Ontology highlight
ABSTRACT:
SUBMITTER: Bhatia S
PROVIDER: S-EPMC6249066 | biostudies-literature | 2018 Nov
REPOSITORIES: biostudies-literature
Bhatia Sanil S Krieger Viktoria V Groll Michael M Osko Jeremy D JD Reßing Nina N Ahlert Heinz H Borkhardt Arndt A Kurz Thomas T Christianson David W DW Hauer Julia J Hansen Finn K FK
Journal of medicinal chemistry 20181108 22
Dual- or multitarget drugs have emerged as a promising alternative to combination therapies. Proteasome inhibitors (PIs) possess synergistic activity with histone deacetylase (HDAC) inhibitors due to the simultaneous blockage of the ubiquitin degradation and aggresome pathways. Here, we present the design, synthesis, binding modes, and anticancer properties of RTS-V5 as the first-in-class dual HDAC-proteasome ligand. The inhibition of both targets was confirmed by biochemical and cellular assays ...[more]