Garrido M N, Lisa T A, Domenech C E
Departamento de Biología Molecular, Facultad de Ciencias Exactas, Universidad Nacional de Río Cuarto, Córdoba, Argentina.
Mol Cell Biochem. 1988 Nov;84(1):41-9. doi: 10.1007/BF00235191.
In this work the action of the following compounds upon Ps. aeruginosa acid phosphatase has been studied: 1) alkylammonium compounds; 2) aminoalcohols and aminoacids with different substituents (-H, -CH2OH and -CH3) attached to the nitrogen atom; 3) alcohols analogous to some compounds of the above series, but without the amino group. It was found that the enzyme inhibition was more effective with N-trimethylated compounds than with the triethylated ones. The degree of inhibition depended on the number of methyl groups bound to the nitrogen atom. Taking into account the choline and betaine series the hydroxyl derivatives showed more affinity for the enzyme than the carboxylated ones. In each series the Ki values increased with the decrease of methyl groups bound to the nitrogen atom. The presence of a positively charged nitrogen atom in the molecule of the effector was essential. These results enable us to confirm that in the molecule of Ps. aeruginosa acid phosphatase there exists an anionic site with one subsite with affinity for methyl groups.
在本研究中，我们研究了以下化合物对铜绿假单胞菌酸性磷酸酶的作用：1）烷基铵化合物；2）氮原子上连接有不同取代基（-H、-CH2OH和-CH3）的氨基醇和氨基酸；3）与上述系列某些化合物类似但不含氨基的醇。结果发现，N-三甲基化化合物对该酶的抑制作用比对三乙基化化合物更有效。抑制程度取决于与氮原子结合的甲基数量。考虑到胆碱和甜菜碱系列，羟基衍生物对该酶的亲和力比羧基化衍生物更高。在每个系列中，Ki值随着与氮原子结合的甲基数量的减少而增加。效应分子中带正电荷的氮原子的存在至关重要。这些结果使我们能够确认，在铜绿假单胞菌酸性磷酸酶分子中存在一个阴离子位点，其中一个亚位点对甲基具有亲和力。
