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Mining Public Domain Data to Develop Selective DYRK1A Inhibitors.

Scott H Henderson1, Fiona Sorrell2, James Bennett3

  • 1Sussex Drug Discovery Centre, University of Sussex, Brighton BN1 9RH, U.K.

ACS Medicinal Chemistry Letters
|August 25, 2020
PubMed
Summary
This summary is machine-generated.

Researchers developed a new method to repurpose existing compounds for targeted kinase inhibition. This approach led to the creation of 8b, a highly selective inhibitor for dual-specificity tyrosine-regulated kinase 1A (DYRK1A).

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Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays
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Area of Science:

  • Biochemistry
  • Pharmacology
  • Medicinal Chemistry

Background:

  • Kinases are critical targets in drug discovery, but achieving selective inhibition among the ~500 human kinases is challenging.
  • Selective kinase inhibitors are essential for studying specific biological pathways and target engagement.
  • Repurposing existing compounds offers an efficient strategy to develop novel inhibitors.

Purpose of the Study:

  • To present an open-source software pipeline for repurposing kinase inhibitor compounds.
  • To develop a highly selective inhibitor for dual-specificity tyrosine-regulated kinase 1A (DYRK1A).
  • To demonstrate efficient chemical modification for achieving target selectivity.

Main Methods:

  • Utilized an open-source software pipeline to analyze public domain data.
  • Identified and repurposed compounds from previous kinase inhibitor projects.
  • Employed targeted chemical modification (addition of a methyl group) to a GSK3β/CDK chemotype.
  • Assessed selectivity against other kinases, including GSK3β and CDK.

Main Results:

  • Successfully repurposed a GSK3β/CDK inhibitor chemotype.
  • Developed compound 8b, a potent and highly selective inhibitor of DYRK1A.
  • Demonstrated removal of inhibitory activity against GSK3β and CDK through a single methyl group addition.

Conclusions:

  • The presented pipeline enables efficient repurposing of known compounds for selective kinase inhibition.
  • Compound 8b represents a valuable tool for studying DYRK1A biology due to its high selectivity.
  • Targeted chemical modifications can effectively enhance selectivity and repurpose existing drug scaffolds.