Related Experiment Video

Updated: Aug 19, 2026

A Method for Screening and Validation of Resistant Mutations Against Kinase Inhibitors
12:40

A Method for Screening and Validation of Resistant Mutations Against Kinase Inhibitors

Published on: December 7, 2014

Cancer treatment with kinase inhibitors: what have we learnt from imatinib?

D M Ross1, T P Hughes

  • 1Division of Haematology, Institute of Medical and Veterinary Science, PO Box 14 Rundle Mall, Adelaide SA 5000, Australia.

British Journal of Cancer
|January 8, 2004
PubMed

Insights

Targeted anticancer drugs like imatinib mesylate show promise but face resistance. Identifying oncogenic kinase targets and monitoring patient response are crucial for effective cancer therapy.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Development of targeted anticancer drugs focusing on oncogenic kinases.
  • Imatinib mesylate as a leading example, targeting ABL, KIT, and PDGFR.
  • Significant efficacy in chronic myeloid leukemia (CML) but challenges with drug resistance.

Purpose of the Study:

  • To present principles of kinase inhibition based on imatinib's success in CML.
  • To discuss broader applicability in targeted anticancer therapy.
  • To highlight the importance of target identification and response monitoring.

Main Methods:

  • Review of imatinib mesylate's clinical data and mechanism of action.
  • Analysis of resistance mechanisms in chronic myeloid leukemia.
  • Extrapolation of principles for general kinase inhibitor therapy.

Main Results:

  • Imatinib mesylate demonstrates high effectiveness against specific leukemias.
  • Drug resistance is a significant limitation to long-term treatment success.
  • Kinase inhibition principles derived from imatinib experience offer insights.

Conclusions:

  • Optimizing targeted anticancer therapy requires careful selection of activated kinase targets.
  • Continuous monitoring of treatment response is essential to detect and manage emerging resistance.
  • These principles can guide the development and application of future kinase inhibitors.

More Related Videos

Assessment of Resistance to Tyrosine Kinase Inhibitors by an Interrogation of Signal Transduction Pathways by Antibody Arrays07:42

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

Published on: September 19, 2018

Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays13:22

Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays

Published on: October 23, 2019

Related Concept Videos

Inhibition of Cdk Activity02:34

Inhibition of Cdk Activity

The orderly progression of the cell cycle depends on the activation of Cdk protein by binding to its cyclin partner. However, the cell cycle must be restricted when undergoing abnormal changes. Most cancers correlate to the deregulated cell cycle, and since Cdks are a central component of the cell cycle, Cdk inhibitors are extensively studied to develop anticancer agents. For instance, cyclin D associates with several Cdks, such as Cdk 4/6, to form an active complex. The cyclin D-Cdk4/6 complex...
M-Cdk Drives Transition Into Mitosis02:15

M-Cdk Drives Transition Into Mitosis

Checkpoints throughout the cell cycle serve as safeguards and gatekeepers, allowing the cell cycle to progress in favorable conditions and slow or halt it in problematic ones. This regulation is known as the cell cycle control system.
Cyclin-dependent kinases, or Cdks, work in concert with cyclins to control cell cycle transitions. M-Cdk, a complex of Cdk1 bound to M cyclin, is a well-known example of this coordinated control that drives the transition from the G2 to the M phase.
M cyclin...
Mitogens and the Cell Cycle02:38

Mitogens and the Cell Cycle

Mitogens and their receptors play a crucial role in controlling the progression of the cell cycle. However, the loss of mitogenic control over cell division leads to tumor formation. Therefore, mitogens and mitogen receptors play an important role in cancer research. For instance, the epidermal growth factor (EGF) - a type of mitogen and its transmembrane receptor (EGFR), decides the fate of the cell's proliferation. When EGF binds to EGFR, a member of the ErbB family of tyrosine kinase...
Targeted Cancer Therapies02:57

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against specific...
Combination Therapies and Personalized Medicine02:50

Combination Therapies and Personalized Medicine

Combining two or more treatment methods increases the life span of cancer patients while reducing damage to vital organs or tissue from the overuse of a single treatment. Combination therapy also targets different cancer-inducing pathways, thus reducing the chances of developing resistance to treatment.
The combination of the drug acetazolamide and sulforaphane is a good example of combination therapy to treat cancer. The cells in the interior of a large tumor often die due to the hypoxic and...
Targeted Cancer Therapies02:57

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against specific...