Related Experiment Video
Updated: Aug 9, 2026

10:49
Pre-clinical Evaluation of Tyrosine Kinase Inhibitors for Treatment of Acute Leukemia
Published on: September 19, 2013
Receptor tyrosine kinases and their targets
1Department of Pediatrics, National Jewish Center for Immunology and Respiratory Medicine, Denver, Colorado 80206.
Current Opinion in Genetics & Development
|February 1, 1994
Summary
Higher eukaryotes use cell surface receptor tyrosine kinases to receive environmental signals. These proteins facilitate intracellular signal relay through autophosphorylation, enabling the binding of key signaling enzymes.
Area of Science:
- Molecular Biology
- Cell Signaling
- Biochemistry
Background:
- Higher eukaryotes utilize cell surface receptor tyrosine kinases (RTKs) for environmental communication.
- RTKs are transmembrane proteins featuring extracellular growth factor binding domains and intracellular tyrosine kinase domains.
- These receptors play a crucial role in transmitting external stimuli into cellular responses.
Purpose of the Study:
- To review recent advances in understanding receptor tyrosine kinase signaling.
- To elucidate the mechanisms by which RTKs mediate intracellular signal transduction.
- To highlight the role of RTKs in cellular communication and response.
Main Methods:
- Review of current scientific literature on receptor tyrosine kinases.
- Analysis of molecular mechanisms involved in RTK activation and signaling.
- Summary of recent findings on SH2 domain-containing protein interactions.
Main Results:
- Receptor tyrosine kinases initiate signaling cascades upon growth factor binding.
- Receptor autophosphorylation is a critical step enabling downstream signaling.
- Phosphorylated RTKs serve as docking sites for SH2 domain-containing signal transduction enzymes.
Conclusions:
- Receptor tyrosine kinases are essential mediators of environmental signals in higher eukaryotes.
- Autophosphorylation and subsequent protein-protein interactions are key to RTK signal relay.
- Recent advances provide deeper insights into the complex signaling networks regulated by RTKs.
Related Concept Videos
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...
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...
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...
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...
Receptor Downregulation in MVBs
Multivesicular bodies (MVBs) are mature endosomes that sort ubiquitinated proteins and then fuse with lysosomes to degrade the sorted proteins. Epidermal growth factor (EGF) and its receptor (EGFR) form a complex that can be internalized through endocytosis, sorted into an MVB, and later degraded.
The EGFR can initiate signaling pathways that lead to cell proliferation, migration, and differentiation. Overexpression of EGFR stimulates cells to proliferate. Excessive EGFR activation may...
The EGFR can initiate signaling pathways that lead to cell proliferation, migration, and differentiation. Overexpression of EGFR stimulates cells to proliferate. Excessive EGFR activation may...
Amplifying Signals via Enzymatic Cascade
When a ligand binds to a cell-surface receptor, the receptor's intracellular domain changes shape, which may either activate its enzyme function or allow its binding to other molecules. The initial signal is amplified by most signal transduction pathways. This means that a single ligand molecule can activate multiple molecules of a downstream target. Proteins that relay a signal are most commonly phosphorylated at one or more sites, activating or inactivating the protein. Kinases catalyze the...
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 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:
Major types that are helpful drug targets include:

