title: Clinical pharmacokinetic and metabolism of PET radiotracers for imaging P-glycoprotein in chemoresistant tumor of colorectal cancer.
abstract: The pharmacological treatment of colorectal tumour leads to MultiDrug Resistance due to overexpression of several ABC transporters such as P-glycoprotein and some Multidrug associated Resistance Proteins (MRPs) that are able to efflux the chemotherapeutic agent out of the cell. A strategy to reverse MDR is the co-administration of antineoplastic agent with a P-glycoprotein inhibitor. These inhibitors are an useful tool for investigating, by PET, the expression and the activity of P-gp and MRPs that are overexpressed in chemoresistant colorectal tumor cells. In this review will be focused the aspect on P-gp and MRPs ligands employed as PET radiotracers considering their pharmacokinetic pharmacodynamic profile and their selectivity towards ABC transporters involved in chemoresistant cell of colorectal tumour.
authors.affiliation: Dipartimento Farmacochimico, Universita degli Studi di Bari, via Orabona 4, 70125, Bari, Italy.
authors.forename: Mariangela
authors.initials: M
authors.lastname: Cantore
authors.forename: Elena
authors.initials: E
authors.lastname: Capparelli
authors.forename: Francesco
authors.initials: F
authors.lastname: Berardi
authors.forename: Roberto
authors.initials: R
authors.lastname: Perrone
authors.forename: Nicola Antonio
authors.initials: NA
authors.lastname: Colabufo
mesh_terms: D018528:ATP-Binding Cassette Transporters / Q000378:metabolism*; D015179:Colorectal Neoplasms / Q000000981:diagnostic imaging*; D019008:Drug Resistance, Neoplasm; D006801:Humans; D008024:Ligands; D049268:Positron-Emission Tomography; D011849:Radioactive Tracers
chemical_list: D018528:ATP-Binding Cassette Transporters; D008024:Ligands; D011849:Radioactive Tracers