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Towards a RIOK2 chemical probe: cellular potency improvement of a selective 2-(acylamino)pyridine series

Christopher B Wang1,2, Álvaro Lorente-Macías3, Carrow Wells1,2

  • 1Structural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill Chapel Hill NC 27599 USA alison.axtman@unc.edu.

RSC Medicinal Chemistry
|May 28, 2021
PubMed

Insights

Researchers developed novel naphthyl-pyridine compounds to study RIOK2, a kinase implicated in cancers like lung cancer and glioblastoma. These compounds are the best available tools for investigating RIOK2

Area of Science:

  • Biochemistry and Molecular Biology
  • Cancer Research
  • Medicinal Chemistry

Background:

  • RIOK2 (RIO kinase 2) is an understudied kinase implicated in various human cancers.
  • Current research lacks potent, selective, and cell-active chemical probes for RIOK2.
  • Effective probes are crucial for understanding RIOK2's biological functions and therapeutic potential.

Purpose of the Study:

  • To synthesize and characterize novel naphthyl-pyridine based compounds.
  • To improve cellular activity and selectivity for RIOK2.
  • To develop improved tool molecules for RIOK2 research.

Main Methods:

  • Synthesis of naphthyl-pyridine derivatives.
  • Evaluation of compound cellular activity.
  • Assessment of RIOK2 selectivity.

Main Results:

  • Novel naphthyl-pyridine compounds with enhanced cellular activity were synthesized.
  • Compounds demonstrated maintained selectivity for RIOK2.
  • These molecules represent the best available tool compounds for RIOK2 characterization.

Conclusions:

  • The developed naphthyl-pyridine compounds are valuable tools for RIOK2 research.
  • These compounds advance the study of RIOK2 in cancer biology.
  • Further research using these tools may validate RIOK2 as a therapeutic target.

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