AI Article Synopsis

  • Researchers have created a new scaffold called multivalent binding oligomers (MBOs) designed to bind specifically to RNA structures.
  • These MBOs can inhibit the crucial protein-RNA complex Tat-TAR, which plays a significant role in HIV replication.
  • In tests, these MBOs effectively blocked Tat-TAR binding at low concentrations, showing potential for future RNA-targeting treatments.

Article Abstract

We describe the development of a new type of scaffold to target RNA structures. Multivalent binding oligomers (MBOs) are molecules in which multiple sidechains extend from a polyamine backbone such that favorable RNA binding occurs. We have used this strategy to develop MBO-based inhibitors to prevent the association of a protein-RNA complex, Tat-TAR, that is essential for HIV replication. In vitro binding assays combined with model cell-based assays demonstrate that the optimal MBOs inhibit Tat-TAR binding at low micromolar concentrations. Antiviral studies are also consistent with the in vitro and cell-based assays. MBOs provide a framework for the development of future RNA-targeting molecules.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2783946PMC
http://dx.doi.org/10.1016/j.bmcl.2009.10.078DOI Listing

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