Diagnostic and Therapeutic Radiopharmaceuticals: A “Hot” Topic

Lindsley, Craig W.; Müller, Christa E.; Bongarzone, Salvatore

doi:10.1021/acs.jmedchem.3c02281

Cited by 2 publications

(1 citation statement)

References 51 publications

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“…Improved radiopharmaceutical design and delivery, along with deeper insights into the biochemical and genetic mechanisms governing tumor progression, allow for tailored detection and disease stratification as well as therapy. Recently, radiopharmaceutical design has been defined as a “hot” topic and a rapidly evolving matter [ 16 ], and the contributions in this Special Issue encompass a wide range of research studies which elucidate the richness of this field.…”

Section: Discussionmentioning

confidence: 99%

Editorial for the Special Issue “Molecular Biology in Targeted Radionuclide Therapy Radiopharmaceutical Design”

Aprile,

Geatti,

Canziani

et al. 2024

CIMB

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Section: Discussionmentioning

confidence: 99%

Editorial for the Special Issue “Molecular Biology in Targeted Radionuclide Therapy Radiopharmaceutical Design”

Aprile,

Geatti,

Canziani

et al. 2024

CIMB

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Development of a Novel, Easy-to-Prepare, and Potentially Valuable Peptide Coupling Technology Utilizing Amide Acid as a Linker

Wang,

Yang,

2024

Pharmaceuticals

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The process of synthesizing radionuclide-coupled drugs, especially shutdown technology that links bipotent chelators with biomolecules, utilizes traditional coupling reactions, including emerging click chemistry; these reactions involve different drawbacks, such as complex and cumbersome reaction steps, long reaction times, and the use of catalysts at various pH values, which can negatively impact the effects of the chelating agent. To address the above problems in this study, This research designed a novel bipotent chelator coupled with peptides. In the present study, dichloromethane was used as a solvent, and the reaction was conducted at room temperature for 12 h. A one-step ring-opening method was employed to introduce the coupling functional group of tridentate amide acid. The coupling materials consisted of the amino active site of the peptide and diethylene glycol anhydride. In this paper, this study explored the reactions between different equivalents of acid anhydride coupled to the peptide (peptide sequence: HLRKLRKR) and determined that the maximum conversion of the peptide feedstock was 87%. To determine the selectivity of the reaction sites in this polypeptide, This study identified the peptide sequence at the reaction site using nuclear magnetic resonance (NMR) and liquid chromatography–mass spectrometry (LC-MS). For the selected peptide, the first reactive site was on the terminal amino group, followed by the amino group on the tetra- and hepta-lysine side chains. The tridentate amic acid framework functions as a chelating agent, capable of binding a range of lanthanide ions. This significantly reduces and optimizes the time and cost associated with synthesizing radionuclide-coupled drugs.

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Diagnostic and Therapeutic Radiopharmaceuticals: A “Hot” Topic

Cited by 2 publications

References 51 publications

Editorial for the Special Issue “Molecular Biology in Targeted Radionuclide Therapy Radiopharmaceutical Design”

Editorial for the Special Issue “Molecular Biology in Targeted Radionuclide Therapy Radiopharmaceutical Design”

Development of a Novel, Easy-to-Prepare, and Potentially Valuable Peptide Coupling Technology Utilizing Amide Acid as a Linker

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