The role of the functional architecture of the human acetylcholinesterase (HuAChE) active centre in accommodating the non-covalent inhibitors tacrine and huperzine A, or the carbamates pyridostigmine and physostigmine, was analysed using 16 mutants of residues lining the active-centre gorge. Despite the structural diversity of the ligands, certain common properties of the complexes could be obs...

Beagle dogs are commonly used for toxicological and pharmacological studies of drug candidates in the pharmaceutical industry. Recently, we reported a CYP1A2-deficient dog with a nonsense mutation (C1117T). In this study, using CYP1A2-deficient and wild-type dog liver microsomes, substrate specificity of dog CYP1A2 was investigated and compared with human CYP1A2. For this purpose, 11 cytochrome...

To delineate the role of peptide backbone flexibility and rapid molecular motion in acetylcholinesterase catalysis and inhibitor association, we investigated the decay of fluorescence anisotropy at three sites of fluorescein conjugation to cysteine-substitution mutants of the enzyme. One cysteine was placed in a loop at the peripheral site near the rim of the active center gorge (H287C); a seco...

Phase I and Phase II Sh. sonnei exhibit differences in their susceptibility to the T series of bacteriophages. Both microorganisms are lysed by T(2) and T(6), but only the Phase II bacillus is lysed by T(3), T(4), and T(7). Lysis of the Phase I or Phase II bacillus by T(2) or T(6) is not inhibited by the homologous type-specific antigen. In the presence of an appropriate cofactor, however, the ...