title: Disulfide reshuffling triggers the release of a thiol-free anti-HIV agent to make up fast-acting, potent macromolecular prodrugs.
abstract: The release of azidothymidine from macromolecular prodrugs was designed to respond to the intracellular disulfide reshuffling. This drug has no thiol groups, and a response to this trigger was engineered using a self-immolative linker. The resulting formulations were fast-acting, efficacious, and highly potent with regards to suppressing the infectivity of the virus.
authors.affiliation: Department of Chemistry, Aarhus University, Aarhus, Denmark. zelikin@chem.au.dk.
authors.forename: Anders
authors.initials: A
authors.lastname: Kock
authors.forename: Kaja
authors.initials: K
authors.lastname: Zuwala
authors.forename: Anton A A
authors.initials: AA
authors.lastname: Smith
authors.forename: Pau
authors.initials: P
authors.lastname: Ruiz-Sanchis
authors.forename: Benjamin M
authors.initials: BM
authors.lastname: Wohl
authors.forename: Martin
authors.initials: M
authors.lastname: Tolstrup
authors.forename: Alexander N
authors.initials: AN
authors.lastname: Zelikin
mesh_terms: D019380:Anti-HIV Agents / Q000737:chemistry* / Q000494:pharmacology*; D002460:Cell Line; D004220:Disulfides / Q000737:chemistry*; D004305:Dose-Response Relationship, Drug; D015658:HIV Infections / Q000188:drug therapy*; D015497:HIV-1 / Q000187:drug effects*; D006801:Humans; D046911:Macromolecular Substances / Q000737:chemistry / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D011355:Prodrugs / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013997:Time Factors; D015215:Zidovudine / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D019380:Anti-HIV Agents; D004220:Disulfides; D046911:Macromolecular Substances; D011355:Prodrugs; D015215:Zidovudine