Target proteins of ganoderic acid DM provides clues to various pharmacological mechanisms.
作者： Jie Liu , Kuniyoshi Shimizu , Akinobu Tanaka , Wakako Shinobu , Koichiro Ohnuki
DOI: 10.1038/SREP00905
关键词: Cytotoxicity 、 Ganodermataceae 、 Plasma protein binding 、 Tubulin 、 Signal transduction 、 Cell culture 、 Biochemistry 、 Structure–activity relationship 、 Ganoderma 、 Biology
摘要: Ganoderma fungus (Ganodermataceae) is a multifunctional medicinal mushroom and has been traditionally used for the treatment of various types disease. Ganoderic acid DM (1) representative triterpenoid isolated from G. lingzhi exhibits biological activities. However, universal starting point that triggers multiple signaling pathways results in multifunctionality 1 unknown. Here we demonstrate important clues regarding mechanisms underlying multi-medicinal action 1. We examined structure–activity relationships between its analogs found carbonyl group at C-3 was essential cytotoxicity. Subsequently, 1-conjugated magnetic beads as probe identified tubulin specific 1-binding protein. Furthermore, showed similar Kd to vinblastine also affected assembly polymers. This study revealed activities may contribute design development new tubulin-inhibiting agents.
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