Molecular insights into Silodosin’s anti-cancer effects: a promising repurposing strategy for breast cancer

Breast cancer, the most common cancer diagnosed among women worldwide, remains a significant clinical challenge due to its molecular heterogeneity and the development of resistance to conventional therapies. This study investigates the potential of silodosin, an α1A-adrenergic receptor (AR) antagonist, as a novel therapeutic agent in breast cancer, an area where its use has not been previously explored. Through detailed in vitro and in silico analyses, we elucidate the complex molecular mechanisms behind silodosin's antitumor effects. We demonstrate its ability to inhibit cell proliferation, induce apoptosis, reduce migration, and prevent 3D spheroid formation. Importantly, these effects are observed across different breast cancer subtypes. Crucially, our integrated approach reveals that silodosin's mechanism is not solely dependent on α1A-AR blockade. Molecular docking studies strongly suggest that silodosin directly interacts with both isoforms of the estrogen receptor (ERα and ERβ) with high affinity, binding to key residues within the ligand-binding domains of these receptors. This points to a new, dual-targeting mechanism of action. While its known α1A-AR antagonism may contribute to its effects, silodosin could also act as an ER ligand, modulating estrogen-driven pathways essential in breast cancer development. This study provides the first experimental and computational evidence supporting the repurposing of silodosin as a potential multi-targeted therapeutic agent for breast cancer, opening promising new opportunities for patients with limited treatment options and encouraging further preclinical and clinical studies.

Authors

Institutions

Publication Details

Journal
Cell Death Discovery
Published
2026-03-05
DOI
https://doi.org/10.1038/s41420-026-02973-8
Primary Topic
Cancer, Stress, Anesthesia, and Immune Response
Type
article
Field-Weighted Citation Impact
0.00

Funders

Controls
|||
ALL TIME
JAN
FEB
MAR
APR
MAY
JUN
JUL
AUG
SEP
OCT
article

Molecular insights into Silodosin’s anti-cancer effects: a promising repurposing strategy for breast cancer

Stefano Aquaro, Michele Pellegrino, Maria Marra, Paola Tucci et al.
Cell Death Discovery
Cancer, Stress, Anesthesia, and Immune Response
article

Molecular insights into Silodosin’s anti-cancer effects: a promising repurposing strategy for breast cancer

Stefano Aquaro, Michele Pellegrino, Maria Marra, Paola Tucci, Maria Antonietta Occhiuzzi, Stefania Marsico, F. Giordano, Fedora Grande
article en

Abstract

Breast cancer, the most common cancer diagnosed among women worldwide, remains a significant clinical challenge due to its molecular heterogeneity and the development of resistance to conventional therapies. This study investigates the potential of silodosin, an α1A-adrenergic receptor (AR) antagonist, as a novel therapeutic agent in breast cancer, an area where its use has not been previously explored. Through detailed in vitro and in silico analyses, we elucidate the complex molecular mechanisms behind silodosin's antitumor effects. We demonstrate its ability to inhibit cell proliferation, induce apoptosis, reduce migration, and prevent 3D spheroid formation. Importantly, these effects are observed across different breast cancer subtypes. Crucially, our integrated approach reveals that silodosin's mechanism is not solely dependent on α1A-AR blockade. Molecular docking studies strongly suggest that silodosin directly interacts with both isoforms of the estrogen receptor (ERα and ERβ) with high affinity, binding to key residues within the ligand-binding domains of these receptors. This points to a new, dual-targeting mechanism of action. While its known α1A-AR antagonism may contribute to its effects, silodosin could also act as an ER ligand, modulating estrogen-driven pathways essential in breast cancer development. This study provides the first experimental and computational evidence supporting the repurposing of silodosin as a potential multi-targeted therapeutic agent for breast cancer, opening promising new opportunities for patients with limited treatment options and encouraging further preclinical and clinical studies.

Cell Death Discovery
University of L'Aquila (IT), University of Calabria (IT)
Università della Calabria
Good health and well-being
Openalex Percentile: Top 41%
Cancer, Stress, Anesthesia, and Immune Response
AI Navigator

Ask Laika to Summarize, Analyze, and Connect papers live on the map.

Summarize Papers & Methodologies

Extract key findings, datasets, and comparative methods across publications.

Benchmark Rankings & Visual Analytics

Rank top research institutions, authors, funders, topics, and journals by Field-Weighted Citation Impact (FWCI) and paper volume with instant charts.

Connect Distant Disciplines

Bridge topological clusters on the map to find hidden collaborative intersections.