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Related Concept Videos

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...
Treatment for Pulmonary Arterial Hypertension: Receptor Tyrosine Kinase Inhibitors and Calcium Channel Blockers01:26

Treatment for Pulmonary Arterial Hypertension: Receptor Tyrosine Kinase Inhibitors and Calcium Channel Blockers

Receptor tyrosine kinase inhibitors (TKIs) and calcium channel blockers (CCBs) are two critical categories of drugs employed in the treatment of pulmonary artery hypertension (PAH). PAH is a disease that causes high blood pressure in the pulmonary arteries, resulting in chest pain, fatigue, and shortness of breath.
TKIs, such as imatinib (Gleevec), are particularly effective in tackling the growth and mitogenic factors that become upregulated in PAH patients. These factors contribute to the...
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...
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...
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...

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Related Experiment Video

Updated: Jun 23, 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

[Imatinib].

Hideto Kameda1

  • 1Department of Rheumatology/Clinical Immunology, Saitama Medical Center, Saitama Medical University.

Nihon Rinsho Men'Eki Gakkai Kaishi = Japanese Journal of Clinical Immunology
|May 1, 2009
PubMed
Summary
This summary is machine-generated.

Imatinib, a small molecule tyrosine kinase inhibitor, shows promise in treating fibrotic and immune-mediated diseases like systemic sclerosis. Its dual inhibition of PDGF and TGF-β signaling offers a potential new therapeutic avenue.

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Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays
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Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays

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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

Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays
13:22

Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays

Published on: October 23, 2019

Area of Science:

  • Molecular biology
  • Immunology
  • Pharmacology

Context:

  • Molecular targeting therapies are advancing, with small molecule inhibitors gaining traction.
  • Imatinib, a tyrosine kinase inhibitor, targets platelet-derived growth factor (PDGF) and c-Abl.
  • Current treatments for fibrotic lesions are limited.

Purpose:

  • To review the progress and potential of small molecule tyrosine kinase inhibitors, specifically imatinib.
  • To highlight imatinib's efficacy in preclinical models of fibrotic and immune-mediated diseases.
  • To discuss the potential of imatinib as a therapeutic agent against fibrosis.

Summary:

  • Imatinib effectively inhibited PDGF-induced fibroblastic cell proliferation in vitro.
  • Preclinical studies demonstrated imatinib's efficacy in animal models of arthritis, pneumonia, glomerulonephritis, and pulmonary hypertension.
  • Clinical efficacy in systemic sclerosis patients is emerging, positioning imatinib as a potential anti-fibrotic drug.

Impact:

  • Imatinib's dual inhibition of PDGF and transforming growth factor beta (TGF-β) signaling suggests potent anti-fibrotic activity.
  • Further investigation into imatinib's efficacy and safety in fibrotic and immune-mediated diseases is ongoing globally.
  • This research could lead to novel treatments for conditions with significant unmet needs.