Influence of ionic strength on the binding of sodium aurothiosulphate to human serum albumin

Pedersen, Susanne Møller

doi:10.1016/0006-2952(85)90291-6

Cited by 8 publications

(2 citation statements)

References 13 publications

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“…The binding mechanism suggested in the present study agrees with that suggested for the binding of aurothiosulphate to human albumin. '9 20 Although aurothiomalate and aurothiosulphate are respectively organic and inorganic compounds, the similar values for the association contants of the two compounds also support the hypothesis that the same binding mechanism applies. Assuming n=4 identical values of K, are obtained, suggesting that it is the sulphydryl group (SH) of Cys(34) which is the high affinity binding site.…”

Section: Discussionmentioning

confidence: 68%

Binding of sodium aurothiomalate to human serum albumin in vitro at physiological conditions.

Pedersen¹

1986

Annals of the Rheumatic Diseases

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Section: Discussionmentioning

confidence: 68%

Binding of sodium aurothiomalate to human serum albumin in vitro at physiological conditions.

Pedersen¹

1986

Annals of the Rheumatic Diseases

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“…Herein, we proposed a competitive ABPP strategy (Figure B), including identification experiments and reactivity classification experiments for the target profiles in proteomes of four Au(I) complexes: Auranofin (AF), − Aurothioglucose (ATG), − Aurothiomalate (ATM), − and Aaurothiosulfate (ATS) − (Figure A). Of these Au(I) complexes, AF has been approved by the US Food and Drug Administration for Phase II clinical trial to treat cancer .…”

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confidence: 99%

Quantitative Chemoproteomic Profiling of Targets of Au(I) Complexes by Competitive Activity-Based Protein Profiling

et al. 2022

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Owing to the encouraging pharmacological action and acceptable toxicity profile, Au(I) complexes have attracted growing interest in the application of disease treatment. In order to investigate their potential target proteins and related bioinformation, herein, we screened four Au(I) complexes and explored the binding proteins utilizing a competitive activity-based protein profiling (ABPP) strategy, including identification experiments and reactivity classification experiments, which offers a simple and robust method to identify the target proteins of Au(I) complexes. We quantified the target proteins of the four Au(I) complexes and found that most of proteins were associated with cancer. In addition, the newly Au(I)-binding proteins and biological gold− protein interaction pathways were exhibited. Furthermore, we estimated the correlation between target proteins of Au(I) complexes and various cancers, which will promote the development of the gold anticancer drugs.

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Pharmacokinetic modeling of the sinusoidal efflux of anionic ligands from the isolated perfused rat liver: The influence of albumin

Proost

Nijssen

Strating

et al. 1993

Journal of Pharmacokinetics and Biopharmaceutics

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This study contains a pharmacokinetic analysis on the efflux of organic anions from the liver into the bloodstream (sinusoidal efflux) with specific reference to the influence of albumin. The net sinusoidal efflux rate of dibromosulfophthalein (DBSP) from preloaded livers, being the resultant of sinusoidal efflux and reuptake of ligand by hepatocytes downstream the sinusoid, can be strongly increased by the presence of bovine serum albumin (BSA), a protein having multiple binding sites for DBSP. We previously attributed this effect to a reduction of reuptake through extracellular binding of the organic anion to the protein, rather than to an intrinsic stimulatory effect on the actual membrane transport process from the cells. In the present study we tested this hypothesis using a pharmacokinetic multicompartment liver model. This model resembles the parallel tube model in that the liver is described by several compartments placed in series instead of a single well-stirred compartment and it takes into account rates of dissociation and association in binding to proteins in the sinusoidal space. The model parameters were fitted from the sinusoidal efflux and biliary excretion data from efflux experiments measuring the stimulatory effect of various concentrations of BSA. Equilibrium binding of DBSP to albumin as well as the dissociation rate constant (koff) were determined in vitro with rapid filtration techniques. The experimental data could not be fitted satisfactorily when using the experimentally obtained values of the protein association and dissociation rate constants (kon and koff). However, they could be simulated accurately assuming 16 times higher values for the association and dissociation rate constant compared to those determined in vitro. Time constants of the perfusate flow, liver (re)uptake, and protein association and dissociation indicate that binding equilibrium does not exist within the sinusoids and that, in particular at low protein concentrations, the net sinusoidal efflux rate is association rate-limited: A large fraction of the ligand effluxed from the cell into the median is taken up by the hepatocyte before binding to the proteins occurs. Higher kon and koff values predicted by the model might indicate altered DBSP-albumin binding characteristics upon passage through the liver but alternatively can be explained by an intrinsic effect of albumin on the carrier-mediated efflux process. Efflux experiments showed a marked stimulatory effect of the protein on sinusoidal efflux but only a moderate effect on biliary excretion, despite a strong decrease in liver content. These patterns indicate that sinusoidal efflux and biliary excretion occur from two different intracellular compartments that equilibrate slowly.

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Influence of ionic strength on the binding of sodium aurothiosulphate to human serum albumin

Cited by 8 publications

References 13 publications

Binding of sodium aurothiomalate to human serum albumin in vitro at physiological conditions.

Binding of sodium aurothiomalate to human serum albumin in vitro at physiological conditions.

Quantitative Chemoproteomic Profiling of Targets of Au(I) Complexes by Competitive Activity-Based Protein Profiling

Pharmacokinetic modeling of the sinusoidal efflux of anionic ligands from the isolated perfused rat liver: The influence of albumin

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