We have compared multiple assays for the P-glycoprotein (Pgp/MDR1) phenotype in fresh and thawed adult acute leukemia to validate and quantitate measures for the expression and function of Pgp. The results are related to the Pgp-expressing KB8 and KB8-5 call lines. The most sensitive assay was the measurement of modulation of the rhodamine 123 (R123) fluorescence by 2 micromol/L PSC833, followe...

About one-third of the epilepsy patients are resistant to treatment with antiepileptic drugs (AEDs). This refractoriness is not fully understood but is thought to be attributed to overexpression of multidrug transporters at the blood-brain barrier (BBB), particularly Pglycoprotein (Pgp). In certain cases pharmacoresistance can be overcome by add-on therapy, raising the question of whether the c...

Milk thistle (Silybum marianum) is a native plant of Mediterranean Sea areas. Silymarin, an extract from its seeds, is used in various liver diseases for its hepatoprotective effects. It contains silymarin flavonoids (SF) such as silybin, silydianin and silychristin. Cyclosporin A (CsA) is widely used as an immunosuppressant in organ transplantations. Its other applications in many autoimmune d...

In earlier studies insects were proposed as suitable models for vertebrate blood-brain barrier (BBB) permeability prediction and useful in early drug discovery. Here we provide transcriptome and functional data demonstrating the presence of a P-glycoprotein (Pgp) efflux transporter in the brain barrier of the desert locust (Schistocerca gregaria). In an in vivo study on the locust, we found an ...

One potential physiological target for new antischistosomals is the parasite's system for excretion of wastes and xenobiotics. P-glycoprotein (Pgp), a member of the ATP-binding-cassette superfamily of proteins, is an ATP-dependent efflux pump involved in transport of toxins and xenobiotics from cells. In vertebrates, increased expression of Pgp is associated with multidrug resistance in tumor c...

BACKGROUND Pelvic girdle pain (PGP) is a multifactorial condition, which can be mentally and physically compromising both during and after pregnancy. However, long-term pregnancy-related PGP has been poorly investigated. This longitudinal follow-up study uniquely aimed to describe prevalence and predictors of PGP and its consequences on women's health and function up to 11 years after pregnancy...

BACKGROUND Structural and biochemical studies of mammalian membrane proteins remain hampered by inefficient production of pure protein. We explored codon optimization based on highly expressed Pichia pastoris genes to enhance co-translational folding and production of P-glycoprotein (Pgp), an ATP-dependent drug efflux pump involved in multidrug resistance of cancers. METHODOLOGY/PRINCIPAL FIN...

MDR1 P-glycoprotein (Pgp), the product of the MDR1 gene involved in multidrug resistance in cancer cells, is also expressed in normal tissues. In the human kidney, it is localized in the mesangium, the proximal tubule, the thick ascending limb of Henle's loop, and the collecting duct. Pgp actively transports lipophilic xenobiotics, peptides, steroids, and lipids, and perhaps endogenous substrat...

Previous studies reported that, in the absence of drug exposure, multidrug resistance, including resistance to Adriamycin (ADR), could develop in primary rat hepatocyte cultures (B. Carr, Proc. Am. Assoc. Cancer Res., 29:1158, 1988). However, the hepatocytes in that report were cultured on plastic without the benefit of an extracellular matrix (ECM). Because the ECM regulates hepatic gene expre...