Currently several studies are being carried out on various properties of mesenchymal stem cells (MSCs)however there are a few investigations about drug metabolizing properties of these cells. The aim of thisstudy was to measure the key factors involved in drug metabolism in human bone marrow MSCs. For thispurpose, cellular glutathione (GSH), glutathione Stransferase (GSTs) and...

Medroxyprogesterone acetate (MPA: Depo-Provera) is a long-acting synthetic progestin that has been used as a contraceptive for more than 11 million women-years in 80 nations [1]. The U.S. Food and Drug Administration has denied approval of MPA as a contraceptive because of concern about its safety, especially teratogenicity and carcinogenicity [2.3]. In addition to its contraceptive action, MPA...

The past 50 years have witnessed a monumental advance in our understanding of pharmacodynamics (what drugs do to the body) and pharmacokinetics (what the body does to drugs). In the realm of pharmacokinetics, dozens of enzymes responsible for drug biotransformation and transporters responsible for the absorption, distribution and excretion of drugs have been identified. Drug biotransformation (...

Undesirable absorption, distribution, metabolism, excretion (ADME) properties are the cause of many drug development failures and this has led to the need to identify such problems earlier in the development process. This review highlights computational (in silico) approaches that have been used to identify the characteristics of ligands influencing molecular recognition and/or metabolism by th...

Along with minimal toxicity, good drug metabolism and pharmacokinetic (DMPK) properties are essential for the clinical success of a drug candidate. A major cause of failure of orally administered drugs during their development is the discovery that in humans they have low intestinal absorption and/or high clearance causing low and variable bioavailability. In addition, drug interactions and the...

Human carboxylesterase 1 (hCE1) is a serine esterase involved in both drug metabolism and activation, as well as other biological processes. hCE1 catalyses the hydrolysis of heroin and cocaine, and the transesterification of cocaine in the presence of ethanol to the toxic metabolite cocaethylene. We have determined the crystal structures of hCE1 in complex with either the cocaine analogue homat...

In the last years, considerable progress has been made concerning efficient drug design by in silico adapting drug molecule candidates to known binding sites that had been spatially elucidated by methods of structural biology. This allows identification of suitable ligands with regard to both geometry of the binding pocket and affinity as deduced from knowledge of docking points and energy calc...

In 25 years, drug metabolism research went from using subcellular particles of undefined content to an understanding of metabolism at the molecular level. The discoveries of cytochrome P450, enzyme induction, reactive intermediates, and genetic polymorphisms were milestones in the field. New publications from the American Society for Pharmacology and Experimental Therapeutics chronicled the dis...