The cytochrome P450 (P450) enzymes are the predominant enzyme system involved in human drug metabolism. Alterations in the expression and/or activity of these enzymes result in changes in pharmacokinetics (and consequently the pharmacodynamics) of drugs that are metabolized by this set of enzymes. Apart from changes in activity as a result of drug-drug interactions (by P450 induction or inhibit...

In drug discovery, there is a clear and urgent need for detection of cell-membrane ion-channel operation with wide-field capability. Existing techniques are generally invasive or require specialized nanostructures. We show that quantum nanotechnology could provide a solution. The nitrogen-vacancy (NV) center in nanodiamond is of great interest as a single-atom quantum probe for nanoscale proces...

Because modulation of P-glycoprotein (Pgp) through inhibition or induction can lead to drug-drug interactions by altering intestinal, central nervous system, renal, or biliary efflux, it is anticipated that information regarding the potential interaction of drug candidates with Pgp will be a future regulatory expectation. Therefore, to be able to utilize in vitro Pgp inhibition findings to guid...

The pregnane X receptor (PXR) regulates the metabolism and excretion of xenobiotics and endobiotics by regulating the expression of drug-metabolizing enzymes and transporters. The unique structure of PXR allows it to bind many drugs and drug leads, possibly causing undesired drug-drug interactions. Therefore, it is crucial to evaluate whether chemicals or drugs bind to PXR. Fluorescence-based a...

The rapid accurate detection of drug resistance mutations in Mycobacterium tuberculosis is essential for optimizing the treatment of tuberculosis and limiting the emergence and spread of drug-resistant strains. The TB Resistance line probe assay from Autoimmun Diagnostika GmbH (AID) (Strassburg, Germany) was designed to detect the most prevalent mutations that confer resistance to isoniazid, ri...

Small-molecule chemical probes or tools have become progressively more important in recent years as valuable reagents to investigate fundamental biological mechanisms and processes causing disease, including cancer. Chemical probes have also achieved greater prominence alongside complementary biological reagents for target validation in drug discovery. However, there is evidence of widespread c...

Electron transport characteristics are investigated through some molecular chains attached with two non-superconducting electrodes by the use of Green's function method. Here we do parametric calculations based on the tight-binding formulation to characterize the electron transport through such bridge systems. The transport properties are significantly influenced by (a) the length of the molecu...

Abstract Background In humans, the drug metabolizing enzyme CYP2D6 is highly polymorphic resulting in substantial differences metabolism of drugs including anti-arrhythmics, neuroleptics, and opioids. The objective this study was to phenotype a population 100 horses from five different breeds assess metabolic activity equine homolog using codeine as probe drug. Administration common method used...

This paper reviews the use of texture analysis in studying the performance of hydrophilic matrices of highly soluble drugs and different types of excipients (i.e. water-soluble, water-insoluble and swellable, and water insoluble and non-swellable). Tablets were prepared by direct compression, and their swelling and erosion in presence of these different excipients were assessed with the help of...