Stabilization of neurotensin analogues: effect on peptide catabolism, biodistribution and tumor binding

Nuclear Medicine and Biology
Matthias BruehlmeierPeter Bläuenstein

Abstract

Neurotensin (NT) receptors in pancreatic and other neuroendocrine tumors are promising targets for imaging and therapeutic purposes. Here, we report on the effect of distinct changes in the peptide chain on catabolism in vitro for five radiolabeled [99mTc] neurotensin analogues having high affinity for neurotensin receptors. Substitution of NT(1-7) by (NalphaHis)Ac--the Tc-binding moiety--combined with a reduced bond 8-9 (CH2NH), N-methylation of peptide bonds or replacement of Ile(12) by tertiary leucin (Tle) led to peptide stabilization of various degrees. Biodistribution studies in nude mice bearing HT29 xenografts showed higher tumor uptake with more stable peptides, yielding high tumor to blood ratios of up to 70.

References

Jan 1, 1992·Annals of the New York Academy of Sciences·P KitabgiJ N Bidard
Jun 1, 1993·The American Review of Respiratory Disease·T DragovićS F Rabito
Sep 28, 1998·Pharmacology & Therapeutics·E Hermans, J M Maloteaux

❮ Previous
Next ❯

Citations

Jun 28, 2007·European Journal of Nuclear Medicine and Molecular Imaging·Theodosia MainaBerthold A Nock
Aug 12, 2008·European Journal of Nuclear Medicine and Molecular Imaging·Elisa García-GarayoaP August Schubiger
Sep 6, 2005·Amino Acids·R Bergmann, J Pietzsch
Mar 19, 2004·Nuclear Medicine and Biology·B KuhnastW A Weber
Jan 24, 2009·The Journal of Biological Chemistry·Karen S HarrisMichael Foley
Jul 27, 2007·Cancer Biotherapy & Radiopharmaceuticals·Paul J J M JanssenMarion de Jong
Apr 21, 2004·Nuclear Medicine Communications·Tim A D SmithPaul H Walton
Sep 9, 2015·Bioconjugate Chemistry·Alba MascarinThomas L Mindt
May 25, 2006·Nuclear Medicine and Biology·Elisa García-GarayoaP August Schubiger
May 25, 2006·Nuclear Medicine and Biology·Kaijun ZhangMohan R Aruva
Oct 22, 2016·Bioconjugate Chemistry·Yinnong JiaJered Garrison
Jan 12, 2007·Molecular BioSystems·Stephen J Mather
Feb 26, 2016·Natural Product Reports·C L CharronL G Luyt
Nov 9, 2017·Journal of Labelled Compounds & Radiopharmaceuticals·Simone Maschauer, Olaf Prante
Aug 18, 2017·Chemical Biology & Drug Design·Iman EmrarianSaeid Abediankenari
Oct 26, 2012·ChemMedChem·Cornelia HeldPeter Gmeiner
May 4, 2006·Journal of Peptide Science : an Official Publication of the European Peptide Society·Veronique MaesDirk Tourwé
Feb 26, 2011·Dalton Transactions : an International Journal of Inorganic Chemistry·João D G CorreiaIsabel Santos
Aug 13, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Lisa-Maria RečnikThomas L Mindt
Sep 16, 2003·The Journal of Biological Chemistry·Luisa BracciPaolo Neri
Jul 21, 2009·Bioconjugate Chemistry·Faisal AlshoukrAnne Gruaz-Guyon
Jun 1, 2006·Bioorganic & Medicinal Chemistry·Christina HultschFrank Wuest
Mar 3, 2006·Journal of Medicinal Chemistry·Veronique MaesDirk Tourwé
May 11, 2010·Bioorganic & Medicinal Chemistry Letters·Susan RichterFrank Wuest
Apr 19, 2011·Journal of Inorganic Biochemistry·Anika RöhrichHolger Stephan

❮ 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.