Labeling of fatty acid ligands with the strong electrophilic metal fragment [99mTc(N)(PNP)]2+ (PNP=diphosphane ligand)

Bioconjugate Chemistry
Emiliano CazzolaA Duatti

Abstract

The electrophilic metal fragment [(99m)Tc(N)(PNP)](2+) (PNP=diphosphane ligand) has been employed for the labeling of fatty acid chains of different lengths. To provide a site-specific group for the attachment of the metallic moiety, the fatty acid derivatives were functionalized by appending a bis-mercapto or, alternatively, a dithiocarbamato pi-donor chelating systems to one terminus of the carbon chain to yield both dianionic and monoanionic bifunctional ligands (L). The resulting complexes, [(99m)Tc(N)(PNP)(L)] (0/+), exhibited the usual asymmetrical structure in which a Tc(triple bond)N group was surrounded by two different bidentate chelating ligands. Dianionic ligands gave rise to neutral complexes, while monoanionic ligands afforded monocationic species. Biodistribution studies were carried out in rats. An isolated perfused rat heart model was employed to assess how structural changes in the radiolabeled fatty acid compound affect the myocardial first pass extraction. Results showed that only monocationic complexes accumulated in myocardium to a significant extent. Conversely, neutral complexes were not efficiently retained into the heart region and rapidly washed out. In isolated perfused rat heart experiments, monocat...Continue Reading

References

Jan 1, 1991·International Journal of Radiation Applications and Instrumentation. Part B, Nuclear Medicine and Biology·R H MachY Z Guo
May 1, 1986·Proceedings of the National Academy of Sciences of the United States of America·W Stremmel, P D Berk
Aug 5, 1999·Seminars in Nuclear Medicine·J R Corbett
Jan 6, 2001·Annals of Biomedical Engineering·H R Schelbert
Nov 20, 2003·Bioconjugate Chemistry·Alessandra BoschiPier Andrea Borea
Mar 18, 2004·Bioconjugate Chemistry·Yasuhiro MagataHideo Saji
Apr 28, 2004·Applied Radiation and Isotopes : Including Data, Instrumentation and Methods for Use in Agriculture, Industry and Medicine·Taiwei ChuXiangyun Wang
Dec 19, 2006·Journal of Nuclear Cardiology : Official Publication of the American Society of Nuclear Cardiology·Kengo HatadaDavid K Glover
Feb 3, 2007·Journal of Medicinal Chemistry·Tomoya UeharaYasushi Arano
Jul 13, 2007·Nuclear Medicine Communications·Anke C HeintzAndreas Deussen

❮ Previous
Next ❯

Citations

Jul 26, 2014·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Oxana V KharissovaPerla Elizondo Martínez
Feb 12, 2017·Journal of Labelled Compounds & Radiopharmaceuticals·Jianping LiuHuabei Zhang
Aug 3, 2017·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Anna Lucia TorneselloFranco Maria Buonaguro
Nov 29, 2013·Journal of Labelled Compounds & Radiopharmaceuticals·Huahui ZengMei Tian
Jan 17, 2013·Dalton Transactions : an International Journal of Inorganic Chemistry·Huahui ZengHuabei Zhang
Jun 27, 2014·Journal of Labelled Compounds & Radiopharmaceuticals·Akanksha JindalAshutosh Dash

❮ Previous
Next ❯

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.