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Related Concept Videos

Receptor Tyrosine Kinases01:26

Receptor Tyrosine Kinases

21.0K
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...
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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

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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...
654
Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

4.9K
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:
4.9K
Enzyme-linked Receptors01:00

Enzyme-linked Receptors

89.2K
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...
89.2K
Targeted Cancer Therapies02:57

Targeted Cancer Therapies

9.1K
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...
9.1K
Inhibition of Cdk Activity02:34

Inhibition of Cdk Activity

6.2K
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...
6.2K

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Related Experiment Video

Updated: Apr 8, 2026

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

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Discovering the first tyrosine kinase.

Tony Hunter1

  • 1Salk Institute for Biological Studies, La Jolla, CA 92037-1002 hunter@salk.edu.

Proceedings of the National Academy of Sciences of the United States of America
|July 2, 2015
PubMed
Summary

Researchers discovered that tyrosine kinase activity, not threonine, is key to how tumor viruses transform cells. This finding revealed the mechanism behind viral oncogenesis and cancer development.

Area of Science:

  • Molecular Biology
  • Virology
  • Oncology

Background:

  • Animal tumor viruses were investigated as models for human cancer in the mid-20th century.
  • By the mid-1970s, research focused on the molecular mechanisms of viral cell transformation, including viral gene products.

Observation:

  • Prompted by the discovery of threonine kinase activity in Rous sarcoma virus (RSV) v-Src, experiments investigated the polyomavirus middle T-transforming protein.
  • Initial experiments aimed to identify similar kinase activity in the middle T antigen.

Findings:

  • A kinase activity associated with polyomavirus middle T antigen was identified.
  • This activity was found to be specific for tyrosine phosphorylation in vitro.
  • This led to the discovery that the v-Src-associated kinase activity is also specific for tyrosine.

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Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays
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Assessment of Resistance to Tyrosine Kinase Inhibitors by an Interrogation of Signal Transduction Pathways by Antibody Arrays
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Implications:

  • The findings confirmed that v-Src is a tyrosine kinase, transforming cells by phosphorylating proteins on tyrosine.
  • This established tyrosine phosphorylation as a critical mechanism in viral-induced cancer.
  • The rapid discovery highlighted the potential for swift breakthroughs in understanding cancer mechanisms.