A Selective Carborane-Functionalized Gastrin-Releasing Peptide Receptor Agonist as Boron Delivery Agent for Boron Neutron Capture Therapy
| Autor: | Hans-Georg Lerchen, Stefan Saretz, Bernd Riedl, Evamarie Hey-Hawkins, Johannes Köbberling, Annette G. Beck-Sickinger, Sylvia Els-Heindl, Robert Kuhnert, Paul Hoppenz, Martin Kellert |
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| Rok vydání: | 2019 |
| Předmět: |
inorganic chemicals
Agonist Boron Compounds medicine.drug_class medicine.medical_treatment chemistry.chemical_element Healthy tissue Boron Neutron Capture Therapy 010402 general chemistry 01 natural sciences medicine Gastrin-releasing peptide receptor Boron Boranes Boron Delivery Agent 010405 organic chemistry Organic Chemistry 0104 chemical sciences Radiation therapy Receptors Bombesin Neutron capture chemistry Cancer research Carborane Peptides |
| Zdroj: | The Journal of organic chemistry. 85(3) |
| ISSN: | 1520-6904 |
| Popis: | Boron neutron capture therapy (BNCT) allows the selective elimination of malignant tumor cells without affecting healthy tissue. Although this binary radiotherapy approach has been known for decades, BNCT failed to reach the daily clinics to date. One of the reasons is the lack of selective boron delivery agents. Using boron loaded peptide conjugates, which address G protein-coupled receptors overexpressed on tumor cells allow the intracellular accumulation of boron. The gastrin-releasing peptide receptor (GRPR) is a well-known target in cancer diagnosis and can potentially be used for BNCT. Here, we present the successful introduction of multiple bis-deoxygalactosyl-carborane building blocks to the GRPR-selective ligand [d-Phe |
| Databáze: | OpenAIRE |
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