CRA-024781 is a novel, broad spectrum hydroxamic acid-based inhibitor of histone deacetylase (HDAC) that shows antitumor activity in vitro and in vivo preclinically and is under evaluation in phase I clinical trials for cancer. CRA-024781 inhibited pure recombinant HDAC1 with a K(i) of 0.007 mumol/L, and also inhibited the other HDAC isozymes HDAC2, HDAC3/SMRT, HDAC6, HDAC8, and HDAC10 in the n...

Interactions between complementary protein and carbohydrate structures on different genera of human oral bacteria have been implicated in the formation of dental plaque. The carbohydrate receptor on Streptococcus sanguis H1 (one of the primary colonizing species) that is specific for the adhesin on Capnocytophaga ochracea ATCC 33596 (a secondary colonizer) has been isolated from the streptococc...

This paper reports that the acetylation of lysine epsilon-NH3(+) groups of alpha-amylase--one of the most important hydrolytic enzymes used in industry--produces highly negatively charged variants that are enzymatically active, thermostable, and more resistant than the wild-type enzyme to irreversible inactivation on exposure to denaturing conditions (e.g., 1 h at 90 degrees C in solutions cont...

The inclusion of low-acetylated Gellan Gum and κ-carrageenan into amyloid fibril gels reinforces them mechanically, while preserving the surface functionality fibrils.

1. Acetylated chymotrypsinogen was prepared by the reaction of crystallized chymotrypsinogen with acetic anhydride at pH 6.7 and 4O, and purification of the product. End group analysis and Van Slyke amino nitrogen determination indicated that all the free Eand or-amino groups of the chymotrypsinogen molecule had been blocked by acetylation. 2. Activation of acetylated chymotrypsinogen by trypsi...

Contributions of tyrosyl residues to trypsinand chymotrypsin-inhibitory activities in two homologous proteinase inhibitors were investigated by modifying them with N-acetylimidazole under various conditions. In Bowman-Birk soybean proteinase inhibitor, Tyr 55, immediately following the antichymotryptic site, Leu 53-Ser 54, is relatively inaccessible to N-acetylimidazole and can only be acetylat...

Monocytes/macrophages (Mo) appear to play a critical role in the initiation and progression of atherosclerotic lesions. In this study, we characterized in vitro-differentiated embryonic stem (ES) cell macrophages as a model system for studying atherosclerosis-associated Mo functions. Using immunofluorescence staining and Western analysis, we demonstrate that ES Mo express typical macrophage cel...

Group B Streptococcus (GBS) is the leading cause of human neonatal sepsis and meningitis. The GBS capsular polysaccharide is a major virulence factor and the active principle of vaccines in phase II trials. All GBS capsules have a terminal alpha 2-3-linked sialic acid [N-acetylneuraminic acid (Neu5Ac)], which interferes with complement-mediated killing. We show here that some of the Neu5Ac resi...