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Updated: Sep 21, 2025

A Method for Screening and Validation of Resistant Mutations Against Kinase Inhibitors
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Targeting protein kinases benefits cancer immunotherapy

Zhengkun Zhang1, Lang Bu2, Junhang Luo3

  • 1Department of Urology, the First Affiliated Hospital, Sun Yat-sen University, Guangzhou, Guangdong 510080, China; Institute of Precision Medicine, the First Affiliated Hospital, Sun Yat-sen University, Guangzhou, Guangdong 510080, China.

Biochimica Et Biophysica Acta. Reviews on Cancer
|June 6, 2022
PubMed

Insights

Combining kinase inhibitors with immune checkpoint inhibitors (ICIs) shows promise for cancer therapy. This approach targets drug resistance and enhances anti-tumor immunity by modulating the tumor microenvironment.

Area of Science:

  • Oncology
  • Immunology
  • Pharmacology

Background:

  • Small-molecule kinase inhibitors are established cancer therapies.
  • Drug resistance limits the clinical efficacy of kinase inhibitors.
  • Immune checkpoint inhibitors (ICIs) have revolutionized cancer treatment.

Purpose of the Study:

  • To summarize the role of protein kinases in immune checkpoint regulation.
  • To explore the combination of kinase inhibitors and ICIs for cancer therapy.
  • To highlight strategies for improving cancer immunotherapy.

Main Methods:

  • Comprehensive review of scientific literature.
  • Analysis of clinical trial data for combined therapies.
  • Evaluation of kinase roles in immune modulation and tumor microenvironment.

Main Results:

  • Protein kinases significantly influence immune checkpoints on tumor and immune cells.
  • Combined kinase inhibitor and ICI therapy demonstrates promising clinical outcomes across various cancers.
  • This combination strategy can evoke innate immune responses and enhance neoantigen presentation.

Conclusions:

  • Kinase inhibitors can overcome resistance to immunotherapy.
  • Targeting protein kinases enhances the efficacy of immune checkpoint inhibitors.
  • Combined therapies offer a promising strategy to improve cancer treatment outcomes.
Keywords:
Immune checkpointKinase inhibitorPhosphorylationProtein kinasecancer immunotherapy

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