scholarly journals X-ray crystal structure and specificity of the Toxoplasma gondii ME49 TgAPN2

2020 ◽  
Vol 477 (19) ◽  
pp. 3819-3832
Author(s):  
Emilia M. Marijanovic ◽  
Karolina Weronika Swiderska ◽  
James Andersen ◽  
Jasmin C. Aschenbrenner ◽  
Chaille T. Webb ◽  
...  

Toxoplasmosis is a parasitic disease caused by infection with Toxoplasma gondii that currently has few therapeutic options. The M1 aminopeptidase enzymes have been shown to be attractive targets for anti-parasitic agents and/or vaccine candidates, suggesting potential to re-purpose inhibitors between parasite M1 aminopeptidase targets. The M1 aminopeptidase TgAPN2 has been suggested to be a potential new drug target for toxoplasmosis. Here we investigate the structure and function of TgAPN2, a homologue of the antimalarial drug target PfA-M1, and evaluate the capacity to use inhibitors that target PfA-M1 against TgAPN2. The results show that despite a similar overall fold, the TgAPN2 has a unique substrate specificity and inhibition profile. Sequence and structure differences are investigated and show how comparative structure-activity relationships may provide a route to obtaining potent inhibitors of TgAPN2.

1999 ◽  
Vol 82 (08) ◽  
pp. 271-276 ◽  
Author(s):  
Glen Spraggon ◽  
Stephen Everse ◽  
Russell Doolittle

IntroductionAfter a long period of anticipation,1 the last two years have witnessed the first high-resolution x-ray structures of fragments from fibrinogen and fibrin.2-7 The results confirmed many aspects of fibrinogen structure and function that had previously been inferred from electron microscopy and biochemistry and revealed some unexpected features. Several matters have remained stubbornly unsettled, however, and much more work remains to be done. Here, we review several of the most significant findings that have accompanied the new x-ray structures and discuss some of the problems of the fibrinogen-fibrin conversion that remain unresolved. * Abbreviations: GPR—Gly-Pro-Arg-derivatives; GPRPam—Gly-Pro-Arg-Pro-amide; GHRPam—Gly-His-Arg-Pro-amide


2010 ◽  
Vol 98 (3) ◽  
pp. 46a
Author(s):  
Reinhard Kraemer ◽  
Susanne Ressl ◽  
Vera Ott ◽  
Sascha Nicklisch ◽  
Heinz-Juergen Steinhoff ◽  
...  

2015 ◽  
Vol 1125 ◽  
pp. 60-63
Author(s):  
Chutharat Paikaew ◽  
Juthamas Inthanont ◽  
Adisak Punyanut ◽  
Ekachai Hoonnivathana ◽  
Pichet Limsuwan ◽  
...  

The purpose of this research was to investigate physical properties, configuration and color of topaz. Topazes were irradiated with electron beam linear accelerator at different dose from 40 to 180 MGy. The color of topaz was analyzed by UV-vis and it was shown that the color of topaz was becoming strong color with increased electron beam dose. Crystal structure and function group of topaz were characterized by X- ray diffraction (XRD) and Fourier transform infrared (FTIR) spectroscopy. The results showed that the topaz has orthorhombic structure and no other crystalline. After irradiated, topaz released OH indicating higher crystallinity of topaz and this was confirmed with the results of electron spin resonance (ESR). Electron beam dose response of topaz was investigated. ESR results showed that the Al3+ ion was substituted in Si4+ site and Ti3+ impurity in Al4+ site and this result corresponds to the results of FTIR. The experiment result indicated that electron beam could be making defect on crystal structure and color enhancement of topaz.


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