The first enantioselective synthesis of lysine(4-ene) and lysine(4-yne) is described. These amino acids, as well as histidine and diaminopropionic-acid-glycine, were incorporated at the P1 and/or P3 positions of oligopeptide vinyl sulfones. All inhibitors were found to inhibit proteasome subunit β2, but with a loss of potency compared to our most potent and selective β2 inhibitor, LU-102.

中文翻译：

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碱性降低的赖氨酸类似物的不对称合成及其掺入蛋白酶体抑制剂。

描述了赖氨酸（4-ene）和赖氨酸（4-yne）的第一次对映选择性合成。这些氨基酸以及组氨酸和二氨基丙酸-甘氨酸被掺入到寡肽乙烯基砜的P1和/或P3位置。发现所有抑制剂均能抑制蛋白酶体亚基β2，但与我们最有效和选择性最强的β2抑制剂LU-102相比，其功效却有所降低。