A 192-member library of N,N'-disubstituted urea inhibitors was synthesized by a solid-phase method. The ureas were tested for their inhibitory activities against recombinant human soluble epoxide hydrolase. Simple carbocyclic or para/meta-substituted phenyl groups showed inhibition potencies that were equal to or greater than adamantane-based sEH inhibitors, while the presence of bulky or ioniz...

Electrostatic interactions are of vital importance in diverse aspects of protein structure and function [1-5], including the catalytic activity [6,7], ligand binding [8], complex formation [9], proton transport [10,11], as well as their stability of folded proteins [12,13]. These interactions involve full charges on the side chains of ionizable amino acids that arise from the association and di...

A multiwavelength spectrophotometric approach has been developed to determine acid dissociation constants (pKa values) of sparingly soluble drug compounds. UV absorption spectra of the drug solution are acquired using a versatile device based on a fiber optics dip probe, a light source and a photodiode array (PDA) detector while the PH and the ionic strength of the chemical system is manipulate...

PROTEIN IONIZABLE GROUPS: pK VALUES AND THEIR CONTRIBUTION TO PROTEIN STABILITY AND SOLUBILITY C. Nick Pace, Gerald R. Grimsley, and J. Martin Scholtz From the Department of Molecular and Cellular Medicine, Texas A&M Health Science Center, College Station, TX 77843 Running head: Protein pK values Address correspondence to: C. Nick Pace, Department of Molecular and Cellular Medicine, 440 Reynold...

Ionization mechanisms in the low-temperature thermal plasma, which contains alkali metal atoms as ionizable component and nanosized dust grains, are studied. In such a electrons captured by because work function of grains depends on their sizes, electron adsorption rate is more than thermionic emission for grains. Accordingly, an increase grain number leads to decrease volume ionization recombi...

Lipid nanoparticles (LNPs) containing short-interfering RNA (LNP-siRNA systems) are a promising approach for silencing disease-causing genes in hepatocytes following intravenous administration. LNP-siRNA systems generated by rapid mixing of lipids ethanol with siRNA aqueous buffer (pH 4.0) where the ionizable lipid is positively charged, followed dialysis to remove and raise pH 7.4. Ionizable c...