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羟基磷灰石结合分子的构效关系(SAR)

Structure-activity relationships (SAR) of hydroxyapatite-binding molecules.

作者信息

Myers H M

出版信息

Calcif Tissue Int. 1987 Jun;40(6):344-8. doi: 10.1007/BF02556697.

Abstract

Carboxyl-containing molecules can bind to HA with sufficient affinity to prevent the uptake of AZ by this mineral. Structural features that favor binding can be discerned. Isolated carboxyls are inactive; adjacent dicarboxylic functions are marginally active. Crowding of oxygens in the form of vicinal carboxyls or hydroxyls contributes the property of HA binding ability. This property exhibits gradation in magnitude and the variation can be correlated with structural features of the carboxyl-containing molecule. Phospho functions are generally more powerful contributors to HA binding property than are carboxyls.

摘要

含羧基的分子能够以足够的亲和力与透明质酸(HA)结合,从而阻止这种矿物质对阿霉素(AZ)的摄取。可以识别出有利于结合的结构特征。孤立的羧基没有活性;相邻的二羧酸官能团活性微弱。以邻位羧基或羟基形式存在的氧原子密集排列有助于形成与HA的结合能力。这种性质在程度上呈现出渐变,并且这种变化可以与含羧基分子的结构特征相关联。磷酸官能团对HA结合性质的贡献通常比羧基更强。

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