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Updated: Aug 3, 2025

Sample Preparation for Mass Spectrometry-based Identification of RNA-binding Regions
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Sample Preparation for Mass Spectrometry-based Identification of RNA-binding Regions

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RNA-binding proteins in cancer drug discovery

Jean B Bertoldo1, Simon Müller2, Stefan Hüttelmaier3

  • 1Children's Cancer Institute, Lowy Cancer Research Centre, UNSW Sydney, Sydney, NSW, Australia; School of Clinical Medicine, UNSW Sydney, Sydney, NSW, Australia.

Drug Discovery Today
|April 9, 2023
PubMed

Insights

RNA-binding proteins (RBPs) are key in cancer, but challenging to target. This review explores RBP inhibitors, their mechanisms, and potential for cancer drug discovery.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • RNA-binding proteins (RBPs) play significant roles in cancer development.
  • RBPs are often considered 'undruggable' due to complex RNA-protein interactions.
  • Targeting RNA-protein interactions is an emerging strategy in cancer therapy.

Purpose of the Study:

  • To review the role of structurally distinct RBPs in cancer.
  • To discuss mechanisms of small-molecule inhibitors (SMOIs) targeting RBPs.
  • To evaluate the translational potential of RBP-directed therapies.

Main Methods:

  • Literature review of RBP roles in cancer.
  • Analysis of RBP-directed small-molecule inhibitors (SMOIs).
  • Examination of drug-protein interactions, binding surfaces, and potency.

Main Results:

  • Over the past decade, clinically relevant RBP inhibitors have been developed.
  • Disruption of RNA-protein networks shows therapeutic promise.
  • Small-molecule inhibitors target specific RBP functions and interactions.

Conclusions:

  • Targeting RBPs represents a promising, albeit challenging, avenue for cancer drug discovery.
  • Understanding drug-protein interactions and binding surfaces is crucial for developing effective SMOIs.
  • Further development of assays and strategies is needed to overcome limitations in RBP-targeting drug discovery.
Keywords:
Drug discoveryRNA biologyRNA-binding proteinsRNA-protein interactionscancer therapeutics

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