (MM) is a challenging cancer with fast relapse rate where novel treatment options are the need of the hour. We have designed and developed novel, LSD1 and HDAC6 selective dual inhibitors to target MM. Our dual inhibitor compound 1 shows superior potency in multiple MM cell lines. In MM.1S xenograft model compound 1 shows superior efficacy compared to single agent LSD1 and HDAC6 inhibitors by oral administration and is well tolerated. Further evaluation of the molecule in other cancers is in progress.
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