A 99mTc-Labeled Ligand of Carbonic Anhydrase IX Selectively Targets Renal Cell Carcinoma In Vivo.

Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine
Nikolaus KrallDario Neri

Abstract

Small organic ligands, selective for tumor-associated antigens, are increasingly being considered as alternatives to monoclonal antibodies for the targeted delivery of diagnostic and therapeutic payloads such as radionuclides and drugs into neoplastic masses. We have previously described a novel acetazolamide derivative, a carbonic anhydrase ligand with high affinity for the tumor-associated isoform IX (CAIX), which can transport highly potent cytotoxic drugs into CAIX-expressing solid tumors. The aim of the present study was to quantitatively investigate the biodistribution properties of said ligand and understand whether acetazolamide conjugates merit further development as drug carriers and radioimaging agents. The conjugate described in this study, consisting of a derivative of acetazolamide, a spacer, and a peptidic (99m)Tc chelator, was labeled using sodium pertechnetate under reducing conditions and injected intravenously into CAIX-expressing SKRC-52 xenograft-bearing mice. Animals were sacrificed, and organ uptake as percentage injected activity of radiolabeled ligand per gram of tissues (%IA/g) was evaluated between 10 min and 24 h. Additionally, postmortem imaging by SPECT was performed. The acetazolamide conjugate de...Continue Reading

References

Dec 1, 1989·The Journal of Experimental Medicine·M BrüggemannM S Neuberger
May 9, 1998·The Journal of Histochemistry and Cytochemistry : Official Journal of the Histochemistry Society·J SaarnioW S Sly
Mar 10, 2001·The American Journal of Pathology·S IvanovE J Stanbridge
Sep 28, 2002·International Journal of Cancer. Journal International Du Cancer·Laura BorsiLuciano Zardi
Aug 28, 2004·Organic Letters·Timothy R ChanValery V Fokin
Jan 11, 2007·Cancer Research·Mark S DennisRalph Schwall
Apr 9, 2008·Physiological Reviews·Börje HaraldssonWilliam M Deen
May 17, 2008·Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine·Ronald E FisherRobert J Amato
Jul 21, 2009·Radiotherapy and Oncology : Journal of the European Society for Therapeutic Radiology and Oncology·Ludwig DuboisPhilippe Lambin
Dec 6, 2012·Journal of Clinical Oncology : Official Journal of the American Society of Clinical Oncology·Chaitanya R DivgiPaul Russo
Jan 11, 2013·Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine·John A BarrettJohn W Babich
May 24, 2013·Cancer Biotherapy & Radiopharmaceuticals·Alexander B StillebroerOtto C Boerman
Mar 1, 2014·European Journal of Nuclear Medicine and Molecular Imaging·Christian M ZechmannUwe Haberkorn
Mar 29, 2014·Angewandte Chemie·Ravi V J ChariWayne C Widdison
Apr 4, 2014·Molecular Imaging and Biology : MIB : the Official Publication of the Academy of Molecular Imaging·Mohan DossJian Q Yu
Feb 24, 2015·Nature Reviews. Drug Discovery·Madduri SrinivasaraoPhilip S Low
Feb 25, 2015·Molecular Imaging and Biology : MIB : the Official Publication of the Academy of Molecular Imaging·Sarah G J A PeetersPhilippe Lambin
Apr 1, 2014·Annals of Oncology : Official Journal of the European Society for Medical Oncology·R T MorrisW A Harb

❮ Previous
Next ❯

Citations

Apr 8, 2017·Journal of Enzyme Inhibition and Medicinal Chemistry·Zhengxing ZhangKuo-Shyan Lin
Nov 15, 2018·Expert Opinion on Investigational Drugs·Claudiu T Supuran
Jun 8, 2019·Expert Opinion on Therapeutic Patents·Sabina ZamanovaMarc A Ilies
Jan 27, 2018·Oncotarget·Allison S CohenDavid L Morse
Jul 30, 2020·Organic & Biomolecular Chemistry·Kuo-Ting ChenYann Seimbille
Aug 30, 2019·Cancer Cell International·Yongchang LaiWenqi Wu
Dec 13, 2019·Scientific Reports·Fokko J HuizingSandra Heskamp
Jan 11, 2018·Current Opinion in Urology·Alexa R MeyerMichael A Gorin
Dec 24, 2018·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Kuo-Ting ChenYann Seimbille
Oct 18, 2020·Metabolites·Andrea AngeliClaudiu T Supuran
Sep 10, 2016·Molecular Cancer Therapeutics·Samuele CazzamalliDario Neri
Apr 25, 2018·Clinical Cancer Research : an Official Journal of the American Association for Cancer Research·Samuele CazzamalliDario Neri
Dec 29, 2020·Journal of Experimental Pharmacology·Claudiu T Supuran
Jul 19, 2020·Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine·Oana C KultererAlexander R Haug
Sep 5, 2017·Journal of Controlled Release : Official Journal of the Controlled Release Society·Alberto Dal CorsoDario Neri
Nov 29, 2016·Journal of Controlled Release : Official Journal of the Controlled Release Society·Samuele CazzamalliDario Neri
Mar 21, 2019·Molecular Pharmaceutics·Shimpei IikuniMasahiro Ono
Aug 28, 2021·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Siao-Syun GuanShing-Hwa Liu
Jan 22, 2022·Journal of Enzyme Inhibition and Medicinal Chemistry·Chiara TestaPaolo Rovero

❮ 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.

© 2022 Meta ULC. All rights reserved