Current State of Radiolabeled Heterobivalent Peptidic Ligands in Tumor Imaging and Therapy
Over the past few years, an approach emerged that combines different receptor-specific peptide radioligands able to bind different target structures on tumor cells concomitantly or separately. The reason for the growing interest in this special field of radiopharmaceutical development is rooted in t...
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| Format: | Article |
| Language: | English |
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MDPI AG
2020-07-01
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| Series: | Pharmaceuticals |
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| Online Access: | https://www.mdpi.com/1424-8247/13/8/173 |
| _version_ | 1797560750741389312 |
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| author | Benedikt Judmann Diana Braun Björn Wängler Ralf Schirrmacher Gert Fricker Carmen Wängler |
| author_facet | Benedikt Judmann Diana Braun Björn Wängler Ralf Schirrmacher Gert Fricker Carmen Wängler |
| author_sort | Benedikt Judmann |
| collection | DOAJ |
| description | Over the past few years, an approach emerged that combines different receptor-specific peptide radioligands able to bind different target structures on tumor cells concomitantly or separately. The reason for the growing interest in this special field of radiopharmaceutical development is rooted in the fact that bispecific peptide heterodimers can exhibit a strongly increased target cell avidity and specificity compared to their corresponding monospecific counterparts by being able to bind to two different target structures that are overexpressed on the cell surface of several malignancies. This increase of avidity is most pronounced in the case of concomitant binding of both peptides to their respective targets but is also observed in cases of heterogeneously expressed receptors within a tumor entity. Furthermore, the application of a radiolabeled heterobivalent agent can solve the ubiquitous problem of limited tumor visualization sensitivity caused by differential receptor expression on different tumor lesions. In this article, the concept of heterobivalent targeting and the general advantages of using radiolabeled bispecific peptidic ligands for tumor imaging or therapy as well as the influence of molecular design and the receptors on the tumor cell surface are explained, and an overview is given of the radiolabeled heterobivalent peptides described thus far. |
| first_indexed | 2024-03-10T18:04:56Z |
| format | Article |
| id | doaj.art-2611f8967a024c50aa6358d448bc0dcc |
| institution | Directory Open Access Journal |
| issn | 1424-8247 |
| language | English |
| last_indexed | 2024-03-10T18:04:56Z |
| publishDate | 2020-07-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceuticals |
| spelling | doaj.art-2611f8967a024c50aa6358d448bc0dcc2023-11-20T08:32:39ZengMDPI AGPharmaceuticals1424-82472020-07-0113817310.3390/ph13080173Current State of Radiolabeled Heterobivalent Peptidic Ligands in Tumor Imaging and TherapyBenedikt Judmann0Diana Braun1Björn Wängler2Ralf Schirrmacher3Gert Fricker4Carmen Wängler5Biomedical Chemistry, Department of Clinical Radiology and Nuclear Medicine, Medical Faculty Mannheim of Heidelberg University, 68167 Mannheim, GermanyBiomedical Chemistry, Department of Clinical Radiology and Nuclear Medicine, Medical Faculty Mannheim of Heidelberg University, 68167 Mannheim, GermanyMolecular Imaging and Radiochemistry, Department of Clinical Radiology and Nuclear Medicine, Medical Faculty Mannheim of Heidelberg University, 68167 Mannheim, GermanyDepartment of Oncology, Division of Oncological Imaging, University of Alberta, Edmonton, AB T6G 1Z2, CanadaInstitute of Pharmacy and Molecular Biotechnology, University of Heidelberg, 69120 Heidelberg, GermanyBiomedical Chemistry, Department of Clinical Radiology and Nuclear Medicine, Medical Faculty Mannheim of Heidelberg University, 68167 Mannheim, GermanyOver the past few years, an approach emerged that combines different receptor-specific peptide radioligands able to bind different target structures on tumor cells concomitantly or separately. The reason for the growing interest in this special field of radiopharmaceutical development is rooted in the fact that bispecific peptide heterodimers can exhibit a strongly increased target cell avidity and specificity compared to their corresponding monospecific counterparts by being able to bind to two different target structures that are overexpressed on the cell surface of several malignancies. This increase of avidity is most pronounced in the case of concomitant binding of both peptides to their respective targets but is also observed in cases of heterogeneously expressed receptors within a tumor entity. Furthermore, the application of a radiolabeled heterobivalent agent can solve the ubiquitous problem of limited tumor visualization sensitivity caused by differential receptor expression on different tumor lesions. In this article, the concept of heterobivalent targeting and the general advantages of using radiolabeled bispecific peptidic ligands for tumor imaging or therapy as well as the influence of molecular design and the receptors on the tumor cell surface are explained, and an overview is given of the radiolabeled heterobivalent peptides described thus far.https://www.mdpi.com/1424-8247/13/8/173aviditydual targetingheterobivalencyimagingpeptidesPET |
| spellingShingle | Benedikt Judmann Diana Braun Björn Wängler Ralf Schirrmacher Gert Fricker Carmen Wängler Current State of Radiolabeled Heterobivalent Peptidic Ligands in Tumor Imaging and Therapy Pharmaceuticals avidity dual targeting heterobivalency imaging peptides PET |
| title | Current State of Radiolabeled Heterobivalent Peptidic Ligands in Tumor Imaging and Therapy |
| title_full | Current State of Radiolabeled Heterobivalent Peptidic Ligands in Tumor Imaging and Therapy |
| title_fullStr | Current State of Radiolabeled Heterobivalent Peptidic Ligands in Tumor Imaging and Therapy |
| title_full_unstemmed | Current State of Radiolabeled Heterobivalent Peptidic Ligands in Tumor Imaging and Therapy |
| title_short | Current State of Radiolabeled Heterobivalent Peptidic Ligands in Tumor Imaging and Therapy |
| title_sort | current state of radiolabeled heterobivalent peptidic ligands in tumor imaging and therapy |
| topic | avidity dual targeting heterobivalency imaging peptides PET |
| url | https://www.mdpi.com/1424-8247/13/8/173 |
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