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(SiFA)SeFe: A Hydrophilic Silicon-Based Fluoride Acceptor Enabling Versatile Peptidic Radiohybrid Tracers.
Deiser, Sandra; Fenzl, Sebastian; König, Victor; Drexler, Marike; Smith, Lydia M; George, Madeleine E; Beck, Roswitha; Witney, Timothy H; Inoue, Shigeyoshi; Casini, Angela.
Afiliação
  • Deiser S; Chair of Medicinal and Bioinorganic Chemistry, Department of Chemistry, School of Natural Sciences, Technical University of Munich, Lichtenbergstr. 4, 85748 Garching b. München, Germany.
  • Fenzl S; Chair of Pharmaceutical Radiochemistry, Department of Chemistry, School of Natural Sciences, Technical University of Munich, Walther-Meißner-Str. 3, 85748 Garching b. München, Germany.
  • König V; Chair of Pharmaceutical Radiochemistry, Department of Chemistry, School of Natural Sciences, Technical University of Munich, Walther-Meißner-Str. 3, 85748 Garching b. München, Germany.
  • Drexler M; Institute of Silicon Chemistry, Department of Chemistry, School of Natural Sciences, Technical University of Munich, Lichtenbergstr. 4, 85748 Garching b. München, Germany.
  • Smith LM; Chair of Pharmaceutical Radiochemistry, Department of Chemistry, School of Natural Sciences, Technical University of Munich, Walther-Meißner-Str. 3, 85748 Garching b. München, Germany.
  • George ME; Chair of Medicinal and Bioinorganic Chemistry, Department of Chemistry, School of Natural Sciences, Technical University of Munich, Lichtenbergstr. 4, 85748 Garching b. München, Germany.
  • Beck R; Chair of Pharmaceutical Radiochemistry, Department of Chemistry, School of Natural Sciences, Technical University of Munich, Walther-Meißner-Str. 3, 85748 Garching b. München, Germany.
  • Witney TH; School of Biomedical Engineering and Imaging Sciences King's College London St Thomas' Hospital, London SE1 7EH, U.K.
  • Inoue S; School of Biomedical Engineering and Imaging Sciences King's College London St Thomas' Hospital, London SE1 7EH, U.K.
  • Casini A; Chair of Pharmaceutical Radiochemistry, Department of Chemistry, School of Natural Sciences, Technical University of Munich, Walther-Meißner-Str. 3, 85748 Garching b. München, Germany.
J Med Chem ; 67(16): 14077-14094, 2024 Aug 22.
Article em En | MEDLINE | ID: mdl-39115131
ABSTRACT
The radiohybrid (rh) concept to design targeted (and chemically identical) radiotracers for imaging or radionuclide therapy of tumors has gained momentum. For this strategy, a new bifunctional Silicon-based Fluoride Acceptor (SiFA) moiety (SiFA)SeFe was synthesized, endowed with improved hydrophilicity and high versatility of integration into rh-compounds. Preliminary radiolabeling and stability studies under different conditions were conducted using model bioconjugate peptides. Further, three somatostatin receptor 2 (sstR2)-targeted rh-compounds ((SiFA)SeFe-rhTATE1-3, TATE = (Tyr3)-octreotate) were developed. Compound (SiFA)SeFe-rhTATE3, enables labeling with 18F for PET imaging or chelation of 177Lu for therapy. The rh-compounds possess comparable receptor binding affinity and in vitro performance as good as the clinically proven gold standards. SstR2-specificity was further shown for (SiFA)SeFe-rhTATE2 using the chicken chorioallantoic membrane (CAM) model. The biodistribution of two compounds in mice showed high accumulation in tumors and excretion via the kidneys, demonstrating the clinical applicability of the (SiFA)SeFe moiety.
Assuntos

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Receptores de Somatostatina / Interações Hidrofóbicas e Hidrofílicas Limite: Animals / Humans Idioma: En Revista: J Med Chem Assunto da revista: QUIMICA Ano de publicação: 2024 Tipo de documento: Article País de afiliação: Alemanha

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Receptores de Somatostatina / Interações Hidrofóbicas e Hidrofílicas Limite: Animals / Humans Idioma: En Revista: J Med Chem Assunto da revista: QUIMICA Ano de publicação: 2024 Tipo de documento: Article País de afiliação: Alemanha