The term apoptosis describes the regulated and gradual death of a cell. In contrast to uncontrolled necrosis, apoptosis is limited to one or a few cells and is not accompanied by inflammation. Through apoptosis, the organism can get rid of cells, which are non-functional or which are...
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Receptor tyrosine kinases transmit signals from outside the cell via the membrane into the cytosol. After activation by an external factor, the receptor monomers dimerize and phosphorylate each other’s intracellular domains. Cytosolic proteins bind to the phosphorylated domains and...
The most important family of receptor tyrosine kinases is the family of the receptors for EGF (Epidermal Growth Factor). Activation of the EGF receptor tyrosine kinase by extracellular EGF results in its dimerization and its autophosphorylation on its cytosolic domains. The phosphorylated...
The EGF receptor tyrosine protein kinases and the therapy of tumors with activated EGF receptors – Part 1: Inhibition of receptor activation via antibodies
In many tumors, EGF receptors are over-activated, which leads to a stronger signal and a high rate of proliferation. In order to inhibit the signal and to reduce the rate of proliferation, the EGF receptors can be inhibited by antibodies. Prominent examples are Cetuximab and Trastuzumab...
The EGF receptor tyrosine protein kinases and the therapy of tumors with activated EGF receptors – Part 2: Blocking of EGF receptor signaling via tyrosine kinase inhibitors
Tumors with activated EGF receptors can be treated with drugs that inhibit the kinase activity by binding to intracellular domains. Most of these drugs are ATP analogs that block ATP binding and thus prevent auto- and transphosphorylation by the intracellular receptor domains. Mutations...