Testing carrier models of cotransport using the binding kinetics of non-transported competitive inhibitors

1980 ◽  
Vol 596 (2) ◽  
pp. 272-291 ◽  
Author(s):  
R.James Turner ◽  
M. Silverman
2021 ◽  
Vol 14 (10) ◽  
pp. 1032
Author(s):  
Markus Schweipert ◽  
Niklas Jänsch ◽  
Neha Upadhyay ◽  
Kalpana Tilekar ◽  
Ewelina Wozny ◽  
...  

Recently, we have reported that non-hydroxamate thiazolidinedione (TZD) analogs are capable of inhibiting human deacetylase 4 (HDAC4). This study aims at the dissection of the molecular determinants and kinetics of the molecular recognition of TZD ligands by HDAC4. For this purpose, a structure activity relationship analysis of 225 analogs was combined with a comprehensive study of the enzyme and binding kinetics of a variety of HDAC4 mutant variants. The experimental data were rationalized by docking to the two major conformations of HDAC4. TZD ligands are competitive inhibitors and bind via a two-step mechanism involving principal molecular recognition and induced fit. The residence time of 24 g is (34 ± 3) min and thus much larger than that of the canonical pan-HDAC inhibitor SAHA ((5 ± 2) min). Importantly, the binding kinetics can be tuned by varying the structure of the CAP group.


2013 ◽  
Author(s):  
Robert Tower ◽  
Graeme Campbell ◽  
Marc Muller ◽  
Olga Will ◽  
Frederieka Grundmann ◽  
...  

2018 ◽  
Author(s):  
Luke Jordan ◽  
Nathan Wittenberg

This is a comprehensive study of the effects of the four major brain gangliosides (GM1, GD1b, GD1a, and GT1b) on the adsorption and rupture of phospholipid vesicles on SiO2 surfaces for the formation of supported lipid bilayer (SLB) membranes. Using quartz crystal microbalance with dissipation monitoring (QCM-D) we show that gangliosides GD1a and GT1b significantly slow the SLB formation process, whereas GM1 and GD1b have smaller effects. This is likely due to the net ganglioside charge as well as the positions of acidic sugar groups on ganglioside glycan head groups. Data is included that shows calcium can accelerate the formation of ganglioside-rich SLBs. Using fluorescence recovery after photobleaching (FRAP) we also show that the presence of gangliosides significantly reduces lipid diffusion coefficients in SLBs in a concentration-dependent manner. Finally, using QCM-D and GD1a-rich SLB membranes we measure the binding kinetics of an anti-GD1a antibody that has similarities to a monoclonal antibody that is a hallmark of a variant of Guillain-Barre syndrome.


1995 ◽  
Vol 270 (10) ◽  
pp. 5014-5018 ◽  
Author(s):  
Aditya P. Koley ◽  
Jeroen T. M. Buters ◽  
Richard C. Robinson ◽  
Allen Markowitz ◽  
Fred K. Friedman

iScience ◽  
2021 ◽  
Vol 24 (2) ◽  
pp. 102104
Author(s):  
Yunjin Song ◽  
Hoibin Jeong ◽  
Song-Rae Kim ◽  
Yiseul Ryu ◽  
Jonghwi Baek ◽  
...  

2011 ◽  
Vol 50 (8) ◽  
pp. 3458-3463 ◽  
Author(s):  
Shari U. Dunham ◽  
Todd S. Remaley ◽  
Bryn S. Moore ◽  
Debra L. Evans ◽  
Stephen U. Dunham

Biochemistry ◽  
2013 ◽  
Vol 52 (14) ◽  
pp. 2482-2491 ◽  
Author(s):  
Harriet E. Seward ◽  
Jaswir Basran ◽  
Roanne Denton ◽  
Mark Pfuhl ◽  
Frederick W. Muskett ◽  
...  

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