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A Bis-Boron Amino Acid for Positron Emission Tomography and Boron Neutron Capture Therapy.
Chen, Junyi; Xu, Mengxin; Li, Zhu; Kong, Ziren; Cai, Jie; Wang, Chunhong; Mu, Bo-Shuai; Cui, Xi-Yang; Zhang, Zizhu; Liu, Tong; Liu, Zhibo.
Afiliação
  • Chen J; Peking University, College of Chemistry and Molecular Engineering, CHINA.
  • Xu M; Peking University, College of Chemistry and Molecular Engineering, CHINA.
  • Li Z; Peking University Cancer Hospital, Department of Nuclear Medicine, CHINA.
  • Kong Z; Chinese Academy of Medical Sciences & Peking Union Medical College, Department of Head and Neck Surgery, CHINA.
  • Cai J; Beijing Changping Laboratory, None, CHINA.
  • Wang C; Peking University, College of Chemistry and Molecular Engineering, CHINA.
  • Mu BS; Peking University, College of Chemistry and Molecular Engineering, CHINA.
  • Cui XY; Beijing Changping Laboratory, None, CHINA.
  • Zhang Z; Beijing Nuclear Industry Hospital, None, CHINA.
  • Liu T; Beijing Capture Tech Co.Ltd, None, CHINA.
  • Liu Z; Peking University, College of Chemistry and Molecular Engineering, #5 Yiheyuan Road, Haidian District, 100871, Beijing, CHINA.
Angew Chem Int Ed Engl ; : e202413249, 2024 Sep 30.
Article em En | MEDLINE | ID: mdl-39349362
ABSTRACT
Trifluoroborate boronophenylalanine (BBPA) is a boron amino acid analog of 4­boronophenylalanine (BPA) but with a trifluoroborate group (-BF3-) instead of a carboxyl group (-COOH). Clinical studies have shown that 18F-labeled BBPA ([18F]BBPA) can produce high-contrast tumor images in positron emission tomography (PET). Beyond PET imaging, BBPA is a theranostic agent for boron neutron capture therapy (BNCT). Because BBPA possesses an identical chemical structure to BNCT and PET, it can potentially predict the boron concentration for BNCT using [18F]BBPA-PET. The synthesis of BBPA was achieved by selectively fluorinating the α-aminoborate compound, taking advantage of the varying rates of solvolysis of the B-F bond. The study showcased the high-contrast [18F]BBPA-PET imaging in various tumor models, highlighting its broad applicability for both [18F]BBPA-PET and BBPA-BNCT. [18F]BBPA-PET tumor uptake remains consistent across various doses, including those used in BNCT. This enables accurate estimation of the boron concentration in tumors using [18F]BBPA-PET. With its dual boron structure, BBPA increases boron concentration in tumor cells and tumor tissues compared to BPA. Thus, less boron carrier is needed. This study introduces a new theranostic boron carrier that enhances boron accumulation in tumors, predicts boron concentration, and enhances the accuracy and effectiveness of BNCT.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Idioma: En Revista: Angew Chem Int Ed Engl Ano de publicação: 2024 Tipo de documento: Article País de afiliação: China País de publicação: Alemanha

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Idioma: En Revista: Angew Chem Int Ed Engl Ano de publicação: 2024 Tipo de documento: Article País de afiliação: China País de publicação: Alemanha