Center for Drug Discovery, Graduate School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Suruga-ku, Shizuoka 422-8526, Japan.
Bioorg Med Chem Lett. 2010 Mar 1;20(5):1578-80. doi: 10.1016/j.bmcl.2010.01.088. Epub 2010 Jan 21.
Biochemical analysis of the cellular target of S-trityl-l-cysteine (STLC) derivatives was performed by using the newly synthesized STLC derivative-immobilized affinity beads (3d). The affinity beads efficiently captured KSP in HCT116 cytoplasmic cell lysate. The results obtained from pull-down and competition experiments using 3d with STLC derivatives provided the first evidence for direct interaction of these derivatives with KSP in cancer cells. Design, synthesis and application of 3d were reported.
通过使用新合成的 STLC 衍生物固定亲和珠（3d）对 S-三苯甲基-L-半胱氨酸（STLC）衍生物的细胞靶标进行了生化分析。亲和珠可有效捕获 HCT116 细胞质细胞裂解液中的 KSP。使用 3d 与 STLC 衍生物进行下拉和竞争实验的结果首次提供了这些衍生物与癌细胞中 KSP 直接相互作用的证据。报道了 3d 的设计、合成和应用。
