<sup>99m</sup>Tc Labeling of Highly Potent Small Peptides

Liu, S; Edwards, David S.; Barrett, John

doi:10.1021/bc970058b

Cited by 149 publications

(112 citation statements)

References 114 publications

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“…This conclusion is also supported by the coligand effect observed in this and our previous studies [28]. The HYNIC technology and its utility in the development of targetspecific radiopharmaceuticals have been reviewed extensively [49][50][51][52].…”

Section: Radiochemistrysupporting

confidence: 83%

Coligand effects on the solution stability, biodistribution and metabolism of the 99mTc-labeled cyclic RGDfK tetramer

Liu

Kim

Hsieh

et al. 2008

Nuclear Medicine and Biology

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In this study, we present the evaluation of two new ternary ligand 99m Tc complexes [ 99m Tc(HYNICtetramer)(tricine)(L)] (L = ISONIC and PDA) as potential radiotracers for tumor imaging. The athymic nude mice bearing the MDA-MB-435 human breast cancer xenografts were used to evaluate their biodistribution and metabolic properties. The solution stability data showed that [ 99m Tc (HYNIC-tetramer)(tricine)(L)] (L = ISONIC and PDA) had a significant (14% and 35%, respectively) at 6 h in the absence of excess ISONIC or PDA coligand. Biodistribution data clearly showed that [ 99m Tc(HYNIC-tetramer)(tricine)(PDA)] has much lower uptake in most organs of interest than [ 99m Tc(HYNIC-tetramer)(tricine)(ISONIC)] during the 2 h study period. Results from metabolism studies revealed that ~50% of [ 99m Tc(HYNIC-tetramer)(tricine)(ISONIC)] remained intact in feces samples at 120 min p.i. Only 10% of [ 99m Tc(HYNIC-tetramer)(tricine)(PDA)] remained intact in feces samples. The extent of metabolism correlates well with the radiotracer solution stability. The results from this and our previous studies clearly demonstrated that coligands (TPPTS, ISONIC and PDA) have a significant impact on tumor uptake, excretion kinetics and metabolism of the 99m Tc-labeled cyclic RGDfK tetramer. Among the three radiotracers evaluated in this tumor-bearing animal model, [ 99m Tc(HYNIC-tetramer)(tricine)(TPPTS)] remains the best with respect to blood clearance, tumor uptake, target/background ratios.

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Section: Radiochemistrysupporting

confidence: 83%

Coligand effects on the solution stability, biodistribution and metabolism of the 99mTc-labeled cyclic RGDfK tetramer

Liu

Kim

Hsieh

et al. 2008

Nuclear Medicine and Biology

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“…They may be classified into three main categories: direct labeling, preformed chelate approach, and indirect labeling approach (26,27). The direct labeling approach usually uses a reducing agent to convert a number of disulfide linkages into free thiols, which are able to bind to 99mTc efficiently.…”

Section: Discussionmentioning

confidence: 99%

Comparison of two purified toxic fractions from Mesobuthus eupeus scorpion venom

Shirmardi¹,

Shamsaei²,

Ghanei³

et al. 2010

J. Venom. Anim. Toxins incl. Trop. Dis

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Abstract:Iranian scorpions belong mainly to the Buthidae and Scorpionidae families, distributed into 16 genera and 25 species. In Iran, similar to other parts of the world, there are a few known species of scorpions responsible for severe envenoming; amongst which Mesobuthus eupeus is the most common. Its venom contains several toxin fractions that may affect the ion channel. In the present study purification, labeling and biological evaluation of M. eupeus venom are described. For separation, soluble venom was loaded on a chromatography column packed with Sephadex G-50 gel. Subsequently, the fractions were collected according to UV absorption at a wavelength of 280 nm. Toxic fraction (F3) was loaded on an anionic ion exchanger resin and then on a cationic resin. Finally, toxic subfractions F3.1.6 and F3.1.9 were labeled with 99m Tc and injected into normal mice to distinguish excretion pathway. The venom toxic fraction was successfully obtained in its purified form. Radiolabeling of toxic fractions was performed at high specific activity with radiochemical purity of more than 97 and 95% respectively for F3.1.6 and F3.1.9. Biodistribution studies in normal mice with two toxic fractions usually show rapid clearance of the compounds from blood and tissue except for kidneys. Since tissue distribution studies are very important for clinical purpose, the present findings suggest that 99m Tc labeling of venom is a useful tool for in vivo studies and comprises an excellent approach to monitoring the process of biodistribution and kinetics of toxins.

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“…One particular radionuclide that is commonly used is technetium-99 m, or 99m Tc. This radioisotope has an ideal half-life of 6 h and emits readily detectable 140 keV gamma rays (107). It currently has several applications in the medical field, ranging from identifying angiogenesis via attachment to monoclonal antibodies to evaluating ventricular function by conjugation to red blood cells (108,109).…”

Section: Radiolabelingmentioning

confidence: 99%

“…One of the most common methods used is to take an organometallic precursor, such as the tricarbonyl molecule [ 99m Tc(OH 2 ) 3 (CO) 3 ] + (110), and complex it to a tridentate ligand that is already attached to the molecule of interest (107). This ligand is typically based on the amino acids cysteine, lysine, and especially histidine (111).…”

Section: Radiolabelingmentioning

confidence: 99%

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Click Chemistry, A Powerful Tool for Pharmaceutical Sciences

2008

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Abstract. Click chemistry refers to a group of reactions that are fast, simple to use, easy to purify, versatile, regiospecific, and give high product yields. While there are a number of reactions that fulfill the criteria, the Huisgen 1,3-dipolar cycloaddition of azides and terminal alkynes has emerged as the frontrunner. It has found applications in a wide variety of research areas, including materials sciences, polymer chemistry, and pharmaceutical sciences. In this manuscript, important aspects of the Huisgen cycloaddition will be reviewed, along with some of its many pharmaceutical applications. Bioconjugation, nanoparticle surface modification, and pharmaceutical-related polymer chemistry will all be covered. Limitations of the reaction will also be discussed.

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^99mTc Labeling of Highly Potent Small Peptides

Cited by 149 publications

References 114 publications

Coligand effects on the solution stability, biodistribution and metabolism of the 99mTc-labeled cyclic RGDfK tetramer

Coligand effects on the solution stability, biodistribution and metabolism of the 99mTc-labeled cyclic RGDfK tetramer

Comparison of two purified toxic fractions from Mesobuthus eupeus scorpion venom

Click Chemistry, A Powerful Tool for Pharmaceutical Sciences

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