activation of transmembrane receptor protein tyrosine kinase activity

Definition

Target type: biologicalprocess

Any process that initiates the activity of the inactive transmembrane receptor protein tyrosine kinase activity. [GOC:dph, GOC:tb]

Transmembrane receptor protein tyrosine kinase (RTK) activation is a complex process involving a cascade of events that ultimately lead to signal transduction within the cell. Here's a detailed description of the biological process:

1. **Ligand Binding:** The process begins with the binding of a specific ligand to the extracellular domain of the RTK. This binding event triggers a conformational change in the receptor, bringing its intracellular tyrosine kinase domains closer together.

2. **Dimerization and Autophosphorylation:** The conformational change facilitates the dimerization of the RTK, where two receptor molecules associate with each other. This dimerization brings the intracellular tyrosine kinase domains into close proximity, allowing them to phosphorylate each other on specific tyrosine residues. This process, known as autophosphorylation, is crucial for activating the RTK.

3. **Recruitment of Adaptor Proteins:** The phosphorylated tyrosine residues on the activated RTK serve as docking sites for various adaptor proteins. These adaptor proteins, such as growth factor receptor-bound protein 2 (GRB2) and Src homology 2 domain-containing protein (SHC), contain specific domains that recognize and bind to the phosphorylated tyrosines.

4. **Activation of Downstream Signaling Pathways:** The adaptor proteins, once bound to the activated RTK, initiate a cascade of downstream signaling events. This can involve the activation of various signaling pathways, including the Ras-MAPK pathway, the PI3K-AKT pathway, and the PLCγ pathway.

5. **Signal Transduction and Cellular Responses:** The activated signaling pathways ultimately lead to various cellular responses, such as cell proliferation, differentiation, survival, and migration. These responses are mediated by the downstream targets of the activated pathways, including transcription factors, kinases, and other proteins involved in cellular processes.

Overall, the activation of transmembrane receptor protein tyrosine kinases is a highly regulated process that involves a series of steps, starting with ligand binding and culminating in the activation of downstream signaling pathways. These pathways then orchestrate diverse cellular responses, playing a crucial role in various physiological processes.'
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Proteins (2)

Compounds (148)