Imaging drug resistance with radiolabeled molecules

Current Pharmaceutical Design
Ganesan Vaidyanathan, Michael R Zalutsky

Abstract

A major obstacle to successful cancer chemotherapy is drug resistance. Multidrug resistance (MDR) is often seen with chemotherapeutic agents such as anthracycline derivatives, vinca alkaloids and taxanes. Multiple aspects of cellular biochemistry have been implicated in the MDR process. Cellular mechanisms of resistance are due to the presence of efflux pumps, P-glycoprotein (P-gp) and multiple resistance-associated protein (MRP), which belong to the ATP-binding cassette (ABC) family of transporters. Another form of drug resistance is involved in the chemotherapy of cancers with alkylating agents such as nitrosourea derivatives and nitrogen mustards. The cytotoxicity of these agents is primarily due to alkylation of the DNA guanine residues at their O6-position, which leads, via a cascade of events, to DNA strand breaks. The DNA repair protein, alkylguanine-DNA alkyl transferase (AGT) removes the alkyl groups from the lesions stoichiometrically to a cysteine in its active site. This process is irreversible and results in the degradation of the protein and its recovery is entirely from de novo synthesis. Noninvasive methodologies for monitoring the transport activity of these efflux pumps and determining tumor content of AGT cou...Continue Reading

Citations

Mar 17, 2009·Journal of Nuclear Cardiology : Official Publication of the American Society of Nuclear Cardiology·Young-Seung KimShuang Liu
Aug 5, 2008·Journal of Nuclear Cardiology : Official Publication of the American Society of Nuclear Cardiology·Young-Seung KimShuang Liu
Jun 24, 2011·Bioconjugate Chemistry·Yang Zhou, Shuang Liu
Jun 19, 2007·Biochimica Et Biophysica Acta·Jean-Pierre GilletJosé Remacle
Mar 14, 2007·Dalton Transactions : an International Journal of Inorganic Chemistry·Shuang Liu
Dec 17, 2010·World Journal of Hepatology·Young-Seung KimShuang Liu
Feb 8, 2019·Current Radiopharmaceuticals·Wei Fang, Shuang Liu

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