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Related Experiment Video

Updated: May 14, 2025

Assessment of Resistance to Tyrosine Kinase Inhibitors by an Interrogation of Signal Transduction Pathways by Antibody Arrays
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Discovery of Novel TYRO3/MERTK Dual Inhibitors.

Deyu Kong1, Jichen Zhao1, Daowei Huang1

  • 1Center for Integrative Chemical Biology and Drug Discovery, Division of Chemical Biology and Medicinal Chemistry, Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599, United States.

Journal of Medicinal Chemistry
|April 11, 2025
PubMed
Summary
This summary is machine-generated.

Researchers discovered UNC9435, the first potent dual inhibitor targeting TYRO3 and MERTK receptor tyrosine kinases. This new compound shows promise for treating cancers reliant on these specific oncogenic pathways.

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Area of Science:

  • Biochemistry
  • Molecular Biology
  • Oncology

Background:

  • The TAM receptor tyrosine kinase family (TYRO3, AXL, MERTK) plays critical roles in oncogenesis and innate immunity.
  • Differential expression and function of TAM family members necessitate context-specific therapeutic strategies.
  • Targeting coordinated TYRO3 and MERTK action may offer therapeutic advantages in certain diseases and tumors.

Purpose of the Study:

  • To discover and characterize the first potent dual inhibitor of TYRO3 and MERTK.
  • To evaluate the selectivity and efficacy of the novel inhibitor against cancer-relevant targets and pathways.

Main Methods:

  • Discovery of UNC9435, a novel small molecule inhibitor.
  • Biochemical assays (NanoBRET) to determine enzyme inhibition and selectivity.
  • Cell-based assays to assess inhibition of downstream signaling and cellular effects (colony formation).

Main Results:

  • UNC9435 is the first identified potent dual inhibitor of TYRO3 and MERTK.
  • The compound exhibits high selectivity for MERTK over AXL and FLT3, and broad selectivity against other kinases.
  • UNC9435 effectively inhibits TYRO3 and MERTK signaling in cancer cells and reduces non-small cell lung cancer colony formation.

Conclusions:

  • UNC9435 represents a promising novel therapeutic candidate for cancers dependent on TYRO3 and MERTK signaling.
  • The dual inhibition strategy targeting TYRO3 and MERTK warrants further investigation for cancer treatment.