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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:
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...
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...
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: Jun 13, 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.

C Natoli1, B Perrucci, F Perrotti

  • 1Department of Oncology and Neurosciences, Foundation University G. d'Annunzio Medical School, Chieti-Pescara, Italy. natoli@unich.it

Current Cancer Drug Targets
|April 14, 2010
PubMed
Summary

First and second-generation tyrosine kinase inhibitors (TKIs) offer oral cancer treatments. This review examines their mechanisms, clinical activity, and resistance development, a key challenge in cancer research.

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Last Updated: Jun 13, 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

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10:49

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

Published on: September 18, 2013

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13:22

Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays

Published on: October 23, 2019

Area of Science:

  • Oncology
  • Pharmacology
  • Molecular Biology

Background:

  • Tyrosine kinase inhibitors (TKIs) represent a significant advancement in cancer therapy.
  • These orally available drugs target critical signaling pathways in various neoplasms.
  • TKIs have gained worldwide approval for treating lung, breast, kidney, pancreatic cancers, GIST, and CML.

Purpose of the Study:

  • To review the most relevant first and second-generation TKIs.
  • To explore their molecular mechanisms of action against receptor and nonreceptor tyrosine kinases.
  • To discuss clinical activity and the challenge of acquired resistance.

Main Methods:

  • Comprehensive literature review of TKIs.
  • Analysis of molecular mechanisms in in vitro and in vivo models.
  • Evaluation of clinical data on efficacy and resistance.

Main Results:

  • First and second-generation TKIs demonstrate significant clinical efficacy across multiple cancer types.
  • Understanding molecular mechanisms is crucial for optimizing TKI therapy.
  • Drug resistance remains a major hurdle, necessitating further research.

Conclusions:

  • TKIs are vital, well-tolerated oral agents for treating diverse cancers.
  • Further research into TKI mechanisms and resistance is essential for improving patient outcomes.