Breast cancer is the leading cause of
cancer deaths among women of all ages worldwide. With advances in molecular imaging procedures, it has been possible to detect
breast cancer in its early stage, determine the extent of the disease to administer appropriate therapeutic protocol and also monitor the effects of treatment. By accurately characterizing the
tumor properties and biological processes involved, molecular imaging can play a crucial role in minimizing the morbidity and mortality associated with
breast cancer. The
integrin αvβ3 plays an important role in
breast cancer angiogenesis and is expressed on
tumor endothelial cells as well as on some
tumor cells. It is a receptor for the
extracellular matrix proteins with the exposed
arginine-glycine-aspartic acid (
RGD) tripeptide sequence and therefore RGD
peptides can preferentially bind to
integrin αvβ3. In this context, targeting
tumor vasculature or
tumor cells by RGD-based probes is a promising strategy for molecular imaging of
breast cancer. Using RGD-based probes, several preclinical studies have employed different imaging modalities such as positron emission tomography (PET), single photon emission computed tomography (SPECT), magnetic resonance imaging (MRI), ultrasound and optical imaging for visualization of
integrin αvβ3 expression in
breast cancer models. Limited clinical trials using (18)F-labeled RGD
peptides have also been initiated for non-invasive detection and staging of
breast cancer. Herein, we provide a comprehensive overview of the latest advances in molecular imaging of
breast cancer using
RGD peptide-based probes and discuss the challenges and opportunities for advancement of the field. The reported strategies for molecular imaging of
breast cancer using
RGD peptide-based probes holds promise for making clinically translatable advances that can positively impact the overall diagnostic and therapeutic processes and result in improved quality of life for
breast cancer patients.