Four Decades of Cytochrome P450 2B Research: From Protein Adducts to Protein Structures and Beyond.

This article features selected findings from the senior author and colleagues dating back to 1978 and covering approximately three-fourths of the 60 years since the discovery of cytochrome P450. Considering the vast number of P450 enzymes in this amazing superfamily and their importance for so many fields of science and medicine, including drug design and development, drug therapy, environmental health, and biotechnology, a comprehensive review of even a single topic is daunting. To make a meaningful contribution to the 50th anniversary of , we trace the development of the research in a single P450 laboratory through the eyes of seven individuals with different backgrounds, perspectives, and subsequent career trajectories.

Studying tautomerism in an important pharmaceutical glibenclamide confined in the thin nanometric layers.

The uniform thin films with variable thicknesses (d = 49, 120, 220 nm) of active pharmaceutical ingredient (API) glibenclamide (GCM) was spin-coated and investigated using broadband dielectric, grazing incident FTIR spectroscopies, atomic force microscopy, and ellipsometry. Data analysis revealed that nanoconfined systems consist of a mixture of amide and imidic acid forms of this pharmaceutical, wherein the ratios of both tautomeric forms in the thin films were different with respect to the molten supercooled bulk system. Moreover, changes in the populations of glibenclamide tautomers, i.

Testing density scaling in nanopore-confinement for hydrogen-bonded liquid dipropylene glycol.

Recently, it has been demonstrated that the glassy dynamics of the molecular liquids and polymers confined at the nanoscale level might satisfy the density scaling law ( /) with the same value of the scaling exponent, , as that determined from the high-pressure studies of the bulk material. In this work, we have tested the validity of this interesting experimental finding for strongly hydrogen-bonded molecular liquid, dipropylene glycol (DPG), which is known to violate the / scaling rule in the supercooled liquid bulk state. The results of the independent dielectric relaxation studies carried out on increased pressure and in nanopores, have led to an important finding that when the density change induced by geometrical confinement is not very large, DPG can still obey the density scaling law with the same value of the scaling exponent as that found for the bulk sample.

An Effective Approach to Teaching Pharmacogenomics in the First Year of Pharmacy Curriculum.

To develop an effective method in teaching pharmacogenomics as a part of a new course, Biopharmaceutics and Pharmacogenomics. Teaching effectiveness was measured by quizzes, retrospective pre- and post-surveys, team activities, and journal reflections. Four team activities were included in the course: genomic disease, patient case, genetic counselor and a debate about personalized medicine.

Increased Phenacetin Oxidation upon the L382V Substitution in Cytochrome P450 1A2 is Associated with Altered Substrate Binding Orientation.

Leucine382 of cytochrome P450 1A2 (CYP1A2) plays an important role in binding and -dealkylation of phenacetin, with the L382V mutation increasing substrate oxidation (Huang and Szklarz, 2010, . 38:1039⁻1045). This was attributed to altered substrate binding orientation, but no direct experimental evidence had been available.