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用于癌症PET/CT成像的放射性标记生长抑素释放肽受体（GRPR）配体的研究进展

Advances of radiolabeled GRPR ligands for PET/CT imaging of cancers.

作者信息

Ma Yuze, Gao Feng

机构信息

Research Center for Experimental Nuclear Medicine, School of Basic Medical Sciences, Cheeloo College of Medicine, Shandong University, Jinan, 250012, Shandong, China.

出版信息

Cancer Imaging. 2024 Jan 26;24(1):19. doi: 10.1186/s40644-024-00658-y.

DOI:10.1186/s40644-024-00658-y
PMID:38279185
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10811881/
Abstract

GRPR is a type of seven-transmembrane G-protein coupled receptor that belongs to the bombesin protein receptor family. It is highly expressed in various cancers, including prostate cancer, breast cancer, lung cancer, gastrointestinal cancer, and so on. As a result, molecular imaging studies have been conducted using radiolabeled GRPR ligands for tumor diagnosis, as well as monitoring of recurrence and metastasis. In this paper, we provided a comprehensive overview of relevant literature from the past two decades, with a specific focus on the advancements made in radiolabeled GRPR ligands for imaging prostate cancer and breast cancer.

摘要

胃泌素释放肽受体（GRPR）是一种七跨膜G蛋白偶联受体，属于蛙皮素蛋白受体家族。它在多种癌症中高度表达，包括前列腺癌、乳腺癌、肺癌、胃肠道癌等。因此，已经开展了使用放射性标记的GRPR配体进行分子成像研究，用于肿瘤诊断以及复发和转移的监测。在本文中，我们对过去二十年的相关文献进行了全面综述，特别关注放射性标记的GRPR配体在前列腺癌和乳腺癌成像方面取得的进展。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/efec/10811881/d05975253d46/40644_2024_658_Fig6_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/efec/10811881/d10094af0c02/40644_2024_658_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/efec/10811881/de8ef04d72d0/40644_2024_658_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/efec/10811881/75102bca0634/40644_2024_658_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/efec/10811881/de28518105b8/40644_2024_658_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/efec/10811881/d47f932253f7/40644_2024_658_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/efec/10811881/d05975253d46/40644_2024_658_Fig6_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/efec/10811881/d10094af0c02/40644_2024_658_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/efec/10811881/de8ef04d72d0/40644_2024_658_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/efec/10811881/75102bca0634/40644_2024_658_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/efec/10811881/de28518105b8/40644_2024_658_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/efec/10811881/d47f932253f7/40644_2024_658_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/efec/10811881/d05975253d46/40644_2024_658_Fig6_HTML.jpg

相似文献

[1]
Advances of radiolabeled GRPR ligands for PET/CT imaging of cancers.

Cancer Imaging. 2024-1-26

[2]
Prospective Study of the Radiolabeled GRPR Antagonist BAY86-7548 for Positron Emission Tomography/Computed Tomography Imaging of Newly Diagnosed Prostate Cancer.

Eur Urol Oncol. 2018-9-22

[3]
Synthesis and biological evaluation of copper-64 radiolabeled [DUPA-6-Ahx-(NODAGA)-5-Ava-BBN(7-14)NH2], a novel bivalent targeting vector having affinity for two distinct biomarkers (GRPr/PSMA) of prostate cancer.

Nucl Med Biol. 2014-4

[4]
A comparative PET imaging study of Sc- and Ga-labeled bombesin antagonist BBN2 derivatives in breast and prostate cancer models.

Nucl Med Biol. 2020

[5]
Preclinical and first clinical experience with the gastrin-releasing peptide receptor-antagonist [⁶⁸Ga]SB3 and PET/CT.

Eur J Nucl Med Mol Imaging. 2016-5

[6]
In vitro and in vivo characterization of novel 18F-labeled bombesin analogues for targeting GRPR-positive tumors.

Bioconjug Chem. 2010-10-20

[7]
In vitro and in vivo evaluation of a 64Cu-labeled NOTA-Bn-SCN-Aoc-bombesin analogue in gastrin-releasing peptide receptor expressing prostate cancer.

Nucl Med Biol. 2012-1-20

[8]
Prostate Cancer Theranostics Targeting Gastrin-Releasing Peptide Receptors.

Mol Imaging Biol. 2018-8

[9]
An update of radiolabeled bombesin analogs for gastrin-releasing peptide receptor targeting.

Curr Pharm Des. 2013

[10]
Small-animal PET of tumors with (64)Cu-labeled RGD-bombesin heterodimer.

J Nucl Med. 2009-7

引用本文的文献

[1]
LAMP1 as a Target for PET Imaging in Adenocarcinoma Xenograft Models.

Pharmaceuticals (Basel). 2025-7-27

[2]
PSMA-Directed Theranostics in Prostate Cancer.

Biomedicines. 2025-7-28

[3]
Emerging PET Imaging Agents and Targeted Radioligand Therapy: A Review of Clinical Applications and Trials.

Tomography. 2025-7-28

[4]
The additive value of Ga-RM26 PET/CT to Ga-PSMA-617 PET/CT in assessing Post-treatment outcomes of ARSIs in mCRPC patients.

Eur J Nucl Med Mol Imaging. 2025-6-16

[5]
Development of Novel Gastrin-Releasing Peptide Receptor-Targeted Radioligand with Albumin Binder to Improve Accumulation in Tumor.

ACS Med Chem Lett. 2025-4-25

[6]
GRPR Drives Metastasis via CRABP2 and FNDC4 Pathways in Lung Adenocarcinoma.

Cells. 2024-12-23

[7]
Peptide-Oligonucleotide Conjugation: Chemistry and Therapeutic Applications.

Curr Issues Mol Biol. 2024-9-30

本文引用的文献

[1]
Comparison of Ga-PSMA-617 PET/CT and Ga-RM2 PET/CT in Patients with Localized Prostate Cancer Who Are Candidates for Radical Prostatectomy: A Prospective, Single-Arm, Single-Center, Phase II Study.

J Nucl Med. 2023-3

[2]
Ga-Labeled [LeuψThz]Bombesin(7-14) Derivatives: Promising GRPR-Targeting PET Tracers with Low Pancreas Uptake.

Molecules. 2022-6-11

[3]
Cancer statistics, 2022.

CA Cancer J Clin. 2022-1

[4]
Radiolabeled Bombesin Analogs.

Cancers (Basel). 2021-11-17

[5]
GRPr Antagonist Ga-SB3 PET/CT Imaging of Primary Prostate Cancer in Therapy-Naïve Patients.

J Nucl Med. 2021-11

[6]
A comparative PET imaging study of Sc- and Ga-labeled bombesin antagonist BBN2 derivatives in breast and prostate cancer models.

Nucl Med Biol. 2020

[7]
Comparison of dedicated breast positron emission tomography and whole-body positron emission tomography/computed tomography images: a common phantom study.

Ann Nucl Med. 2019-11-25

[8]
Comparison of the binding of the gastrin-releasing peptide receptor (GRP-R) antagonist 68Ga-RM2 and 18F-FDG in breast cancer samples.

PLoS One. 2019-1-15

[9]
An Overview of PET Radiochemistry, Part 1: The Covalent Labels F, C, and N.

J Nucl Med. 2018-7-24

[10]
Innovations in Instrumentation for Positron Emission Tomography.

Semin Nucl Med. 2018-3-12

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