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Small molecule targeting of biologically relevant RNA tertiary and quaternary structures.

Publication ,  Journal Article
Zafferani, M; Hargrove, AE
Published in: Cell chemical biology
May 2021

Initial successes in developing small molecule ligands for non-coding RNAs have underscored their potential as therapeutic targets. More recently, these successes have been aided by advances in biophysical and structural techniques for identification and characterization of more complex RNA structures; these higher-level folds present protein-like binding pockets that offer opportunities to design small molecules that could achieve a degree of selectivity often hard to obtain at the primary and secondary structure level. More specifically, identification and small molecule targeting of RNA tertiary and quaternary structures have allowed researchers to probe several human diseases and have resulted in promising clinical candidates. In this review we highlight a selection of diverse and exciting successes and the experimental approaches that led to their discovery. These studies include examples of recent developments in RNA-centric assays and ligands that provide insight into the features responsible for the affinity and biological outcome of RNA-targeted chemical probes. This report highlights the potential and emerging opportunities to selectively target RNA tertiary and quaternary structures as a route to better understand and, ultimately, treat many diseases.

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Published In

Cell chemical biology

DOI

EISSN

2451-9448

ISSN

2451-9456

Publication Date

May 2021

Volume

28

Issue

5

Start / End Page

594 / 609

Related Subject Headings

  • Small Molecule Libraries
  • RNA
  • Nucleic Acid Conformation
  • Ligands
  • Humans
  • 3404 Medicinal and biomolecular chemistry
  • 3101 Biochemistry and cell biology
 

Citation

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Zafferani, M., & Hargrove, A. E. (2021). Small molecule targeting of biologically relevant RNA tertiary and quaternary structures. Cell Chemical Biology, 28(5), 594–609. https://doi.org/10.1016/j.chembiol.2021.03.003
Zafferani, Martina, and Amanda E. Hargrove. “Small molecule targeting of biologically relevant RNA tertiary and quaternary structures.Cell Chemical Biology 28, no. 5 (May 2021): 594–609. https://doi.org/10.1016/j.chembiol.2021.03.003.
Zafferani M, Hargrove AE. Small molecule targeting of biologically relevant RNA tertiary and quaternary structures. Cell chemical biology. 2021 May;28(5):594–609.
Zafferani, Martina, and Amanda E. Hargrove. “Small molecule targeting of biologically relevant RNA tertiary and quaternary structures.Cell Chemical Biology, vol. 28, no. 5, May 2021, pp. 594–609. Epmc, doi:10.1016/j.chembiol.2021.03.003.
Zafferani M, Hargrove AE. Small molecule targeting of biologically relevant RNA tertiary and quaternary structures. Cell chemical biology. 2021 May;28(5):594–609.

Published In

Cell chemical biology

DOI

EISSN

2451-9448

ISSN

2451-9456

Publication Date

May 2021

Volume

28

Issue

5

Start / End Page

594 / 609

Related Subject Headings

  • Small Molecule Libraries
  • RNA
  • Nucleic Acid Conformation
  • Ligands
  • Humans
  • 3404 Medicinal and biomolecular chemistry
  • 3101 Biochemistry and cell biology