Probing the serum albumin binding site of fenamates and photochemical protein labeling with a fluorescent dye

Abstract

Human serum albumin (HSA) can bind with numerous drugs, leading to significant influence to drug pharmacokinetics as well as undesirable drug-drug interaction due to the competitive binding. Probing HSA drug...

Probe and dye design through copper-mediated reactions of N-arylhydroxylamines

“…The lowest limit of detection (LOD) is estimated by a well-established method. 14 Briefly,LOD = 3 σ / b where σ is the standard deviation obtained from three individual measurements of the fluorescence intensity in the absence of Cu 2+ , and b is the slope from the linear fitting of the regression line.…”

Improved Analytical Performance of an Amphiphilic Probe upon Protein Encapsulation: Spectroscopic Investigation along with Computational Rationalization

“…For instance, serum albumin affects the Zn 2+ uptake by epithelial cells and modulates its ionic transport into erythrocytes. 10,11 In vitro evidence even points to the transport of the Zn-albumin complex into endothelium cells. Besides sequestering Zn 2+ , serum albumins have affinity for various ligands, including hydrophobic/amphipathic molecules.…”

“…In light of the vital role played by Zn 2+ ions, a variety of Zn 2+ sensors have been developed, primarily confined to sensing in organic solvents or aqueous medium. , Probing distributions of the Zn 2+ ion (or any other metal ion) at lipid membrane/water interfaces or in the protein-bound form have been rarely explored. , However, in mammals, at least two-thirds of the Zn 2+ ion present in the blood plasma of the organism is bound to serum albumins. , Serum albumins have been implicated in various facets of zinc biology due to their strong affinity for the zinc ion. For instance, serum albumin affects the Zn 2+ uptake by epithelial cells and modulates its ionic transport into erythrocytes. , In vitro evidence even points to the transport of the Zn-albumin complex into endothelium cells. Besides sequestering Zn 2+ , serum albumins have affinity for various ligands, including hydrophobic/amphipathic molecules. − It is the affinity toward multiple types of ligands that is crucial to the role played by albumins in transport.…”

Using Human Serum Albumin Binding Affinities as a Proactive Strategy to Affect the Pharmacodynamics and Pharmacokinetics of Preclinical Drug Candidates

“…With HSA−SAR information 23 for any drug candidate lead series, adjustments to PK/PD parameters 6 during the drug design phase can positively affect clinical trial protocols. Other characterizations of HSA interactions have been reported, including pyrogallol, 24 juglone, 25 fenamates, 26 caffeic acid, 27 among others. 28 HSA's fluorescent properties are due to tryptophan 214, a nonpolar amino acid, present in subdomain IIA (λ ex = 280 nm and λ em = 334 nm).…”

“…With HSA–SAR information for any drug candidate lead series, adjustments to PK/PD parameters during the drug design phase can positively affect clinical trial protocols. Other characterizations of HSA interactions have been reported, including pyrogallol, juglone, fenamates, caffeic acid, among others …”