NHS-MAS3: a bifunctional chelator alternative to NHS-MAG3.

  title={NHS-MAS3: a bifunctional chelator alternative to NHS-MAG3.},
  author={F. Chang and T. Qu and M. Rusckowski and D. Hnatowich},
  journal={Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine},
  volume={50 4},
  • F. Chang, T. Qu, +1 author D. Hnatowich
  • Published 1999
  • Chemistry, Medicine
  • Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine
This laboratory uses an N-hydroxysuccinimide derivative of S-acetylmercaptoacetyltriglycine (NHS-MAG3) to conjugate amines for subsequent labeling with 99mTc. However, the synthesis from triglycerine is general and not restricted to this tripeptide. We had earlier selected a small number of alternative tripeptides and synthesized the corresponding NHS derivatives. Each was then evaluated in a search for bifunctional chelators with properties superior to NHS-MAG3, such as lower serum protein… Expand
Technetium-99m labeled peptides--an investigation of multiple HPLC peaks.
One conclusion from this investigation is that the appearance of a single peak by any HPLC analysis offers no assurance that multiple peaks would not appear on alternative HPLC analyses, and evidence that each species is due to radiolabeled active peptide and not to radiocontaminants is therefore potentially more important than evidence of asingle peak. Expand
99mTc-chelator engineering to improve tumour targeting properties of a HER2-specific Affibody molecule
The introduction of serine residues in the chelator results in better tumour imaging properties of the Affibody molecule ZHER2:342 compared with glycyl-containing chelators and is favourable for imaging of tumours and metastases in the abdominal area. Expand
The solid phase synthesis and NMR spectroscopy of a 99Tc chelate–bombesin derived peptide conjugate
Abstract A bombesin derived peptide–99Tc chelate conjugate was prepared using a solid phase synthetic methodology. The reported approach involved linking a prefabricated bifunctional N2N′S technetiumExpand
A comparison in monkeys of (99m)Tc labeled to a peptide by 4 methods.
The method of radiolabeling had an important effect on the biodistribution of (99m)Tc and although biodist distribution results in mice should be used with caution to predict biodistributions in primates, in major organs, these results in monkeys were similar. Expand
Production of Multimeric Prostate-Specific Membrane Antigen Small-Molecule Radiotracers Using a Solid-Phase 99mTc Preloading Strategy
A simple cartridge-based, solid-phase prelabeling strategy that converts readily available and inexpensive 99mTc-pertechnetate into a chemically pure complex, with a reactive N-hydroxysuccinimide (NHS) ester, in neat organic solvent is developed. Expand
An HPLC/mass spectrometry platform for the development of multimodality contrast agents and targeted therapeutics: prostate-specific membrane antigen small molecule derivatives.
A general-purpose HPLC/mass spectrometry platform capable of purifying virtually any targeted agent for any modality and the preparation of five small molecule derivatives specific for prostate-specific membrane antigen (PSMA) is described. Expand
Preparation, 99mTc-labeling and biodistribution studies of a PNA oligomer containing a new ligand derivative of 2,2'-dipicolylamine.
A new azido derivative of 2,2'-dipicolylamine (Dpa), 2-azido-N,N-bis((pyridin-2-yl)methyl)ethanamine, (Dpa-N(3)) was readily prepared from the known 2-(bis(pyridin-2-ylmethyl)amino)ethanol (Dpa-OH).Expand
Update: affibody molecules for molecular imaging and therapy for cancer.
Affibody molecules meet the requirements which are key for successful clinical use as imaging agents: high-affinity binding to the chosen target; short plasma half-life time; rapid renal clearance for nonbound drug substance and, high, continuously increasing tumor-to-organ ratios, resulting in high-contrast in vivo images shortly after injection of the diagnostic agent. Expand
Synthesis, characterization, and evaluation of radiometal-containing peptide nucleic acids.
This book chapter reports on the current developments towards the preparation of radiometal-containing PNA constructs and summarizes the protocols for labeling these probes with (99m)Tc, (111)In, (64)Cu, (90)Y, and (177)Lu. Expand
Metal-containing peptide nucleic acid conjugates.
The latest advances on the preparation and utilisation of PNA monomers and oligomers containing metal complexes are discussed, including in the sequence-specific detection of nucleic acids and peptides. Expand


Preparation and use of NHS-MAG3 for technetium-99m labeling of DNA.
It is concluded that the S-acetyl NHS MAG3 bifunctional chelator may prove to be an attractive alternative method of radiolabeling DNA and other biologically important molecules with 99mTc. Expand
The influence of temperature and alkaline pH on the labeling of free and conjugated MAG3 with technetium-99m.
S-acetyl MAG3 conjugated compounds may be radiolabeled at ambient temperature and neutral pH in most cases, and the radiochemical species produced appear to be identical to those formed when labeling is accomplished at 95 degrees C or pH 11. Expand
In vivo hybridization of technetium-99m-labeled peptide nucleic acid (PNA).
The ability of the PNA to hybridize in vitro with its complement appeared to be unimpaired after conjugation and radiolabeling and 99mTc-PNA displays stability and pharmacokinetic properties suitable for eventual use as radiopharmaceuticals. Expand
Can a cysteine challenge assay predict the in vivo behavior of 99mTc-labeled antibodies?
The relative in vivo behaviour of 99mTc when administered to mice while labeled to two IgG antibodies were successfully predicted based on the results of an in vitro cysteine challenge assay. Expand
Early results in the irrational design of new bifunctional chelators
The development of a simple route for the synthesis of the N‐hydroxysuccinimide (NHS) ester of S‐acetyl‐protected mercaptoacetyltriglycine (MAG3) has opened the possibility of preparing novelExpand
A new reagent which may be used to introduce sulfhydryl groups into proteins, and its use in the preparation of conjugates for immunoassay.
A synthesis of the N-hydroxysuccinimide ester of S-acetylthioacetic acid is described, which has advantages over the currently available reagents used to introduce sulfhydryl groups into a variety of proteins. Expand