Review: Radionuclide Molecular Imaging Targeting HER2 in Breast Cancer with a Focus on Molecular Probes into Clinical Trials and Small Peptides

Molecules. 2021 Oct 27;26(21):6482. doi: 10.3390/molecules26216482.

Abstract

As the most frequently occurring cancer worldwide, breast cancer (BC) is the leading cause of cancer-related death in women. The overexpression of HER2 (human epidermal growth factor receptor 2) is found in about 15% of BC patients, and it is often associated with a poor prognosis due to the effect on cell proliferation, migration, invasion, and survival. As a result of the heterogeneity of BC, molecular imaging with HER2 probes can non-invasively, in real time, and quantitatively reflect the expression status of HER2 in tumors. This will provide a new approach for patients to choose treatment options and monitor treatment response. Furthermore, radionuclide molecular imaging has the potential of repetitive measurements, and it can help solve the problem of heterogeneous expression and conversion of HER2 status during disease progression or treatment. Different imaging probes of targeting proteins, such as monoclonal antibodies, antibody fragments, nanobodies, and affibodies, are currently in preclinical and clinical development. Moreover, in recent years, HER2-specific peptides have been widely developed for molecular imaging techniques for HER2-positive cancers. This article summarized different types of molecular probes targeting HER2 used in current clinical applications and the developmental trend of some HER2-specific peptides.

Keywords: HER2; breast cancer; clinical trials; molecular imaging; radionuclide molecular probes.

Publication types

  • Review

MeSH terms

  • Animals
  • Antibodies, Monoclonal / administration & dosage
  • Antibodies, Monoclonal / chemistry
  • Biomarkers, Tumor*
  • Breast Neoplasms / diagnosis*
  • Breast Neoplasms / etiology
  • Breast Neoplasms / metabolism
  • Clinical Trials as Topic
  • Female
  • Humans
  • Immunoconjugates
  • Isotope Labeling
  • Molecular Imaging / methods*
  • Molecular Probes*
  • Peptides* / chemistry
  • Positron-Emission Tomography
  • Radioisotopes
  • Radionuclide Imaging / methods*
  • Receptor, ErbB-2 / metabolism*
  • Recombinant Fusion Proteins
  • Tomography, Emission-Computed, Single-Photon

Substances

  • Antibodies, Monoclonal
  • Biomarkers, Tumor
  • Immunoconjugates
  • Molecular Probes
  • Peptides
  • Radioisotopes
  • Recombinant Fusion Proteins
  • ERBB2 protein, human
  • Receptor, ErbB-2