title: Development of highly cytotoxic and actin-depolymerizing biotin derivatives of aplyronine A.
abstract: Tied up: a PEG-linked biotin derivative of marine macrolide aplyronine A (ApA) is shown to exhibit potent cytotoxicity and cause actin disassembly in tumor cells. This method of introducing a PEG linker at the end of the aliphatic tail should offer perspectives for developing and using versatile actin-targeting molecular probes. PEG=poly(ethylene glycol).
authors.affiliation: Graduate School of Pure and Applied Sciences, University of Tsukuba, Tennodai, Japan. mkita@chem.tsukuba.ac.jp
authors.forename: Masaki
authors.initials: M
authors.lastname: Kita
authors.forename: Yuichiro
authors.initials: Y
authors.lastname: Hirayama
authors.forename: Miyuki
authors.initials: M
authors.lastname: Sugiyama
authors.forename: Hideo
authors.initials: H
authors.lastname: Kigoshi
mesh_terms: D000199:Actins / Q000737:chemistry*; D001710:Biotin / Q000737:chemistry*; D002470:Cell Survival / Q000187:drug effects; D018360:Crystallography, X-Ray; D004305:Dose-Response Relationship, Drug; D006367:HeLa Cells; D006801:Humans; D018942:Macrolides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D008958:Models, Molecular; D008968:Molecular Conformation; D013329:Structure-Activity Relationship
chemical_list: D000199:Actins; D018942:Macrolides; C104057:aplyronine A; D001710:Biotin