This following article is written for Prof. Abba Kastin's Festschrift, to add to the tribute to his important role in the advancement of the role of peptides in physiological, as well as pathophysiological processes. There have been many advances during the 35 years of his prominent role in the Peptide field, not only as editor of the journal Peptides, but also as a scientific investigator and editor of two volumes of the Handbook of Biological Active Peptides [146,147]. Similar to the advances with many different peptides, during this 35 year period, there have been much progress made in the understanding of the pharmacology, cell biology and the role of (bombesin) Bn receptors and their ligands in various disease states, since the original isolation of bombesin from skin of the European frog Bombina bombina in 1970 [76]. This paper will briefly review some of these advances over the time period of Prof. Kastin 35 years in the peptide field concentrating on the advances since 2007 when many of the results from earlier studies were summarized [128,129]. It is appropriate to do this because there have been 280 articles published in Peptides during this time on bombesin-related peptides and it accounts for almost 5% of all publications. Furthermore, 22 Bn publications we have been involved in have been published in either Peptides [14,39,55,58,81,92,93,119,152,216,225,226,231,280,302,309,355,361,362] or in Prof. Kastin's Handbook of Biological Active Peptides [137,138,331].
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http://dx.doi.org/10.1016/j.peptides.2015.04.026 | DOI Listing |
Theranostics
December 2024
Department of Nuclear Medicine, Inselspital, University of Bern, Bern, Switzerland.
Radiopharmaceutical therapy (RPT) is an emerging prostate cancer treatment that delivers radiation to specific molecules within the tumor microenvironment (TME), causing DNA damage and cell death. Given TME heterogeneity, it's crucial to explore RPT dosimetry and biological impacts at the cellular level. We integrated spatial transcriptomics (ST) with computational modeling to investigate the effects of RPT targeting prostate-specific membrane antigen (PSMA), fibroblast activation protein (FAP), and gastrin-releasing peptide receptor (GRPR) each labelled with beta-emitting lutetium-177 (Lu) and alpha-emitting actinium-225 (Ac).
View Article and Find Full Text PDFPharmaceutics
October 2024
Immunology and Molecular Oncology Diagnostics Unit, Veneto Institute of Oncology IOV-IRCCS, 35128 Padua, Italy.
Prostate cancer (PC) represents the second most diagnosed form of cancer in men on a global scale. Despite the theranostic efficacy of prostate-specific membrane antigen (PSMA) radioligands, there is a spectrum of PC disease in which PSMA expression is low or absent. The gastrin-releasing peptide receptor (GRPR), also known as the bombesin type 2 receptor, has been identified as a target in both the early and advanced stages of PC.
View Article and Find Full Text PDFSovrem Tekhnologii Med
November 2024
DSc, Leading Researcher, Laboratory for Peptide Drugs and Vaccines Development, S.P. Kapitsa Research Institute of Technology; Ulyanovsk State University, 42 Leo Tolstoy St., Ulyanovsk, 432017, Russia.
Unlabelled: Bombesin receptors on the cell surface are of great interest as a target for targeted cancer therapy. One of the strategies of targeting bombesin receptors involves the use of tropic short peptides. However, the main limitation for the wide application of peptides as drugs is their low stability due to their sensitivity to extreme conditions of the internal body environment such as temperature and action of enzymes.
View Article and Find Full Text PDFMol Pharm
December 2024
Department of Molecular Oncology, BC Cancer Research Institute, Vancouver, British Columbia V5Z 1L3, Canada.
The gastrin-releasing peptide receptor (GRPR) is overexpressed in a variety of cancers and represents a promising target for diagnosis and therapy. However, the extremely high accumulation in the pancreas observed for most of the clinically evaluated GRPR-targeted radiopharmaceuticals could limit their applications. In this study, we synthesized one GRPR antagonist (ProBOMB5) and two GRPR agonists (LW02056 and LW02057) by replacing the 4-thiazolidinecarboxylic acid (Thz) residue in our previously reported GRPR-targeted tracers with Pro.
View Article and Find Full Text PDFFront Nucl Med
September 2023
Radiochemical Studies Laboratory, Energy & Safety, Institute of Nuclear & Radiological Sciences & Technology (INRASTES), National Centre for Scientific Research (NCSR) "Demokritos", Athens, Greece.
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