Target intelligence / Profile preview

Boron-10-enriched tumor cell DNA and cellular structures (10B-DNA)

Target
10B-DNA
Molecular classification
Isotope-labeled biomolecule, DNA-boron complex, Other
01

Overview

Tumor cell Boron-10-loaded DNA and cellular structures serve as the primary therapeutic target in Boron Neutron Capture Therapy (BNCT), a binary treatment modality for invasive cancers (Barth et al., 2018, CA: A Cancer Journal for Clinicians). This target is established by the selective delivery of the stable isotope boron-10 (10B) into malignant cells using carrier agents such as boronophenylalanine (BPA) or sodium borocaptate (BSH) (Sauerwein et al., 2012, Boron Neutron Capture Therapy). Upon irradiation with low-energy thermal or epithermal neutrons, the 10B atoms within the cellular structures capture a neutron and undergo a nuclear fission reaction [10B(n, alpha)7Li]. This reaction releases high-energy alpha particles and lithium-7 nuclei with a short range of 5–9 micrometers, which is roughly equivalent to one cell diameter (Nedunchezhian et al., 2016, Journal of Clinical and Diagnostic Research). Because the radiation damage is confined to the cells containing the boron, this approach allows for highly localized cell death, primarily through irreparable DNA double-strand breaks, while sparing surrounding healthy tissue. The clinical success of targeting these structures depends on achieving a high tumor-to-normal tissue boron concentration ratio and sufficient neutron flux at the tumor site (Moss, 2014, Applied Radiation and Isotopes).

Other names
10B-loaded cellular structuresBoron-10 targetBNCT targetBoronated DNATumor-localized boron-10
02

Mechanism of action

The target undergoes a boron neutron capture reaction [10B(n, alpha)7Li] upon neutron irradiation, releasing high-linear energy transfer (LET) alpha particles and lithium nuclei that cause localized cellular destruction (Barth et al., 2018).

03

Biological functions

Cell deathDNA damage inductionApoptosis
04

Disease associations

CancerGlioblastoma multiformeHead and neck cancerMelanoma
05

Safety considerations

Off-target neutron capture in healthy tissueInadequate boron delivery to all tumor cellsRadiation-induced necrosisBlood-brain barrier penetration for boron carriers
06

Interacting drugs

Boronophenylalanine (BPA)

2 more in the full profile.

07

Biomarkers

Intracellular boron concentrationTumor-to-blood (T/B) ratio18F-FBPA PET imaging uptake

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