Histone acetylation status, an epigenetic determinant of gene transcription, is controlled by histone acetyltransferases (HATs) and histone deacetylases (HDACs). The potent HDAC inhibitor FK228 [(E)-(1S,4S,10S,21R)-7-[(Z)-ethylidene]-4,21-diisopropyl-2-oxa-12,13-dithia-5,8,20,23-tetraazabicyclo[8,7,6]-tricos-16-ene-3,6,9,22-pentanone] is a substrate for multidrug resistance protein (MDR1) and m...

BACKGROUND Cannabis is the most widely used illicit drug in the world that is often used by cancer patients in combination with conventional anticancer drugs. Multidrug resistance (MDR) is a major obstacle in the treatment of cancer. An extensively characterized mechanism of MDR involves overexpression of P-glycoprotein (P-gp), which reduces the cellular accumulation of cytotoxic drugs in tumor...

P-glycoprotein (P-gp), the product of MDR1 gene, is a protein which mediates transmembrane transport of a great number of xenobiotics including cyclosporin A used as an immunosuppressive drug in patients with allogenic kidney grafts. The P-gp activity and expression is dependent on the MDR1 gene polymorphism in position C3435T of exon 26. In this study, C3435T polymorphism was analyzed in 116 p...

Multidrug resistance (MDR) caused by overexpression of p-glycoprotein is a major obstacle in chemotherapy of malignant cancer, which usually is characterized by constitutive activation of signal transducer and activator of transcription 3 (STAT3), but their relation between MDR and STAT3 remains unclear. Here, we showed that STAT3 was overexpressed and highly activated in adriamycin-resistant K...

Rifampicin, one of the primary tuberculosis drugs, is a PGP substrate that is encoded by MDR 1 gene. The objectives of the research was to study the impacts of MDR1 gene polymorphism toward plasma rifampicin levels in Javanese patients with pulmonary tuberculosis. The subjects of this research are Javanese tuberculosis patients treated by fixed dosage combination (FDC) of anti-tuberculosis drug...

Several distinct strategies have been used to modulate the expression of cancer-associated genes, including antisense oligonucleotides, small interfering RNAs (siRNAs), and artificial transcriptional factors. One major cause for chemotherapeutic treatment failure in cancer is the overexpression of P-glycoprotein, the product of the multidrug resistance gene MDR1. In this study, we tested the ab...

P-glycoprotein (P-gp), the protein product of MDR1 gene, is an important factor regulating the bioavailability of many therapeutics. Recently, the C3435T polymorphism of MDR1 was correlated to altered expression and function of P-gp in normal tissues. In this study, polymerase chain reaction-restriction fragment length polymorphism (PCR-RFLP) assay was applied to assess C3435T MDR1 polymorphism...

Upregulation of the MDR1 (multidrug resistance 1) gene is involved in the development of resistance to antifungal agents in clinical isolates of the pathogen Candida albicans. To better understand the molecular mechanisms underlying the phenomenon, the cis-acting regulatory elements present in the MDR1 promoter were characterized using a beta-galactosidase reporter system. In an azole-susceptib...

Background: Genetic variation that modifies the gut barrier function or the inflammatory response may modify the risk of colorectal cancer (CRC). The intestinal xenobiotic transporters, Multidrug Resistance 1 (MDR1/ABCB1) and Breast Cancer Resistance Protein (BCRP/ABCG2) contribute to the intestinal homeostasis by exporting a broad spectrum of substrates including potential carcinogens from the...

Background: Genetic variation that modifies the gut barrier function or the inflammatory response may modify the risk of colorectal cancer (CRC). The intestinal xenobiotic transporters, Multidrug Resistance 1 (MDR1/ABCB1) and Breast Cancer Resistance Protein (BCRP/ABCG2) contribute to the intestinal homeostasis by exporting a broad spectrum of substrates including potential carcinogens from the...