Radiolabeled Bombesin Analogs

The gastrin-releasing peptide receptor (GRPR) is expressed in high numbers in a variety of human tumors, including the frequently occurring prostate and breast cancers, and therefore provides the rationale for directing diagnostic or therapeutic radionuclides on cancer lesions after administration o...

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Autores principales:	Rosalba Mansi, Berthold A. Nock, Simone U. Dalm, Martijn B. Busstra, Wytske M. van Weerden, Theodosia Maina
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	gastrin-releasing peptide receptor radiolabeled bombesin cancer theranostics Neoplasms. Tumors. Oncology. Including cancer and carcinogens RC254-282
Acceso en línea:	https://doaj.org/article/b5307ffe34c94955b6238c35c393b099
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id	oai:doaj.org-article:b5307ffe34c94955b6238c35c393b099
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spelling	oai:doaj.org-article:b5307ffe34c94955b6238c35c393b0992021-11-25T17:03:45ZRadiolabeled Bombesin Analogs10.3390/cancers132257662072-6694https://doaj.org/article/b5307ffe34c94955b6238c35c393b0992021-11-01T00:00:00Zhttps://www.mdpi.com/2072-6694/13/22/5766https://doaj.org/toc/2072-6694The gastrin-releasing peptide receptor (GRPR) is expressed in high numbers in a variety of human tumors, including the frequently occurring prostate and breast cancers, and therefore provides the rationale for directing diagnostic or therapeutic radionuclides on cancer lesions after administration of anti-GRPR peptide analogs. This concept has been initially explored with analogs of the frog 14-peptide bombesin, suitably modified at the N-terminus with a number of radiometal chelates. Radiotracers that were selected for clinical testing revealed inherent problems associated with these GRPR agonists, related to low metabolic stability, unfavorable abdominal accumulation, and adverse effects. A shift toward GRPR antagonists soon followed, with safer analogs becoming available, whereby, metabolic stability and background clearance issues were gradually improved. Clinical testing of three main major antagonist types led to promising outcomes, but at the same time brought to light several limitations of this concept, partly related to the variation of GRPR expression levels across cancer types, stages, previous treatments, and other factors. Currently, these parameters are being rigorously addressed by cell biologists, chemists, nuclear medicine physicians, and other discipline practitioners in a common effort to make available more effective and safe state-of-the-art molecular tools to combat GRPR-positive tumors. In the present review, we present the background, current status, and future perspectives of this endeavor.Rosalba MansiBerthold A. NockSimone U. DalmMartijn B. BusstraWytske M. van WeerdenTheodosia MainaMDPI AGarticlegastrin-releasing peptide receptorradiolabeled bombesincancer theranosticsNeoplasms. Tumors. Oncology. Including cancer and carcinogensRC254-282ENCancers, Vol 13, Iss 5766, p 5766 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	gastrin-releasing peptide receptor radiolabeled bombesin cancer theranostics Neoplasms. Tumors. Oncology. Including cancer and carcinogens RC254-282
spellingShingle	gastrin-releasing peptide receptor radiolabeled bombesin cancer theranostics Neoplasms. Tumors. Oncology. Including cancer and carcinogens RC254-282 Rosalba Mansi Berthold A. Nock Simone U. Dalm Martijn B. Busstra Wytske M. van Weerden Theodosia Maina Radiolabeled Bombesin Analogs
description	The gastrin-releasing peptide receptor (GRPR) is expressed in high numbers in a variety of human tumors, including the frequently occurring prostate and breast cancers, and therefore provides the rationale for directing diagnostic or therapeutic radionuclides on cancer lesions after administration of anti-GRPR peptide analogs. This concept has been initially explored with analogs of the frog 14-peptide bombesin, suitably modified at the N-terminus with a number of radiometal chelates. Radiotracers that were selected for clinical testing revealed inherent problems associated with these GRPR agonists, related to low metabolic stability, unfavorable abdominal accumulation, and adverse effects. A shift toward GRPR antagonists soon followed, with safer analogs becoming available, whereby, metabolic stability and background clearance issues were gradually improved. Clinical testing of three main major antagonist types led to promising outcomes, but at the same time brought to light several limitations of this concept, partly related to the variation of GRPR expression levels across cancer types, stages, previous treatments, and other factors. Currently, these parameters are being rigorously addressed by cell biologists, chemists, nuclear medicine physicians, and other discipline practitioners in a common effort to make available more effective and safe state-of-the-art molecular tools to combat GRPR-positive tumors. In the present review, we present the background, current status, and future perspectives of this endeavor.
format	article
author	Rosalba Mansi Berthold A. Nock Simone U. Dalm Martijn B. Busstra Wytske M. van Weerden Theodosia Maina
author_facet	Rosalba Mansi Berthold A. Nock Simone U. Dalm Martijn B. Busstra Wytske M. van Weerden Theodosia Maina
author_sort	Rosalba Mansi
title	Radiolabeled Bombesin Analogs
title_short	Radiolabeled Bombesin Analogs
title_full	Radiolabeled Bombesin Analogs
title_fullStr	Radiolabeled Bombesin Analogs
title_full_unstemmed	Radiolabeled Bombesin Analogs
title_sort	radiolabeled bombesin analogs
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/b5307ffe34c94955b6238c35c393b099
work_keys_str_mv	AT rosalbamansi radiolabeledbombesinanalogs AT bertholdanock radiolabeledbombesinanalogs AT simoneudalm radiolabeledbombesinanalogs AT martijnbbusstra radiolabeledbombesinanalogs AT wytskemvanweerden radiolabeledbombesinanalogs AT theodosiamaina radiolabeledbombesinanalogs
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Radiolabeled Bombesin Analogs

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