Tariquidar-related triazoles as potent, selective and stable inhibitors of ABCG2 (BCRP).

Tariquidar derivatives have been described as potent and selective ABCG2 inhibitors. However, their susceptibility to hydrolysis limits their applicability. The current study comprises the synthesis and characterization of novel tariquidar-related inhibitors, obtained by bioisosteric replacement of the labile moieties in our previous tariquidar analog UR-ME22-1 (9).

ABCG2/BCRP: Specific and Nonspecific Modulators.

Multidrug resistance (MDR) in cancer cells is the development of resistance to a variety of structurally and functionally nonrelated anticancer drugs. This phenomenon has become a major obstacle to cancer chemotherapy seriously affecting the clinical outcome. MDR is associated with increased drug efflux from cells mediated by an energy-dependent mechanism involving the ATP-binding cassette (ABC) transporters, mainly P-glycoprotein (ABCB1), the MDR-associated protein-1 (ABCC1), and the breast cancer resistance protein (ABCG2).

Suramin induces and enhances apoptosis in a model of hyperoxia-induced oligodendrocyte injury.

Recent evidence suggests oxygen as a powerful trigger for cell death in the immature white matter, leading to periventricular leukomalacia (PVL) as a cause of adverse neurological outcome in survivors of preterm birth. This oligodendrocyte (OL) death is associated with oxidative stress, upregulation of apoptotic signaling factors (i.e.

Polycythemia and increased erythropoietin in a patient with chronic kidney disease.

Background: A 16-year-old white male with a history of obstructive uropathy presented to a pediatric outpatient clinic with a first syncope. At presentation, he had a hemoglobin level of 220 g/l, a serum erythropoietin level of 27.4 U/l and a serum creatinine level of 200.

Growth hormone determination in children using an immunofunctional assay in comparison to conventional assays.

Conventional assays for determination of growth hormone (GH) in serum measure immunoreactive molecules of a blood sample. The immunofunctional assay (IFA), on the other hand, is able to determine biologically active molecules. In our study, we evaluated GH determination in children with IFA to compare these data with clinical reliable data of conventional assay systems, since there is only insufficient data concerning the clinical use of IFA in children.