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Design and synthesis of the first PARP-1 and proteasome dual inhibitors to treat breast cancer.

Author: ChenXin, ChenXinyi, HeHualong, HuXiang, LiXinyue, LiuZhihao, ShiYaojie, WangNingyu, YangWan, YangYingyue, YeTinghong, YuLuoting

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Overview

This study describes the design and synthesis of the first dual PARP-1 and proteasome inhibitor, based on Olaparib and Ixazomib. These dual inhibitors demonstrate excellent proliferation inhibition and synergistic effects on cells resistant to PARP-1 inhibitors.
Paper Details　
Original Abstract of the Article :
PARP-1 is a crucial factor in repairing DNA single strand damage and maintaining genomic stability. However, the use of PARP-1 inhibitors is limited to combination with chemotherapy or radiotherapy, or as a single agent for indications carrying HRR defects. The ubiquitin-proteasome system processes ...See full text at original site
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引用元：
https://doi.org/10.1016/j.ejmech.2023.115943

データ提供：米国国立医学図書館（NLM）

PARP-1 and Proteasome Dual Inhibitors: A Novel Approach to Breast Cancer Treatment

This study delves into the potential of dual inhibitors targeting PARP-1 and the proteasome, two key cellular pathways involved in DNA repair and protein degradation. The researchers designed and synthesized novel compounds that simultaneously inhibit both PARP-1 and the proteasome, aiming to enhance the efficacy of breast cancer treatment.

Dual Inhibition Shows Promise for Overcoming Resistance in Breast Cancer

The study demonstrates the potential of dual PARP-1 and proteasome inhibitors to overcome resistance to PARP-1 inhibitors, which are commonly used in breast cancer treatment. The dual inhibitors effectively inhibited cancer cell proliferation and showed synergistic effects in cells that were insensitive to PARP-1 inhibitors alone.

A New Hope for Breast Cancer Treatment

This research offers a promising new approach to breast cancer treatment by targeting multiple cellular pathways involved in cancer progression. Further investigation and clinical trials are needed to explore the safety and efficacy of these dual inhibitors in treating breast cancer.

Dr. Camel's Conclusion

This study explores the exciting potential of targeting multiple cellular pathways simultaneously for breast cancer treatment. Dual PARP-1 and proteasome inhibitors offer a novel approach to overcome resistance to PARP-1 inhibitors and provide a new avenue for effective breast cancer therapy.
Date :
  1. Date Completed n.d.
  2. Date Revised 2023-12-01
Further Info :

Pubmed ID

38039793

DOI: Digital Object Identifier

10.1016/j.ejmech.2023.115943

Related Literature

Article Analysis
・Effects of ixazomib
SNS
PICO Info
in preparation
Languages

English

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