A Metabolically Stable Boron-Derived Tyrosine Serves as a Theranostic Agent for Positron Emission Tomography Guided Boron Neutron Capture Therapy

Li, Jiyuan; Shi, Yaxin; Zhang, Zizhu; Liu, Hui; Lang, Lixin; Liu, Tong; Chen, Xiaoyuan; Liu, Zhibo

doi:10.1021/acs.bioconjchem.9b00578

Cited by 47 publications

(55 citation statements)

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“…Most of the amino acids utilized in BNCT for precise treatment of malignant brain tumors [110], have been reported and the review published recently by Jiyuan et al [111] reported the development of a metabolically stable boron-derived tyrosine (expressed as fluoroboronotyrosine, FBY) as a theranostic agent for both boron delivery and cancer diagnosis, leading to PET imaging-guided BNCT in the treatment of cancer as shown in Figure 9a. The computational study of FBY, Tyrosine, and BPA showed similarities between them to a greater extent.…”

Section: Boron-based Amino Acids For Bnctmentioning

confidence: 99%

Boron Chemistry for Medical Applications

2020

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Boron compounds now have many applications in a number of fields, including Medicinal Chemistry. Although the uses of boron compounds in pharmacological science have been recognized several decades ago, surprisingly few are found in pharmaceutical drugs. The boron-containing compounds epitomize a new class for medicinal chemists to use in their drug designs. Carboranes are a class of organometallic compounds containing carbon (C), boron (B), and hydrogen (H) and are the most widely studied boron compounds in medicinal chemistry. Additionally, other boron-based compounds are of great interest, such as dodecaborate anions, metallacarboranes and metallaboranes. The boron neutron capture therapy (BNCT) has been utilized for cancer treatment from last decade, where chemotherapy and radiation have their own shortcomings. However, the improvement in the already existing (BPA and/or BSH) localized delivery agents or new tumor-targeted compounds are required before realizing the full clinical potential of BNCT. The work outlined in this short review addresses the advancements in boron containing compounds. Here, we have focused on the possible clinical implications of the new and improved boron-based biologically active compounds for BNCT that are reported to have in vivo and/or in vitro efficacy.

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Section: Boron-based Amino Acids For Bnctmentioning

confidence: 99%

Boron Chemistry for Medical Applications

2020

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“…Several other small molecules like [ 18 F]FBPA can be used in this approach, such as the modified boron-derived tyrosine, fluoroboronotyrosine FBY ( Figure 4 ), reported in 2019. FBY, a tyrosine analogue in which a COOH group is replaced by a BF 3 moiety, was proposed as a theranostic agent [ 79 ]. FBY showed superior chemical stability compared with BPA, a high radiochemical yield of 50% and a high radiochemical purity of 98%.…”

Section: Molecular Modalities With Theranostic Applications In Bnctmentioning

confidence: 99%

“…The possibility of non-invasive imaging was indicated by the administration of [ 18 F]FBY to mice followed by PET imaging. Furthermore, FBY shows no obvious systemic toxicity, which renders this compound a very promising theranostic agent for image-guided BNCT [ 79 ]. A small preclinical study with six animals comparing BPA and FBY showed slightly better results for FBY in terms of animal survival and tumor size 3 weeks after BNCT with 1 g/kg intravenous injection of FBY and BPA and 30 min of 10 12 n/(cm 2 s) neutron flux.…”

Section: Molecular Modalities With Theranostic Applications In Bnctmentioning

confidence: 99%

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Theranostics in Boron Neutron Capture Therapy

Sauerwein

Sancey

Hey‐Hawkins

et al. 2021

Life

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Boron neutron capture therapy (BNCT) has the potential to specifically destroy tumor cells without damaging the tissues infiltrated by the tumor. BNCT is a binary treatment method based on the combination of two agents that have no effect when applied individually: 10B and thermal neutrons. Exclusively, the combination of both produces an effect, whose extent depends on the amount of 10B in the tumor but also on the organs at risk. It is not yet possible to determine the 10B concentration in a specific tissue using non-invasive methods. At present, it is only possible to measure the 10B concentration in blood and to estimate the boron concentration in tissues based on the assumption that there is a fixed uptake of 10B from the blood into tissues. On this imprecise assumption, BNCT can hardly be developed further. A therapeutic approach, combining the boron carrier for therapeutic purposes with an imaging tool, might allow us to determine the 10B concentration in a specific tissue using a non-invasive method. This review provides an overview of the current clinical protocols and preclinical experiments and results on how innovative drug development for boron delivery systems can also incorporate concurrent imaging. The last section focuses on the importance of proteomics for further optimization of BNCT, a highly precise and personalized therapeutic approach.

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“…Subsequently, a metabolically stable boron-derived tyrosine (denoted as fluoroboronotyrosine, FBY, Fig. 1b) was developed for boron neutron capture therapy (BNCT), and [ 18 F]-FBY was synthesized and employed for PET image guidance, as well as quantitative and non-invasive evaluation of FBY biodistribution in mouse tumor models [29]. When thermal neutron irradiation was applied, B16F10 tumor-bearing mice injected with FBY showed significantly prolonged median survival without exhibiting obvious systemic toxicity.…”

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confidence: 99%