Peptide Based Imaging Agents for HER2 Imaging in Oncology

Abstract

Breast cancer continues to be the most lethal cancer type in women and one of the most diagnosed. Understanding Breast cancer receptor status is one of the most vital processes for determining treatment options. One type of breast cancer, human epidermal growth factor receptor 2 (HER2) positive, has approved receptor-based therapies including trastuzumab and pertuzumab that can significantly increase the likelihood of survival. Current methods to determine HER2 status include biopsies with immunohistochemical staining and/or fluorescence in situ hybridization. However, positron emission tomography (PET) imaging techniques using 89Zr-trastuzumab or 89Zr-pertuzumab are currently in clinical trials for a non-invasive, full body diagnostic approach. Although the antibodies have strong specificity to the HER2 positive lesions, challenges involving long post-injection time for imaging due to the blood circulation of the antibodies and matching of long-live isotopes leading to increased dose to the patient leave opportunities for alternative PET imaging probes. Peptides have been shown to allow for shorter injection-to-imaging time and can be used with shorter lived isotopes. HER2 specific peptides under development will help improve the diagnosis and potentially therapy options for HER2 positive breast cancer. Peptides showing specificity for HER2 could start widespread development of molecular imaging techniques for HER2 positive cancers.

The Next-Generation Immune Checkpoint LAG-3 and Its Therapeutic Potential in Oncology: Third Time’s a Charm

“…When translated to a clinical setting, the injected patient will have to wait a substantial amount of time before a scan can be performed. Moreover, during this “incubation” time the patient is exposed to a considerable amount of radioactivity [ 94 ]. Therefore, research has focused on using smaller binding moieties with better in vivo penetration capacity to non-invasively detect LAG-3.…”

Anti-cancer peptide-based therapeutic strategies in solid tumors

“…For greater efficiency, attachment of the nuclear localization sequence peptide (NLP) to the KCCYSL peptide leads to translocation of the peptide to the nucleus of HER2 + cells, resulting in cell death. Therefore, KCCYSL-based peptides can be used for imaging of HER2-positive tumors with k d of 295 nM [ 61 ].…”

Phage-Displayed Peptides for Targeting Tyrosine Kinase Membrane Receptors in Cancer Therapy

“…Another HER2-specific peptide (APTHER2) was conjugated with super-paramagnetic nanoparticles (SPION) and injected in HER2-positive tumor-bearing mice, in which it accumulated in the tumor mass, proving the in vivo binding ability to cancer cells [ 121 ]. In this regard, other Her2-targeted peptides have been analyzed in biomedical imaging and treatment as promising tools for imaging HER2-positive cancer patients [ 122 ].…”