TY - JOUR
T1 - Bioconjugates of Chelators with Peptides and Proteins in Nuclear Medicine
T2 - Historical Importance, Current Innovations, and Future Challenges
AU - Jackson, Jessica A
AU - Hungnes, Ingebjørg N
AU - Ma, Michelle T
AU - Rivas, Charlotte
PY - 2020/3/18
Y1 - 2020/3/18
N2 - Molecular radiopharmaceuticals based on bioconjugates of chelators with peptides and proteins have had significant clinical impact in the diagnosis and treatment of several types of cancers. In the 1990s, indium-111 and yttrium-90 labeled chelator-peptide/protein conjugates established the clinical utility of these radiopharmaceuticals for receptor-targeted γ-scintigraphy imaging and systemic radiotherapy. Second-generation bioconjugates based on peptides targeting the somatostatin II receptor and the prostate-specific membrane antigen are now widely used for management of neuroendocrine and prostate cancer, respectively. These bioconjugates are typically radiolabeled with gallium-68 for imaging of target receptor expression with positron emission tomography, and the β--emitter, lutetium-177, for targeted radiotherapy. Innovations in radioisotope technology and biomolecular therapies are likely to drive the future clinical development of radiopharmaceuticals based on radiometals. New chelator-peptide and chelator-protein bioconjugates will underpin nuclear medicine advances in molecular imaging and radiotherapy.
AB - Molecular radiopharmaceuticals based on bioconjugates of chelators with peptides and proteins have had significant clinical impact in the diagnosis and treatment of several types of cancers. In the 1990s, indium-111 and yttrium-90 labeled chelator-peptide/protein conjugates established the clinical utility of these radiopharmaceuticals for receptor-targeted γ-scintigraphy imaging and systemic radiotherapy. Second-generation bioconjugates based on peptides targeting the somatostatin II receptor and the prostate-specific membrane antigen are now widely used for management of neuroendocrine and prostate cancer, respectively. These bioconjugates are typically radiolabeled with gallium-68 for imaging of target receptor expression with positron emission tomography, and the β--emitter, lutetium-177, for targeted radiotherapy. Innovations in radioisotope technology and biomolecular therapies are likely to drive the future clinical development of radiopharmaceuticals based on radiometals. New chelator-peptide and chelator-protein bioconjugates will underpin nuclear medicine advances in molecular imaging and radiotherapy.
UR - http://www.scopus.com/inward/record.url?scp=85082095333&partnerID=8YFLogxK
U2 - 10.1021/acs.bioconjchem.0c00015
DO - 10.1021/acs.bioconjchem.0c00015
M3 - Review article
C2 - 31990543
SN - 1043-1802
VL - 31
SP - 483
EP - 491
JO - Bioconjugate Chemistry
JF - Bioconjugate Chemistry
IS - 3
ER -
