99m Tc-labeling experiments on CCK 4 by a direct method

Rossin, Raffaella; Blok, D.; Visentin, R.; Feitsma, R.I.J.; Giron, Maria Cecilia; Pauwels, E. K. J.; Mazzi, Ulderico

doi:10.1016/s0969-8051(01)00254-2

Cited by 13 publications

(9 citation statements)

References 15 publications

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“…When the target molecule is a high molecular weight homopolymer, 99m Tc labeling leads to minor changes in charge, conformation, and hydrophilicity, without significant changes in biodistribution and physiological interactions. Because HA and HA-But contain many functional groups, useful to bind the 99m Tc(V)oxo core (carboxylic, hydroxylic, and amino groups), a direct method to label the two polymeric species with 99m Tc was applied (14,21). Briefly, 99m Tcpertechnetate, freshly eluted from a 99 Mo/ 99m Tc generator (Nycomed-Amersham-Sorin, Saluggia, Italy), was reduced with 1 l of a 0.1 M SnCl 2 solution (in 0.1 M HCl) in the presence of sodium gluconate (1 l of a 10 -2 M solution) as exchange ligand.…”

Section: Methodsmentioning

confidence: 99%

Inhibition of Hepatocellular Carcinomas in vitro and Hepatic Metastases in vivo in Mice by the Histone Deacetylase Inhibitor HA-But

Coradini

Zorzet

Rossin

et al. 2004

Clinical Cancer Research

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Purpose:The purpose is to evaluate the CD44-mediated cellular targeting of HA-But, a hyaluronic acid esterified with butyric acid (But) residues, to hepatocellular carcinoma cell lines in vitro and to hepatic tumor metastases in vivo.Experimental Design: In vitro, the CD44-dependent cytotoxicity in two human hepatocellular carcinoma cell lines (HepB3 and HepG2) with high and low CD44 expression was investigated; in vivo, the effect on liver metastases originating from intrasplenic implants of Lewis lung carcinoma (LL3) or B16-F10 melanoma in mice was compared with the pharmacokinetics of organ and tissue distribution using different routes of administration.Results: HepB3 and HepG2 cell lines showed different expression of CD44 (78 and 18%, respectively), which resulted in a CD44-dependent HA-But inhibitory effect as demonstrated also by the uptake analysis performed using radiolabeled HA-But ( Conclusions: HA-But tends to concentrate in the liver and spleen and appears to be a promising new drug for the treatment of intrahepatic tumor lesions.

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Section: Methodsmentioning

confidence: 99%

Inhibition of Hepatocellular Carcinomas in vitro and Hepatic Metastases in vivo in Mice by the Histone Deacetylase Inhibitor HA-But

Coradini

Zorzet

Rossin

et al. 2004

Clinical Cancer Research

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“…followed by a substitution reaction. 44 According to a recent finding by the group of Ferro Flores et al, 45,46 the labeling of a fragment of the synthetic cationic antimicrobial peptide ubiquicidin 29-41 results in a dimeric peptide complex with Arg 7 and Lys being the most suitable binding sites for 99m Tc indicating that residual amines are involved (Fig. 3).…”

Section: Labeling Of Peptides With Technetium-99mmentioning

confidence: 98%

The Pharmacology of Radiolabeled Cationic Antimicrobial Peptides

Brouwer

Wulferink

Welling

2008

Journal of Pharmaceutical Sciences

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“…This method is used in the preparations of many Tcessential radiopharmaceuticals because it is easy to perform [7][8][9] ; but it usually applies to macro biomolecules and a few numbers of small biomolecules such as octreotide and CCK, because many small biomolecules have no disulfide linkage, or in many cases, these bonds are crucial for their biological activities. 10,11 In addition, there is little control over the solution stability of the 99m Tc radiotracer. However, there are several questions for this approach that need to be answered such as number of bonded 99m Tc to a biomolecule (BM), oxidation state of technetium, number of technetium-species in the radiolabeled biomolecule, and the effect of 99m Tc-labeling on the biological properties.…”

Section: Direct Labeling Approachmentioning

confidence: 99%

Study of the ^99mTc‐labeling conditions of 6‐hydrazinonicotinamide‐conjugated peptides from a new perspective: Introduction to the term radio‐stoichiometry

Kaihani

Sadeghzadeh

2020

Labelled Comp Radiopharmac

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Specific tumor uptake of peptide radiopharmaceuticals depends on tumor binding affinity and their radiochemical purity. Several important parameters that influence the 99mTc‐labeling and consequently the radiochemical purity of 6‐hydrazinonicotinamide (HYNIC)‐conjugated peptide are radionuclide activity, the amount of peptide, the amount of coligands, and the amount of reducing agents (stannous ion). In this review article, we have attempted studying these parameters in the HYNIC‐conjugated peptides (somatostatin, cholecystokinin/gastrin, bombesin, and RGD analogs) from a new perspective to obtain most used and optimized radio‐stoichiometric relationships. One of the most important results in this review is that for 99mTc‐labeling of HYNIC‐conjugated peptides, it is better to consider the most calculated mole ratio between technetium‐99m and the peptide (mole ratio of technetium‐99m to the peptide 1:200–400). The statistical results also show that among these 99mTc‐labeled peptides, the most used and favorable coligand is tricine/EDDA with two to one (2:1) mole ratio. These optimized radio‐stoichiometric relationships, favorable coligand mole ratio, and applicable radiolabeling points can greatly improve the labeling process of the HYNIC‐conjugated peptides, by reducing trial and error, increasing specific activity, and saving materials.

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99m Tc-labeling experiments on CCK 4 by a direct method

Cited by 13 publications

References 15 publications

Inhibition of Hepatocellular Carcinomas in vitro and Hepatic Metastases in vivo in Mice by the Histone Deacetylase Inhibitor HA-But

Inhibition of Hepatocellular Carcinomas in vitro and Hepatic Metastases in vivo in Mice by the Histone Deacetylase Inhibitor HA-But

The Pharmacology of Radiolabeled Cationic Antimicrobial Peptides

Study of the ^99mTc‐labeling conditions of 6‐hydrazinonicotinamide‐conjugated peptides from a new perspective: Introduction to the term radio‐stoichiometry

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99m Tc-labeling experiments on CCK 4 by a direct method

Cited by 13 publications

References 15 publications

Inhibition of Hepatocellular Carcinomas in vitro and Hepatic Metastases in vivo in Mice by the Histone Deacetylase Inhibitor HA-But

Inhibition of Hepatocellular Carcinomas in vitro and Hepatic Metastases in vivo in Mice by the Histone Deacetylase Inhibitor HA-But

The Pharmacology of Radiolabeled Cationic Antimicrobial Peptides

Study of the 99mTc‐labeling conditions of 6‐hydrazinonicotinamide‐conjugated peptides from a new perspective: Introduction to the term radio‐stoichiometry

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Product

Resources

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Study of the ^99mTc‐labeling conditions of 6‐hydrazinonicotinamide‐conjugated peptides from a new perspective: Introduction to the term radio‐stoichiometry