Bioconjugation Methods for Radiopharmaceutical Chemistry

Cardinale, Jens; Giammei, Carolina; Jouini, Nédra; Mindt, Thomas L.

doi:10.1007/978-3-319-98947-1_25

Cited by 7 publications

(8 citation statements)

References 47 publications

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“…193 To this end, the chemoselectivity and sitespecificity of the modification reaction are essential in creating homogenous radiolabelled bioconjugates. 191,194 The chemoselectivity refers to the ability of the targeting vector to react preferentially at one reactive functional group over another while site-specificity denotes the ability of a biomolecule to be functionalised at a single position. 191,194 Amongst a sea of reactive amines, thiols, carboxylic acids and alcohols located at different positions on biomolecules, the latter often proves to be the most challenging task.…”

Section: Bioconjugation Strategiesmentioning

confidence: 99%

“…191,194 The chemoselectivity refers to the ability of the targeting vector to react preferentially at one reactive functional group over another while site-specificity denotes the ability of a biomolecule to be functionalised at a single position. 191,194 Amongst a sea of reactive amines, thiols, carboxylic acids and alcohols located at different positions on biomolecules, the latter often proves to be the most challenging task. 195 Random conjugation of the BFC to various sites on the biomolecule can affect the biological activity and pharmacokinetics of the resulting conjugate, therefore it is vital that precise control over bioconjugation may be attained for the effective clinical use of the radiopharmaceutical.…”

Section: Bioconjugation Strategiesmentioning

confidence: 99%

“…195 Random conjugation of the BFC to various sites on the biomolecule can affect the biological activity and pharmacokinetics of the resulting conjugate, therefore it is vital that precise control over bioconjugation may be attained for the effective clinical use of the radiopharmaceutical. 191,194 The majority of bioconjugation strategies make use of the side chains of lysine (-NH 2 ) and cysteine (-SH) residues on biomolecules, with the cysteine free thiols having a lower abundance in biomolecules and making their use more siteselective. 195 The popular reaction of the lysine primary amines…”

Section: Bioconjugation Strategiesmentioning

confidence: 99%

Section: Approaches To Radiolabelling Biomolecules With Radiorheniummentioning

confidence: 99%

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Bifunctional chelators for radiorhenium: past, present and future outlook

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Section: Bioconjugation Strategiesmentioning

confidence: 99%

Section: Bioconjugation Strategiesmentioning

confidence: 99%

Section: Bioconjugation Strategiesmentioning

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Bifunctional chelators for radiorhenium: past, present and future outlook

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“…Having understood that both functionalization and radiolabeling procedures must keep the biological properties of native biomolecules unaltered, whatever the approach, two other important aspects need to be considered to generate effective homogenous immunoconjugates: the chemoselectivity and site-specificity of the bioconjugation reaction [24,25]. The first is referred to the ability of a reagent to react selectively with only one type of functional group in the presence of other potential reactive groups.…”

Section: Overview Of Radiolabeling Strategies For Biomoleculesmentioning

confidence: 99%

Enzymatic Methods for the Site-Specific Radiolabeling of Targeting Proteins

Bolzati

Spolaore

2021

Molecules

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Site-specific conjugation of proteins is currently required to produce homogenous derivatives for medicine applications. Proteins derivatized at specific positions of the polypeptide chain can actually show higher stability, superior pharmacokinetics, and activity in vivo, as compared with conjugates modified at heterogeneous sites. Moreover, they can be better characterized regarding the composition of the derivatization sites as well as the conformational and activity properties. To this aim, several site-specific derivatization approaches have been developed. Among these, enzymes are powerful tools that efficiently allow the generation of homogenous protein–drug conjugates under physiological conditions, thus preserving their native structure and activity. This review will summarize the progress made over the last decade on the use of enzymatic-based methodologies for the production of site-specific labeled immunoconjugates of interest for nuclear medicine. Enzymes used in this field, including microbial transglutaminase, sortase, galactosyltransferase, and lipoic acid ligase, will be overviewed and their recent applications in the radiopharmaceutical field will be described. Since nuclear medicine can benefit greatly from the production of homogenous derivatives, we hope that this review will aid the use of enzymes for the development of better radio-conjugates for diagnostic and therapeutic purposes.

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Chemistry of Antimony in Radiopharmaceutical Development: Unlocking the Theranostic Potential of Sb Isotopes

Grundmane,

Radchenko,

Ramogida

2024

ChemPlusChem

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Antimony‐119 (119Sb) holds promise for radiopharmaceutical therapy (RPT), emitting short‐range Auger and conversion electrons that can deliver cytotoxic radiation on a cellular level. While it has high promise theoretically, experimental validation is necessary for 119Sb in vivo applications. Current 119Sb production and separation methods face robustness and compatibility challenges in radiopharmaceutical synthesis. Limited progress in chelator development hampers targeted experiments with 119Sb. This review compiles literature on the toxicological, biodistribution and redox properties of Sb, along with existing Sb complexes, evaluating their suitability for radiopharmaceuticals. Sb(III) is suggested as the preferred oxidation state for radiopharmaceutical elaboration due to its stability in vivo and lack of skeletal uptake. While Sb complexes with both hard and soft donor atoms can be achieved, Sb thiol complexes offer enhanced stability and compatibility with the desired Sb(III) oxidation state. For 119Sb to find application in RPT, scientists need to make discoveries and advancements in the areas of isotope production, and radiometal chelation. This review aims to guide future research towards harnessing the therapeutic potential of 119Sb in RPT.

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Bioconjugation Methods for Radiopharmaceutical Chemistry

Cited by 7 publications

References 47 publications

Bifunctional chelators for radiorhenium: past, present and future outlook

Bifunctional chelators for radiorhenium: past, present and future outlook

Enzymatic Methods for the Site-Specific Radiolabeling of Targeting Proteins

Chemistry of Antimony in Radiopharmaceutical Development: Unlocking the Theranostic Potential of Sb Isotopes

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