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Selective Chelation of the Exotic Meitner-Auger Emitter Mercury-197 m/g with Sulfur-Rich Macrocyclic Ligands: Towards the Future of Theranostic Radiopharmaceuticals.
Randhawa, Parmissa; Gower-Fry, K Lexi; Stienstra, Cailum M K; Tosato, Marianna; Chen, Shaohuang; Gao, Yang; McDonagh, Anthony W; Di Marco, Valerio; Radchenko, Valery; Schreckenbach, Georg; Ramogida, Caterina F.
Afiliación
  • Randhawa P; Department of Chemistry, Simon Fraser University, 8888 University Drive, V5A 1S6, Burnaby, British Columbia, Canada.
  • Gower-Fry KL; Life Sciences Division, TRIUMF, 4004 Wesbrook Mall, V6T 2A3, Vancouver, British Columbia, Canada.
  • Stienstra CMK; Department of Chemistry, Simon Fraser University, 8888 University Drive, V5A 1S6, Burnaby, British Columbia, Canada.
  • Tosato M; Life Sciences Division, TRIUMF, 4004 Wesbrook Mall, V6T 2A3, Vancouver, British Columbia, Canada.
  • Chen S; Life Sciences Division, TRIUMF, 4004 Wesbrook Mall, V6T 2A3, Vancouver, British Columbia, Canada.
  • Gao Y; Department of Chemistry, Simon Fraser University, 8888 University Drive, V5A 1S6, Burnaby, British Columbia, Canada.
  • McDonagh AW; Life Sciences Division, TRIUMF, 4004 Wesbrook Mall, V6T 2A3, Vancouver, British Columbia, Canada.
  • Di Marco V; Department of Chemical Sciences, University of Padova, via Marzolo 1, 35131, Padova, Italy.
  • Radchenko V; Department of Chemistry, Simon Fraser University, 8888 University Drive, V5A 1S6, Burnaby, British Columbia, Canada.
  • Schreckenbach G; Life Sciences Division, TRIUMF, 4004 Wesbrook Mall, V6T 2A3, Vancouver, British Columbia, Canada.
  • Ramogida CF; Department of Chemistry, University of Manitoba, 140 Dysart Rd, R3T 2N2, Winnipeg, Manitoba, Canada.
Chemistry ; 29(21): e202203815, 2023 Apr 13.
Article en En | MEDLINE | ID: mdl-36701527
Mercury-197 m/g are a promising pair of radioactive isomers for incorporation into a theranostic as they can be used as a diagnostic agent using SPECT imaging and a therapeutic via Meitner-Auger electron emissions. However, the current absence of ligands able to stably coordinate 197m/g Hg to a tumour-targeting vector precludes their use in vivo. To address this, we report herein a series of sulfur-rich chelators capable of incorporating 197m/g Hg into a radiopharmaceutical. 1,4,7,10-Tetrathia-13-azacyclopentadecane (NS4 ) and its derivatives, (2-(1,4,7,10-tetrathia-13-azacyclopentadecan-13-yl)acetic acid (NS4 -CA) and N-benzyl-2-(1,4,7,10-tetrathia-13-azacyclopentadecan-13-yl)acetamide (NS4 -BA), were designed, synthesized and analyzed for their ability to coordinate Hg2+ through a combination of theoretical (DFT) and experimental coordination chemistry studies (NMR and mass spectrometry) as well as 197m/g Hg radiolabeling studies and in vitro stability assays. The development of stable ligands for 197m/g Hg reported herein is extremely impactful as it would enable their use for in vivo imaging and therapy, leading to personalized treatments for cancer.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Radiofármacos / Mercurio Idioma: En Revista: Chemistry Asunto de la revista: QUIMICA Año: 2023 Tipo del documento: Article País de afiliación: Canadá Pais de publicación: Alemania
Texto completo
Añadir a Mi BVS
Imprimir
XML
PubMed Links
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Radiofármacos / Mercurio Idioma: En Revista: Chemistry Asunto de la revista: QUIMICA Año: 2023 Tipo del documento: Article País de afiliación: Canadá Pais de publicación: Alemania