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Updated: Nov 2, 2025

Assessment of Resistance to Tyrosine Kinase Inhibitors by an Interrogation of Signal Transduction Pathways by Antibody Arrays
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Assessment of Resistance to Tyrosine Kinase Inhibitors by an Interrogation of Signal Transduction Pathways by Antibody Arrays

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Tyrosine Kinase ROR1 as a Target for Anti-Cancer Therapies

Yuming Zhao1, Dengyang Zhang1, Yao Guo1

  • 1Edmond H. Fischer Translational Medical Research Laboratory, Scientific Research Center, The Seventh Affiliated Hospital, Sun Yat-Sen University, Shenzhen, China.

Frontiers in Oncology
|June 14, 2021
PubMed

Insights

Receptor tyrosine kinase ROR1 is crucial in development and cancer. This review explores ROR1’s structure, function, and therapeutic strategies, including small molecule inhibitors, for targeting ROR1 in cancer treatment.

Area of Science:

  • Oncology
  • Molecular Biology
  • Biochemistry

Background:

  • Receptor tyrosine kinase ROR1 is vital for embryogenesis.
  • ROR1 overexpression is observed in various malignant tumors, promoting oncogenesis via cell survival pathways like WNT signaling.
  • Antibody-based immunotherapies targeting ROR1 show promise in clinical studies.

Purpose of the Study:

  • To analyze the structural and functional characteristics of ROR1.
  • To discuss therapeutic strategies targeting ROR1, with a focus on small molecule inhibitors.
  • To highlight the underappreciated potential of small molecule inhibitors against ROR1.

Main Methods:

  • Review of existing literature on ROR1 structure and function.
  • Analysis of ROR1's role in oncogenesis and WNT signaling.
  • Evaluation of current and potential therapeutic approaches targeting ROR1.

Main Results:

  • ROR1 possesses intrinsic tyrosine kinase activity, though initially mischaracterized.
  • ROR1's role in activating cell survival signaling pathways is confirmed.
  • Evidence suggests ROR1 is a viable target for both antibody and small molecule therapies.

Conclusions:

  • ROR1 is a significant therapeutic target in oncology.
  • Further research into ROR1's tyrosine kinase activity is warranted.
  • Small molecule inhibitors represent an underutilized therapeutic strategy for ROR1-targeted cancer treatment.
Keywords:
ROR1kinase activitykinase functionsmall molecule inhibitorstargeted therapy

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