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  3. A CARM1 Inhibitor Potently Suppresses Breast Cancer Both In Vitro and In Vivo

A CARM1 Inhibitor Potently Suppresses Breast Cancer Both In Vitro and In Vivo

  • J Med Chem. 2024 May 23;67(10):7921-7934. doi: 10.1021/acs.jmedchem.3c02315.
Bing-Ling Peng 1 2 3,  Ting Ran 4,  Xue Chen 1 2 3,  Jian-Cheng Ding 1 2 3,  Zi-Rui Wang 1 2,  Wen-Juan Li 1 2 3,  Wen Liu 1 2 3
Affiliations

Affiliations

  • 1 Fujian Provincial Key Laboratory of Innovative Drug Target Research, School of Pharmaceutical Sciences, Faculty of Medicine and Life Sciences, Xiamen University, Xiang'an South Road, Xiamen, Fujian 361102, China.
  • 2 State Key Laboratory of Cellular Stress Biology, School of Pharmaceutical Sciences, Faculty of Medicine and Life Sciences, Xiamen University, Xiang'an South Road, Xiamen, Fujian 361102, China.
  • 3 Xiang An Biomedicine Laboratory, School of Pharmaceutical Sciences, Faculty of Medicine and Life Sciences, Xiamen University, Xiang'an South Road, Xiamen, Fujian 361102, China.
  • 4 Bioland Laboratory (Guangzhou Regenerative Medicine and Health - Guangdong Laboratory), KaiYuan Road, Guangzhou, Guangdong 510530, China.
PMID: 38713486 DOI: 10.1021/acs.jmedchem.3c02315
Abstract

CARM1, belonging to the protein arginine methyltransferase (PRMT) family, is intricately associated with the progression of Cancer and is viewed as a promising target for both Cancer diagnosis and therapy. However, the number of specific and potent CARM1 inhibitors is limited. We herein discovered a CARM1 inhibitor, iCARM1, that showed better specificity and activity toward CARM1 compared to the known CARM1 inhibitors, EZM2302 and TP-064. Similar to CARM1 knockdown, iCARM1 suppressed the expression of oncogenic estrogen/ERα-target genes, whereas activated type I interferon (IFN) and IFN-induced genes (ISGs) in breast Cancer cells. Consequently, iCARM1 potently suppressed breast Cancer cell growth both in vitro and in vivo. The combination of iCARM1 with either endocrine therapy drugs or etoposide demonstrated synergistic effects in inhibiting the growth of breast tumors. In summary, targeting CARM1 by iCARM1 effectively suppresses breast tumor growth, offering a promising therapeutic approach for managing breast cancers in clinical settings.

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