From previous fits of drug transport kinetics across confluent Madin-Darby canine kidney II cell line overexpressing human multidrug resistance 1 cell monolayers, we found that a drug's binding constant to P-glycoprotein (P-gp) was significantly smaller than its IC(50) when that drug was used as an inhibitor against another P-gp substrate. We tested several IC(50) candidate functions, including...

A 170,000-Da glycoprotein (P170 multidrug transporter) becomes specifically labeled in multidrug-resistant human KB carcinoma cells by the photolabile lipophilic membrane probe 5-[125I]iodonaphthalene-1-azide ([125I]INA) when photoactivation of the probe is triggered by energy transfer from intracellular doxorubicin or rhodamine 123. In contrast, in drug-sensitive cells, drug-induced specific l...

PURPOSE We sought to better characterize the intravitreal profile of different triamcinolone formulations. METHODS The study was performed in vitro and in vivo. Kenalog-40, Triesence, and Transton were characterized for ocular pharmacokinetics, particle size, crystallinity, and dissolving kinetics in vitreous following an intravitreal injection into 12 rabbit eyes. The relationship of free dr...

In vitro evaluation of P-glycoprotein (P-gp) inhibitory potential is now a regulatory issue during drug development, in order to predict clinical inhibition of P-gp and subsequent drug-drug interactions. Assays for this purpose, commonly based on P-gp-expressing cell lines and digoxin as a reference P-gp substrate probe, unfortunately exhibit high variability, raising thus the question of devel...

Many therapeutic leads fail to advance clinically because of bioavailability, selectivity, and formulation problems. Molecular transporters can be used to address these problems. Molecular transporter conjugates of otherwise poorly soluble or poorly bioavailable drugs or probes exhibit excellent solubility in water and biological fluids and at the same time an enhanced ability to enter tissues ...

Differential scanning fluorimetry (DSF) is used to assess protein stability, transition states, or the Kd values of various ligands, drug molecules, and antibodies. All fluorescent probes published to date either are incompatible with hydrophobic proteins/ligands, precluding analyses of transmembrane or membrane-associated proteins, or have excitation and detection wavelengths outside the range...

Introduction: Among the first line drugs used for treatment of Drug Sensitive Tuberculosis, Rifampicin plays a crucial role. Hence it is important to know resistance using molecular technologies like CBNAAT and probe Assay. However, diagnostic dilemma occurs when there discordance in result rifampicin at periphery higher laboratories Intermediate Reference Laboratory (IRL). Aims objectives: To ...

in this research, a fast colorimetric method for the detection of 4-phenylthiosemicarbazid (4-ptsc) in environmental samples, is reported for the first time. semicarbazide compounds have been used as pesticides or fungicides in agriculture and for chemical synthesis in industrial processes. with this method, one or the total amount of semicarbazide in real samples can be detected within 6-7 min...

Introduction. Mycobacterium tuberculosis is the causative agent of tuberculosis. Drug susceptibility testing performed by phenotypic and molecular tests. Commonly used for drug automated BACTEC system in a liquid culture medium. line probe tests was introduced almost 15 years ago. Recently whole genome sequencing (WGS) analysis M. strains demonstrated that genotyping drug-resistance could be ac...

INTRODUCTION Diabetes affects more than 9% of the adult population worldwide. Patients with type 2 diabetes mellitus (T2DM) show variable responses to some drugs which may be due, in part, to variability in the functional activity of drug-metabolising enzymes including cytochromes P450 (CYP450s). CYP450 is a superfamily of enzymes responsible for xenobiotic metabolism. Knowledge must be gained ...