Synthesis and biological characterization of <sup>99m</sup>Tc(I) tricarbonyl cysteine complex, a potential diagnostic for assessment of renal function

Park, Sang Hyun; Jang, Beom Su; Park, Kyung Bae

doi:10.1002/jlcr.897

Cited by 5 publications

(4 citation statements)

References 21 publications

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“…This observation has been confirmed in 2005 by Park et al 13 However, cysteine in proteins is not believed to play an important role in 99m Tc-tricarbonyl fixation, as this amino acid is less common than histidine. Moreover, the thiol function is often oxidized to disulphide bond (cystine), a well known poor chelating group.…”

Section: Introductionsupporting

confidence: 74%

Improvement in radiolabelling proteins with the99mTc-tricarbonyl-core [99mTc(CO)3]+, by thiol-derivatization with iminothiolane: application to γ-globulins and annexin V

Biechlin

d′Hardemare

Fraysse

et al. 2005

J Label Compd Radiopharm

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SummaryThe aim of this study was to improve the radiolabelling of proteins with the 99m Tctricarbonyl-[Tc(I)(CO) 3 ] + core by introducing thiol groups to their structure. To achieve this goal, g-globulins and annexin V were derivatized with mercaptobutyrimidyl groups (MBG) after reaction with 2-iminothiolane. The optimal conditions permitted attachment of an average of 3.3 thiol groups on g-globulins and 1.0 to annexin V. The radiolabelling assays were carried out by incubating 3.2 nmol of either g-globulin-SH or unmodified g-globulin with 60 MBq 99m Tc-tricarbonyl produced from an Isolink 1 kit (Mallinckrodt) under different reaction conditions. Results clearly showed that the introduction of three MBG could double the radiolabelling yields to more than 90% in a short time (30 mn, 378C). Such results would never have been reached with unmodified g-globulins alone. Under the same conditions when using 1-2 nmol derivatized annexin V, the average radiolabelling yield was 55% against 19% with the unmodified protein. The 99m Tc-tricarbonyl-conjugates were challenged with cysteine or histidine and showed good stability.

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Section: Introductionsupporting

confidence: 74%

Improvement in radiolabelling proteins with the99mTc-tricarbonyl-core [99mTc(CO)3]+, by thiol-derivatization with iminothiolane: application to γ-globulins and annexin V

Biechlin

d′Hardemare

Fraysse

et al. 2005

J Label Compd Radiopharm

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“…A 99m Tc-tricarbonyl precursor was successfully prepared using a procedure described (Park et al ., 2005). The yield was higher than 98%.…”

Section: Resultsmentioning

confidence: 99%

“…Many attempts have been made for the labeling of small peptides with 99m Tc (Park et al ., 2005; Reubi, 1995; Fischman et al ., 1993; McAfee and Neumann, 1996; Lee et al ., 2010).…”

Section: Introductionmentioning

confidence: 99%

Biodistribution of^99mTc Tricarbonyl Glycine Oligomers

Jang¹,

Lee²,

Rho³

et al. 2012

Toxicological Research

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99mTc tricarbonyl glycine monomers, trimers, and pentamers were synthesized and evaluated for their radiolabeling and in vivo distribution characteristics. We synthesized a 99mTc-tricarbonyl precursor with a low oxidation state (I). 99mTc(CO)3(H2O)3 + was then made to react with monomeric and oligomeric glycine for the development of bifunctional chelating sequences for biomolecules. Labeling yields of 99mTc-tricarbonyl glycine monomers and oligomers were checked by high-performance liquid chromatography. The labeling yields of 99mTc-tricarbonyl glycine and glycine oligomers were more than 95%. We evaluated the characteristics of 99mTc-tricarbonyl glycine oligomers by carrying out a lipophilicity test and an imaging study. The octanol-water partition coefficient of 99mTc tricarbonyl glycine oligomers indicated hydrophilic properties. Single-photon emission computed tomography imaging of 99mTc-tricarbonyl glycine oligomers showed rapid renal excretion through the kidneys with a low uptake in the liver, especially of 99mTc tricarbonyl triglycine. Furthermore, we verified that the addition of triglycine to prototype biomolecules (AGRGDS and RRPYIL) results in the improvement of radiolabeling yield. From these results, we conclude that triglycine has good characteristics for use as a bifunctional chelating sequence for a 99mTc-tricarbonyl- based biomolecular imaging probe.

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“…Dithiocarbamates provide only two chelating sulfur atoms but, in combination with phosphine derivatives, 161 a suitable environment for Tc(CO) 3 is created. The simple technetium tricarbonyl cysteine complex 162,163 can be used as a radiopharmaceutical in its own right. It has even proved possible to make carborane complexes 164 labelled with technetium tricarbonyl.…”

Section: Technetium ( 94mand99m Tc)mentioning

confidence: 99%

Radiochemistry and radiopharmaceuticals

Urch

Welch

2006

Annu. Rep. Prog. Chem., Sect. A: Inorg. Chem.

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Following last year's precedent this section of Annual Reports will review not only recent progress in radiochemistry, including isotope production and environmental aspects, but also in the production of radiopharmaceuticals and their use in nuclear medicine for imaging. Radiation chemistry (unless related to the stability of labelled molecules), the use of nuclear activation analysis and the inorganic chemistry of elements that are by their nature, radioactive are all excluded. HighlightsThe IAEA published 1 the results of a wide ranging review of nuclear measurements. Conferences held during 2005 which covered progress in radiochemistry, included the '4th all Polish Conference on Radiochemistry and Nuclear Chemistry' 2 and the '7th Nuclear and Radiochemistry Symposium' 3 whilst a more focused meeting dealt with the production and application of labelled compounds 4 in the oil industry. A couple of very interesting articles appeared during 2005 questioning what exactly is meant by many fundamental 'radiochemical' concepts 5 such as 'specific activity' and 'carrier-free' and indeed how the specific activities 6 of 'no-carrier-added' materials can be determined. The Proceedings of the 16th Symposium on Radiopharmaceutical Chemistry 7 covers advances made in radiopharmaceutical development and applications while the Proceedings of the Society of Nuclear Medicine 8 and the European Society of Nuclear Medicine 9 cover both radiopharmaceutical development and the application in diagnosis and therapy. A critical review has been published 10 on the application of positron emitting nuclides for use as radiopharmaceuticals.

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Synthesis and biological characterization of ^99mTc(I) tricarbonyl cysteine complex, a potential diagnostic for assessment of renal function

Cited by 5 publications

References 21 publications

Improvement in radiolabelling proteins with the99mTc-tricarbonyl-core [99mTc(CO)3]+, by thiol-derivatization with iminothiolane: application to γ-globulins and annexin V

Improvement in radiolabelling proteins with the99mTc-tricarbonyl-core [99mTc(CO)3]+, by thiol-derivatization with iminothiolane: application to γ-globulins and annexin V

Biodistribution of^99mTc Tricarbonyl Glycine Oligomers

Radiochemistry and radiopharmaceuticals

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Synthesis and biological characterization of 99mTc(I) tricarbonyl cysteine complex, a potential diagnostic for assessment of renal function

Cited by 5 publications

References 21 publications

Improvement in radiolabelling proteins with the99mTc-tricarbonyl-core [99mTc(CO)3]+, by thiol-derivatization with iminothiolane: application to γ-globulins and annexin V

Improvement in radiolabelling proteins with the99mTc-tricarbonyl-core [99mTc(CO)3]+, by thiol-derivatization with iminothiolane: application to γ-globulins and annexin V

Biodistribution of99mTc Tricarbonyl Glycine Oligomers

Radiochemistry and radiopharmaceuticals

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Synthesis and biological characterization of ^99mTc(I) tricarbonyl cysteine complex, a potential diagnostic for assessment of renal function

Biodistribution of^99mTc Tricarbonyl Glycine Oligomers