Characterization and screening of tight binding inhibitors of xanthine oxidase: an on-flow assay

RSC Advances ◽  
2015 ◽  
Vol 5 (47) ◽  
pp. 37533-37538 ◽  
Author(s):  
M. V. N. Rodrigues ◽  
R. S. Corrêa ◽  
K. L. Vanzolini ◽  
D. S. Santos ◽  
A. A. Batista ◽  
...  
Keyword(s):  
Xanthine Oxidase ◽  
Tight Binding ◽  
Flow Characterization ◽  
Binding Inhibitors

On-flow characterization of tight binders of xanthine oxidase.

The design, synthesis, and characterization of tight-binding inhibitors of calmodulin

1985 ◽  
Vol 29 (2) ◽  
pp. 83-93 ◽  
Author(s):  
William F. DeGrado ◽  
Frank G. Prendergast ◽  
Henry R. Wolfe ◽  
Jos A. Cox
Keyword(s):  
Tight Binding ◽  
Synthesis And Characterization ◽  
Design Synthesis ◽  
Binding Inhibitors

scholarly journals Tight binding inhibitors of xanthine oxidase

1981 ◽  
Vol 14 (2) ◽  
pp. 249-263 ◽  
Author(s):  
Russ Hille ◽  
Vincent Massey
Keyword(s):  
Xanthine Oxidase ◽  
Tight Binding ◽  
Binding Inhibitors

scholarly journals Accurate quantitative determination of affinity and binding kinetics for tight binding inhibition of xanthine oxidase

2021 ◽  
Vol 139 ◽  
pp. 111664
Author(s):  
Haiyang Yang ◽  
Xueyan Li ◽  
Gang Li ◽  
Huating Huang ◽  
Wenning Yang ◽  
...  
Keyword(s):  
Quantitative Determination ◽  
Xanthine Oxidase ◽  
Tight Binding ◽  
Binding Kinetics ◽  
Binding Inhibition

scholarly journals Extended lubrication theory: improved estimates of flow in channels with variable geometry

2017 ◽  
Vol 473 (2206) ◽  
pp. 20170234 ◽  
Author(s):  
Behrouz Tavakol ◽  
Guillaume Froehlicher ◽  
Douglas P. Holmes ◽  
Howard A. Stone
Keyword(s):  
Stokes Equations ◽  
Perturbation Expansion ◽  
Accurate Estimate ◽  
Higher Order ◽  
Lubrication Theory ◽  
Channel Height ◽  
Fluid Films ◽  
Flow Characterization ◽  
Systematic Perturbation

Lubrication theory is broadly applicable to the flow characterization of thin fluid films and the motion of particles near surfaces. We offer an extension to lubrication theory by starting with Stokes equations and considering higher-order terms in a systematic perturbation expansion to describe the fluid flow in a channel with features of a modest aspect ratio. Experimental results qualitatively confirm the higher-order analytical solutions, while numerical results are in very good agreement with the higher-order analytical results. We show that the extended lubrication theory is a robust tool for an accurate estimate of pressure drop in channels with shape changes on the order of the channel height, accounting for both smooth and sharp changes in geometry.

scholarly journals Characterization of human pre-elafin mutants: full antipeptidase activity is essential to preserve lung tissue integrity in experimental emphysema

2007 ◽  
Vol 405 (3) ◽  
pp. 455-463 ◽  
Author(s):  
Alain Doucet ◽  
Dominique Bouchard ◽  
Marie France Janelle ◽  
Audrey Bellemare ◽  
Stéphane Gagné ◽  
...  
Keyword(s):  
Lung Tissue ◽  
Neutrophil Elastase ◽  
Tight Binding ◽  
Biochemical Properties ◽  
Van Der Waals Interactions ◽  
Tissue Destruction ◽  
Methionine Residue ◽  
Experimental Emphysema

Pre-elafin is a tight-binding inhibitor of neutrophil elastase and myeloblastin; two enzymes thought to contribute to tissue damage in lung emphysema. Previous studies have established that pre-elafin is also an effective anti-inflammatory molecule. However, it is not clear whether both functions are linked to the antipeptidase activity of pre-elafin. As a first step toward elucidating the structure/function relationship of this protein, we describe here the construction and characterization of pre-elafin variants with attenuated antipeptidase potential. In these mutants, the P1′ methionine residue of the inhibitory loop is replaced by either a lysine (pre-elafinM25K) or a glycine (pre-elafinM25G) residue. Both mutated variants are stable and display biochemical properties undistinguishable from WT (wild-type) pre-elafin. However, compared with WT pre-elafin, their inhibitory constants are increased by one to four orders of magnitude toward neutrophil elastase, myeloblastin and pancreatic elastase, depending on the variants and enzymes tested. As suggested by molecular modelling, this attenuated inhibitory potential correlates with decreased van der Waals interactions between the variants and the enzymes S1′ subsite. In elastase-induced experimental emphysema in mice, only WT pre-elafin protected against tissue destruction, as assessed by the relative airspace enlargement measured using lung histopathological sections. Pre-elafin and both mutants prevented transient neutrophil alveolitis. However, even the modestly affected pre-elafinM25K mutant, as assayed in vitro with small synthetic substrates, was a poor inhibitor of the neutrophil elastase and myeloblastin elastolytic activity measured with insoluble elastin. We therefore conclude that full antipeptidase activity of pre-elafin is essential to protect against lung tissue lesions in this experimental model.

Estimating KI values for tight binding inhibitors from dose-response plots

1995 ◽  
Vol 5 (17) ◽  
pp. 1947-1952 ◽  
Author(s):  
Robert A. Copeland ◽  
Diane Lombardo ◽  
John Giannaras ◽  
Carl P. Decicco
Keyword(s):  
Dose Response ◽  
Tight Binding ◽  
Binding Inhibitors

Linking Diagenesis, NMR, and Dynamic Data for Accurate Flow Characterization of Heterogeneous Carbonate Reservoir

2014 ◽  
Author(s):  
Umer Farooq ◽  
Reza Iskandar ◽  
El Sayed Moustafa Radwan ◽  
Magdy Ahmed H Hozayen
Keyword(s):  
Carbonate Reservoir ◽  
Dynamic Data ◽  
Flow Characterization

Slow- and tight-binding inhibitors of the 85-kDa human phospholipase A2

Biochemistry ◽  
1993 ◽  
Vol 32 (23) ◽  
pp. 5935-5940 ◽  
Author(s):  
Ian P. Street ◽  
Hung Kuei Lin ◽  
France Laliberte ◽  
Farideh Ghomashchi ◽  
Zhaoyin Wang ◽  
...  
Keyword(s):  
Phospholipase A2 ◽  
Tight Binding ◽  
Binding Inhibitors
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