Abstract
Targeted receptor-mediated imaging techniques have become crucial tools in present targeted diagnosis and radiotherapy as they provide accurate and specific diagnosis of disease information. Peptide-based pharmaceuticals are gaining popularity, and there has been vast interest in developing 68Ga-labeled bombesin (Bn) analogs. The gastrin-releasing peptide (GRP) family and its Bn analog have been implicated in the biology of several human cancers. The three bombesin receptors GRP, NMB, and BRS-3 receptor are most frequently ectopically expressed by common, important malignancies. The low expression of Bn/GRP receptors in normal tissue and relatively high expression in a variety of human tumors can be of biological importance and form a molecular basis for Bn/GRP receptor-mediated imaging. To develop a Bn-like peptide with favorable tumor targeting and pharmacokinetic characteristics for possible clinical use, several modifications in the Bn-like peptides, such as the use of a variety of chelating agents, i.e., acyclic and macrocyclic agents with different spacer groups and with different metal ions (gallium), have been performed in recent years without significant disturbance of the vital binding scaffold. The favorable physical properties of 68Ga, i.e., short half-life, and the fast localization of small peptides make this an ideal combination to study receptor-mediated imaging in patients.
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Abbreviations
- Ac:
-
Acetyl
- Aca:
-
Aminohexanoic acid
- ACMpip:
-
4-Aminocarboxymethylpiperidine
- AMBA:
-
Aminobenzoyl
- Bn/BBN:
-
Bombesin
- BRS-3:
-
Bombesin receptor subtype 3
- Bzdig:
-
p-aminobenzyldiglycolic acid
- BZH3 :
-
[DTyr6,βAla11,Thi13,Nle14]Bn(6–14)
- Cha:
-
Cyclohexylalanine
- DOTA:
-
1,4,7,10-Triazacyclododecanetetraacetic acid
- DTPA:
-
Diethylenetriaminepentaacetic acid
- Des-Met:
-
Methionine removed
- FA01010:
-
(4R,5S)-4-Amino-5-methylheptanoic acid
- GRP:
-
Gastrin-releasing peptide
- GRP-R/GRPR:
-
Gastrin-releasing peptide receptor
- GPR-R/GPRR:
-
G-protein receptor
- Ga:
-
Gallium
- GI:
-
Gastrointestinal
- mIP:
-
meta-phenylalanine
- MBq:
-
Megabecquerel
- NHEt:
-
Et = ethyl
- NMB:
-
Neuromedin B
- NMBR:
-
Neuromedin B receptor
- NOTA:
-
1,4,7-Triazacyclononanetriacetic acid
- PEG2:
-
(2-Aminoethyl)-carboxymethyl ether
- PEG4:
-
15-Amino-4,7,10,13-tetraoxapentadecanoic acid
- PET:
-
Positron emission tomography
- RM1:
-
H-DPhe-Gln-Trp-Ala-Val-Gly-His-Sta-Leu-NH2
- RGD:
-
(Arginine-glycine-aspartic acid)
- SPECT:
-
Single-photon emission computed tomography
- Sta:
-
Statine: (3S,4S)-4-amino-3-hydroxy-6-methylheptanoic acid
- Tha:
-
β-(2-Thienyl) alanine
- Thi:
-
3-(2-Thienyl) alanine
- Tpi:
-
2,3,4,9-Tetrahydro-1H-pyridol[3,4-b]indol-3-carboxylic acid
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Varshney, R., Hazari, P.P., Fernandez, P., Schulz, J., Allard, M., Mishra, A. . (2013). 68Ga-Labeled Bombesin Analogs for Receptor-Mediated Imaging. In: Baum, R., Rösch, F. (eds) Theranostics, Gallium-68, and Other Radionuclides. Recent Results in Cancer Research, vol 194. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-27994-2_12
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