RTK class III
RTK class III is a class of receptor tyrosine kinases (RTKs), a type of cell surface receptor that plays a crucial role in cellular processes such as growth, differentiation, metabolism, and survival. RTK class III includes receptors such as platelet-derived growth factor receptor (PDGFR), colony-stimulating factor 1 receptor (CSF1R), and KIT proto-oncogene receptor tyrosine kinase (c-Kit).
Structure
RTK class III receptors are characterized by a unique structure that includes an extracellular ligand-binding domain, a single transmembrane helix, a juxtamembrane domain, a tyrosine kinase domain, and a C-terminal tail. The extracellular domain is responsible for ligand binding, while the intracellular tyrosine kinase domain is responsible for the receptor's enzymatic activity.
Function
Upon ligand binding, RTK class III receptors undergo dimerization, a process that brings two kinase domains into close proximity. This leads to autophosphorylation, which activates the kinase and initiates a cascade of downstream signaling events. These signals are transmitted to the cell's interior, leading to changes in gene expression and cellular behavior.
Role in Disease
Mutations in RTK class III receptors can lead to a variety of diseases. For example, mutations in the c-Kit receptor are associated with gastrointestinal stromal tumors (GISTs), while mutations in the PDGFR are associated with hypereosinophilic syndrome (HES) and other myeloproliferative disorders.
Therapeutic Target
Due to their role in disease, RTK class III receptors are attractive targets for therapeutic intervention. Several drugs that inhibit these receptors, such as imatinib and sunitinib, have been developed and are used in the treatment of cancers and other diseases.
See Also
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Contributors: Prab R. Tumpati, MD