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Updated: May 21, 2026

Assessment of Resistance to Tyrosine Kinase Inhibitors by an Interrogation of Signal Transduction Pathways by Antibody Arrays
Published on: September 19, 2018
[Protein tyrosine kinase inhibitors in cancer therapy]
S Boutayeb1, F Z Zakkouri, M Aitelhaj
1Service d'oncologie médicale, institut national d'oncologie, CHU Ibn Sina, Rabat, Maroc. boutayebdr@yahoo.fr
Abstract:
The tyrosine kinase inhibitors (TKI) are small molecules of low molecular weight that inhibit tyrosine kinases, enzymes responsible for the activation of signal transduction cascades. Currently, a number of TKI received approval in various cancers, while others are in clinical development process: TKI are specifically clinically active when they target a tyrosine kinase (TK) with constitutional activity subsequent to a mutation, being then a master-gene driving transformation and tumour progression. Already, this drug-family provides a major therapeutic weapon against cancer.
Insights
Tyrosine kinase inhibitors (TKI) are small molecule drugs that block cancer-driving enzymes. These targeted therapies are effective against various cancers by inhibiting mutated tyrosine kinases involved in tumor progression.
Area of Science:
- Biochemistry
- Pharmacology
- Oncology
Context:
- Tyrosine kinases (TK) are key enzymes in cellular signal transduction.
- Aberrant TK activity, often due to mutations, drives cancer development and progression.
- Small molecule tyrosine kinase inhibitors (TKI) have emerged as a significant therapeutic class.
Purpose:
- To review the role and clinical application of tyrosine kinase inhibitors (TKI) in cancer therapy.
- To highlight the mechanism of action of TKI targeting constitutively active tyrosine kinases.
- To discuss the current landscape of approved and developing TKI treatments for various cancers.
Summary:
- Tyrosine kinase inhibitors (TKI) are low molecular weight drugs that selectively inhibit tyrosine kinases.
- Their efficacy is pronounced when targeting mutated TK that act as master genes in cancer.
- TKI represent a crucial advancement in the oncological armamentarium, with numerous agents approved and in development.
Impact:
- TKI have revolutionized cancer treatment by offering targeted therapies with improved efficacy and reduced toxicity.
- The development of TKI has led to better outcomes for patients with specific genetic alterations in their tumors.
- Ongoing research continues to expand the utility of TKI in combination therapies and for new cancer indications.
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