title: Development of a new enzyme-responsive self-immolative spacer conjugate applicable to the controlled drug release.
abstract: A new self-immolative spacer conjugate based on a chemical adaptor unit aiming at controlled releasing drugs was designed and synthesized. It releases a fluorophore which was used as a model drug via a spontaneous cyclization mechanism after cleavage of an enzyme substrate. This system was proved to be stable under physiological conditions and only decomposed triggered by enzyme. It provides a generic linkage allowing connection of a variety of drugs and targeted devices to the chemical adaptor.
authors.affiliation: Key Laboratory of Natural Resources of Changbai Mountain & Functional Molecules, Yanbian University, Ministry of Education, Yanji 133002, China. jinhj@ybu.edu.cn
authors.forename: Hui-juan
authors.initials: HJ
authors.lastname: Jin
authors.forename: Jing
authors.initials: J
authors.lastname: Lu
authors.forename: Xue
authors.initials: X
authors.lastname: Wu
mesh_terms: D003374:Coumarins / Q000737:chemistry* / Q000378:metabolism; D003500:Cyclization; D003545:Cysteine / Q000737:chemistry; D003692:Delayed-Action Preparations / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism*; D015195:Drug Design; D004798:Enzymes / Q000378:metabolism*; D005456:Fluorescent Dyes / Q000737:chemistry / Q000378:metabolism; D015394:Molecular Structure; D010399:Penicillin Amidase / Q000378:metabolism
chemical_list: D003374:Coumarins; D003692:Delayed-Action Preparations; D004798:Enzymes; D005456:Fluorescent Dyes; C055467:7-amino-4-trifluoromethylcoumarin; D010399:Penicillin Amidase; D003545:Cysteine