Williams G, Sallis J D
Biochem J. 1979 Oct 15;184(1):181-4. doi: 10.1042/bj1840181.
The relative abilities of some compounds to inhibit the transformation of amorphous calcium phosphate into hydroxyapatite were determined. Organic diphosphates, fructose 1,6-bisphosphate, pyrophosphate, imidodiphosphate and 3-phospholycerate all inhibited to various degrees. Strong inhibition was observed with phosphonoformate, and phosphocitrate proved to be the most powerful of the inhibitors examined. On the basis of these new findings an improved concept of the structure--activity relationship of inhibitors is proposed and mechanisms for inhibitor action are discussed.
测定了一些化合物抑制无定形磷酸钙转化为羟基磷灰石的相对能力。有机二磷酸盐、果糖1,6-二磷酸、焦磷酸盐、亚氨基二磷酸盐和3-磷酸甘油酸均有不同程度的抑制作用。膦甲酸表现出强烈的抑制作用,而磷酸柠檬酸被证明是所检测的抑制剂中最有效的。基于这些新发现,提出了抑制剂结构-活性关系的改进概念,并讨论了抑制剂作用的机制。