A series of etacrynic acid derivatives was synthesized and screened for their in vitro activity against Plasmodium falciparum, as well as their activity against recombinantly expressed falcipain-2 and -3. The two most active compounds of the series displayed IC50 values of 9.0 and 18.8 μM against Plasmodia.
Enzymes in oligosaccharide synthesis: active-domain overproduction, specificity study, and synthetic use of an .alpha.-1,2-mannosyltransferase with regeneration of GDP-Man
作者:Peng Wang、Gwo Jenn Shen、Yi Fong Wang、Yoshitaka Ichikawa、Chi Huey Wong
DOI:10.1021/jo00067a035
日期:1993.7
The catalytic domain of a membrane-bound alpha-1,2-mannosyltransferase (ManT) from yeast has been overexpressed in E. coli, at a level of approximately 0.7-0.8 units per L with a specific activity of about 1 U/mg (based on a-methyl mannoside) after purification. The E. coli strain has been deposited in ATCC (#77379) and will be available to the public. The isolated ManT is stable in 30% methanol or 20% acetone. It accepts mannose, mannobiose, and O-mannosylglycopeptides as acceptors. A multiple enzyme system with in situ regeneration of GDP-mannose suitable for large-scale synthesis of mannosides and mannosyl glycopeptides has been developed.
Engelfried,C. et al., Liebigs Annalen der Chemie, 1979, p. 973 - 985
作者:Engelfried,C. et al.
DOI:——
日期:——
Wong, Chi-Huey; Schuster, Matthias; Wang, Peng, Journal of the American Chemical Society, 1993, vol. 115, # 14, p. 5893 - 5898
Aqueous solutions containing amino acids and peptides. Part 16.—Solute–solute interactions in solutions containing some N-acetyl-N′-methylamino acid amides
作者:G. Michael Blackburn、Terence H. Lilley、Peter J. Milburn
DOI:10.1039/f19858102191
日期:——
also obtained for the sparingly soluble substance N-acetylglycyl-L-alaninamide. The results obtained have been used to calculate the pairwise free energy and enthalpy coefficients for the homotactic and heterotacticinteractions and these are compared with results obtained earlier on some analogous systems containing the primary amino acid amides. A group-additivity approach has been used to rationalise