Marialessandra Contino

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2-Aryloxazole and 2-arylthiazole derivatives were evaluated for their inhibitory activity toward P-glycoprotein (P-gp) as well as their selectivity toward other ABC transporters involved in multi-drug resistance such as BCRP and MRP1. These derivatives have 6,7-dimethoxytetrahydroisoquinoline or cyclohexylpiperazine moieties, which are the same basic nuclei(More)
Prolonged bicalutamide treatment induced pathology regression although relapses with a more aggressive form of prostate cancer have been observed. This failure could be due to androgen receptor mutation. In the present work we hypothesized an alternative mechanism responsible for bicalutamide failure involving activity of ATP-binding cassette (ABC) pumps(More)
Multidrug resistance (MDR) is a complex phenomenon principally due to the overexpression of some transmembrane proteins belonging to the ATP binding cassette (ABC) transporter family. Among these transporters, P-glycoprotein (P-gp) is mostly involved in MDR and its overexpression is the major cause of cancer therapy failure. The classical approach used to(More)
CSCs are responsible for the high rate of recurrence and chemoresistance of different types of cancer. The current antineoplastic agents able to inhibit bulk replicating cancer cells and radiation treatment are not efficacious toward CSCs since this subpopulation has several intrinsic mechanisms of resistance. Among these mechanisms, the expression of(More)
The goal of the present paper is to establish and validate the link between cancer diagnosis and therapy by microRNAs detection. The induction in vitro of some specific microRNAs after treatment with MDR ligands has been outlined. Starting from the results obtained by in vitro induction of MDCK and MDCK-MDR1 cells treated by a MDR1 ligand, a new scenario in(More)
AD is the most common form of dementia among the aging population. The neuropathological alterations of AD are represented by the neu-rofibrillary tangles and extracellular amyloid plaques formation. These two hallmarks are routinely used as biomarkers for AD diagnosis and can allow the identification of the pathology in a late phase. The urgent need to(More)
An in vitro model was developed to understand if celecoxib could synergize with Mitomycin C (MMC), commonly used for the prevention of non-muscle invasive bladder cancer recurrence, and eventually elucidate if the mechanism of interaction involves multi drug resistance (MDR) transporters. UMUC-3, a non COX-2 expressing bladder cancer cell line, and(More)
BPH could be considered the most common benign tumor for men between 60 and 75 years of age. PSA is an unsatisfactory biomarker to define BPH progression to cancer. Recently, sigma-2 receptors have been recognized in several prostate cancer cell lines such as PC-3, DU-145 and LNCaP. It is reported that, in some cases, BPH could progress to malignancy and(More)
Inhibition of drug efflux pumps such as P-glycoprotein (P-gp) is an approach toward combating multidrug resistance, which is a significant hurdle in current cancer treatments. To address this, N-substituted aryloxymethyl pyrrolidines were designed and synthesized in their homochiral forms in order to investigate the stereochemical requirements for the(More)
Mexiletine is a sodium channel blocker, primarily used in the treatment of ventricular arrhythmias. Moreover, recent studies have demonstrated its therapeutic value to treat myotonic syndromes and to relieve neuropathic pain. The present study aims at investigating the direct blockade of hERG potassium channel by mexiletine and its metabolite(More)