Studies in Drug Albumin Binding Using Hsa and Rsa Affinity Methods

High-Throughput Melanin-Binding Affinity and In Silico Methods to Aid in the Prediction of Drug Exposure in Ocular Tissue

“…Three standards were selected from the literature (low binder: imipramine, high binder: fluphenazine, intermediate binder: quinine), and prior in‐house experiments (low binder: carbamazepine, intermediate binder: amitriptyline) to cover a range of melanin‐binding affinities from log K Mel values 0.51–1.12. It has been previously observed that gradient elution is often necessary to elute compounds from protein‐bound columns within a reasonable timeframe and we have observed this in our own research with human serum albumin affinity . We used this gradient method approach detailed below to analyze the set of five standards with known melanin binding.…”

“…It has been previously observed that gradient elution is often necessary to elute compounds from protein-bound columns within a reasonable timeframe 25 and we have observed this in our own research with human serum albumin affinity. 26 We used this gradient method approach detailed below to analyze the set of five standards with known melanin binding. A linear gradient was performed from 0% to 30% B from 0 to 4.5 min.…”

In vitro membrane binding and protein binding (IAM MB/PB technology) to estimate in vivo distribution: applications in early drug discovery

“…However, they have their limitations and are also very time-consuming. Biomimetic stationary phases have been validated by comparing the retention times obtained on the commercially available ChiralPak-HSA [37][38][39] and ChiralPak-AGP [40][41] stationary phases result in binding values that are proportional to the albumin and AGP binding of compounds obtained by equilibrium dialysis. When using biomimetic stationary phases the retention time of the compounds is directly proportional to the dynamic equilibrium constant between the mobile phase (buffer at physiological pH) and the actual body component (membrane and proteins) in the stationary phase.…”

Methoxy-flavones identified from Ageratum conyzoides induce capase -3 and -7 activations in Jurkat cells

“…These results predict lower non-specific tissue targeting and therefore hopefully higher specific binding to target tissues, due to their ability to permeate the phospholipid bilayer and lower propensity to distribute into all organ tissues (Jiang and Reilly, 2012;Reilly et al, 2011).…”