Current state of radiolabeled heterobivalent peptidic ligands in tumor imaging and therapy

24Citations
Citations of this article
33Readers
Mendeley users who have this article in their library.

Abstract

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.

References Powered by Scopus

Integrins: Bidirectional, allosteric signaling machines

7440Citations
N/AReaders
Get full text

The causes and consequences of genetic heterogeneity in cancer evolution

1743Citations
N/AReaders
Get full text

The molecular evolution of acquired resistance to targeted EGFR blockade in colorectal cancers

1456Citations
N/AReaders
Get full text

Cited by Powered by Scopus

Rgd-binding integrins revisited: How recently discovered functions and novel synthetic ligands (re-)shape an ever-evolving field

137Citations
N/AReaders
Get full text

[<sup>68</sup>Ga]Ga-iPSMA-Lys<sup>3</sup>-Bombesin: Biokinetics, dosimetry and first patient PET/CT imaging

19Citations
N/AReaders
Get full text

PSMA-targeted low-molecular double conjugates for diagnostics and therapy

12Citations
N/AReaders
Get full text

Register to see more suggestions

Mendeley helps you to discover research relevant for your work.

Already have an account?

Cite

CITATION STYLE

APA

Judmann, B., Braun, D., Wängler, B., Schirrmacher, R., Fricker, G., & Wängler, C. (2020). Current state of radiolabeled heterobivalent peptidic ligands in tumor imaging and therapy. Pharmaceuticals, 13(8), 1–31. https://doi.org/10.3390/ph13080173

Readers' Seniority

Tooltip

PhD / Post grad / Masters / Doc 12

67%

Researcher 4

22%

Professor / Associate Prof. 2

11%

Readers' Discipline

Tooltip

Pharmacology, Toxicology and Pharmaceut... 5

38%

Biochemistry, Genetics and Molecular Bi... 4

31%

Chemistry 2

15%

Medicine and Dentistry 2

15%

Article Metrics

Tooltip
Mentions
Blog Mentions: 1
Social Media
Shares, Likes & Comments: 31

Save time finding and organizing research with Mendeley

Sign up for free