Triple-negative Breast Cancer and Poly(ADP-ribose) Polymerase Inhibitors

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)

Volume 17, 14 Issues, 2017

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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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Michelle Prudhomme
Institut de Chimie de Clermont-Ferrand
Université Clermont Auvergne

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Triple-negative Breast Cancer and Poly(ADP-ribose) Polymerase Inhibitors

Anti-Cancer Agents in Medicinal Chemistry, 12(6): 672-677.

Author(s): Youngjin Park, Ayako Moriyama, Tomoaki Kitahara, Yutaka Yoshida, Tasuku Urita and Ryoji Kato.

Affiliation: Breast Surgery, Sakura Medical Center, School of Medicine, Faculty of Medicine, Toho University, Japan.


Recent gene profiling studies have identified at least 5 major subtypes of breast cancer, including normal type, luminal A type, luminal B type, human epidermal growth factor receptor (HER)-2 positive type, and basal-like type. Triple-negative breast cancer (TNBC), showing no or low expressions of estrogen receptor (ER), progesterone receptor (PgR), and HER2, considered important clinical biomarkers, accounts for 10% to 20% of all breast cancers. Hormonal therapy and molecular targeted therapy are not indicated for the management of TNBC, resulting in poor outcomes. Because TNBC lacks clear-cut therapeutic targets, effective treatment strategies remain to be established. However, TNBC is known to share similar biologic characteristics with basal-like type breast cancer and is often accompanied by loss of functional BRCA, a gene-modifying enzyme. Breast cancer with BRCA1 or BRCA2 mutations is accompanied by activation of the enzyme poly(ADP-ribose) polymerase (PARP). PARP, a DNA base-excision repair enzyme, is known to play a central role in gene repair, along with BRCA. Because some breast cancers with BRCA1 or BRCA2 mutations are TNBC, the suppression of PARP has attracted attention as a new treatment strategy for TNBC. In this article, we review the clinical characteristics of TNBC, discuss problems in treatment, and briefly summarize the international development status of PARP inhibitors.


BRCA, Breast cancer, DNA base-excision repair, PARP, PARP inhibitors, Triple-negative breast cancer.

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Article Details

Volume: 12
Issue Number: 6
First Page: 672
Last Page: 677
Page Count: 6
DOI: 10.2174/187152012800617759
Price: $58

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