Proteolysis Targeting Chimeras (PROTACs) in Breast Cancer Therapy

Breast cancer (BC) accounts for 30 % of cancer cases among women cancer patients globally, indicating the urgent need for the development of selective therapies targeting BCs. Recently, proteolysis-targeting chimera (PROTAC) has emerged as a promising strategy to target breast cancer. PROTAC is a chimeric molecule consisting of a target protein ligand, an E3 ligase ligand, and conjugating linkers, enabling it to facilitate the degradation of desired target proteins by recruiting E3 ligase in close proximity. Due to the catalytic behavior and direct degradation of BC-causing proteins, PROTAC could achieve high drug efficacy with low doses, drawing great attention for its potential as therapeutics. This review provides cases of the currently developed PROTACs targeting BCs depending on the type of BCs, limitations, and future perspectives of PROTAC in targeting BCs. PROTAC, composed of a target protein ligand, linker, and E3 ligase ligand, represents a novel strategy for breast cancer (BC) treatment, specifically targeting breast cancer-related proteins such as ER alpha and HER2. With the unique advantages of PROTACs, including catalytic efficacy and targeted protein degradation, it has been considered novel therapeutics for targeting breast cancers. image