title: The natural product hybrid of Syringolin A and Glidobactin A synergizes proteasome inhibition potency with subsite selectivity.
abstract: The preparation of a Syringolin A/Glidobactin A hybrid (SylA-GlbA) consisting of a SylA macrocycle connected to the GlbA side chain and its potent proteasome targeting of all three proteasomal subsites is reported. The influence of the syrbactin macrocycle moiety on subsite selectivity is demonstrated.
authors.affiliation: Zentrum für Medizinische Biotechnologie, Fakultät für Biologie und Geographie, Universität Duisburg-Essen, 45117 Essen, Germany.
authors.forename: Jérôme
authors.initials: J
authors.lastname: Clerc
authors.forename: Nan
authors.initials: N
authors.lastname: Li
authors.forename: Daniel
authors.initials: D
authors.lastname: Krahn
authors.forename: Michael
authors.initials: M
authors.lastname: Groll
authors.forename: André S
authors.initials: AS
authors.lastname: Bachmann
authors.forename: Bogdan I
authors.initials: BI
authors.lastname: Florea
authors.forename: Herman S
authors.initials: HS
authors.lastname: Overkleeft
authors.forename: Markus
authors.initials: M
authors.lastname: Kaiser
mesh_terms: D001665:Binding Sites / Q000187:drug effects; D001688:Biological Products / Q000737:chemistry*; D008958:Models, Molecular; D008968:Molecular Conformation; D010456:Peptides, Cyclic / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011480:Protease Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D061988:Proteasome Inhibitors; D013329:Structure-Activity Relationship; D013379:Substrate Specificity
chemical_list: D001688:Biological Products; D010456:Peptides, Cyclic; D011480:Protease Inhibitors; D061988:Proteasome Inhibitors; C407267:syringolin A; C057878:glidobactin A