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Related Concept Videos

Receptor Tyrosine Kinases01:26

Receptor Tyrosine Kinases

Receptor tyrosine kinases or RTKs are membrane-bound receptors that phosphorylate specific tyrosine on protein substrates. RTKs regulate cellular growth, differentiation, survival, and migration. They contain an extracellular ligand binding domain, a transmembrane domain, and a cytosolic tail with intrinsic kinase activity. Several extracellular signaling molecules activate RTKs in one or more ways and relay the signal downstream. Ligands such as platelet-derived growth factor (PDGF) or...
Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:
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...
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...
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...
Enzyme-linked Receptors01:00

Enzyme-linked Receptors

Enzyme-linked receptors are proteins that act as both receptor and enzyme, activating multiple intracellular signals. This is a large group of receptors that include the receptor tyrosine kinase (RTK) family. Many growth factors and hormones bind to and activate the RTKs.
Neurotrophin (NT) receptors are a family of RTKs, including trkA, trkB, and trkC (tropomyosin-related kinase) receptors. TrkA is specific for nerve growth factor (NGF), neurotrophin-6, and neurotrophin-7. TrkB binds...

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Related Experiment Video

Updated: May 28, 2026

Assessment of Resistance to Tyrosine Kinase Inhibitors by an Interrogation of Signal Transduction Pathways by Antibody Arrays
07:42

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

Published on: September 19, 2018

[Tyrosine kinase inhibitors].

Jacques Robert1

  • 1Université Bordeaux-Segalen, Institut Bergonié, Bordeaux Cedex, France. robert@bergonie.org

Bulletin Du Cancer
|October 26, 2011
PubMed
Summary

Tyrosine kinase inhibitors are crucial in oncology, targeting specific receptors like EGFR and PDGFR. Ongoing research synthesizes new compounds, optimizing interactions for improved cancer therapies.

Area of Science:

  • Oncology
  • Pharmacology
  • Biochemistry

Background:

  • Tyrosine kinases are key targets in cancer therapy.
  • Anilino-quinazoline scaffolds are foundational for synthesizing kinase inhibitors.
  • Kinase crystallography aids in optimizing drug-target interactions.

Purpose of the Study:

  • To review the development and specificity of tyrosine kinase inhibitors.
  • To highlight key inhibitors targeting specific receptors like EGFR, PDGFR, KIT, and VEGF.
  • To discuss formulation, compliance, and future directions in tyrosine kinase inhibitor research.

Main Methods:

  • Structure-based drug design utilizing tyrosine kinase crystallography.
  • Synthesis of novel anilino-quinazoline derivatives.

More Related Videos

Pre-clinical Evaluation of Tyrosine Kinase Inhibitors for Treatment of Acute Leukemia
10:49

Pre-clinical Evaluation of Tyrosine Kinase Inhibitors for Treatment of Acute Leukemia

Published on: September 18, 2013

Related Experiment Videos

Last Updated: May 28, 2026

Assessment of Resistance to Tyrosine Kinase Inhibitors by an Interrogation of Signal Transduction Pathways by Antibody Arrays
07:42

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

Published on: September 19, 2018

Pre-clinical Evaluation of Tyrosine Kinase Inhibitors for Treatment of Acute Leukemia
10:49

Pre-clinical Evaluation of Tyrosine Kinase Inhibitors for Treatment of Acute Leukemia

Published on: September 18, 2013

  • Pharmacokinetic monitoring for oral formulations.

    • Main Results:

    • Development of specific inhibitors for EGFR (e.g., gefitinib, erlotinib).
    • Identification of inhibitors targeting PDGFR and KIT (e.g., imatinib, nilotinib).
    • Discovery of inhibitors targeting VEGF receptors for angiogenesis (e.g., sunitinib, sorafenib).

    Conclusions:

    • Tyrosine kinase inhibitors represent a rapidly expanding class of targeted cancer therapies.
    • Achieving high specificity remains a challenge due to conserved kinase structures.
    • Oral formulations are patient-friendly but may require pharmacokinetic monitoring.