Structure-activity relationship study of leucinostatin A, a natural nonapeptide, was performed to gain insight into the structural requirements for leucinostatin A to exhibit antiproliferative activity against DU-145 prostate cancer cells under cocultured conditions with the corresponding stromal cells. Twenty truncated peptide analogs of leucinostatin A revealed that the nonapeptide structure as a whole is essential for the biological activity. Alanine scanning demonstrated the importance of some of the amino acid components, including hydroxyleucine and the second leucine from the N-terminus. Two of the three aminoisobutyric acids could be substituted with one of the enantiomers of alanine, clearly demonstrating that each methyl group in these portions has a distinct influence on the growth-inhibitory activity.

进行了亮氨酸抑素A（一种天然的九肽）的结构-活性关系研究，以了解亮氨酸抑素A在与相应基质细胞共培养的条件下对DU-145前列腺癌细胞具有抗增殖活性的结构要求。亮氨酸抑素A的二十个截短的肽类似物表明，整个非肽结构对于生物学活性是必不可少的。丙氨酸扫描证明了某些氨基酸成分的重要性，包括羟胺和来自N末端的第二个亮氨酸。三种氨基异丁酸中的两种可以被丙氨酸的对映异构体之一取代，这清楚地表明，这些部分中的每个甲基基团均对生长抑制活性具有独特的影响。