Table of Contents
What does ErbB1 stand for?
Drugs that block ErbB1 proteins are being used in the treatment of some types of cancer. ErbB1s are a type of receptor tyrosine kinase. Also called EGFR, epidermal growth factor receptor, and HER1.
What do ErbB receptors do?
The ERBB receptors are a group of receptor tyrosine kinases (RTKs) involved in key cellular functions, including cell growth and survival. They signal through phosphorylated tyrosines on their intracellular domains. Activation of these receptors leads to this phosphorylation and to subsequent intracellular signaling.
How is ErbB2 activated?
The EGF receptor, ErbB3, and ErbB4 are activated through the binding of a family of homologous ligands (4). Unique among the ErbB receptors, ErbB2 has no known ligand (5, 6). Binding of an ErbB ligand to its receptor induces dimerization of the receptor through interaction of the extracellular domains.
How is ErbB3 activated?
However, once its ligand, heregulin (HRG) (also called neuregulin (NRG)) binds to erbB3, it can recruit another erbB receptor to form hetero-dimers, which leads to activation of the erbB3 receptor. ErbB3 is a more potent partner than other family members for the oncogenic activity of erbB2 [16, 27–29].
Is ErbB same as EGFR?
The ErbB family of proteins contains four receptor tyrosine kinases, structurally related to the epidermal growth factor receptor (EGFR), its first discovered member. In humans, the family includes Her1 (EGFR, ErbB1), Her2 (Neu, ErbB2), Her3 (ErbB3), and Her4 (ErbB4).
How is the EGF receptor activated?
The receptor is activated by the binding of various ligands including epidermal growth factor (EGF), transforming growth factor α (TGFα), amphiregulin (AREG), epigen, β-cellulin, heparin-binding EGF (HB-EGF), and epiregulin [6,7].
How do tyrosine kinase inhibitors work in EGFR?
First-generation EGFR TKIs The working mechanism of first-generation EGFR-TKIs is to block the activation of downstream signaling induced by EGFR through binding to the ATP-binding sites.
What is ErbB signaling?
The ErbB receptors signal through Akt, MAPK, and many other pathways to regulate cell proliferation, migration, differentiation, apoptosis, and cell motility. ErbB family members and some of their ligands are often over-expressed, amplified, or mutated in many forms of cancer, making them important therapeutic targets.
Is HER2 and ERBB2 same?
The HER2 is the legacy gene symbol for ERBB2 and may be more commonly used by the community; HER2 is also commonly used to describe the protein encoded by the ERBB2 gene. One unique feature of HER2 compared with the other receptors in the HER family is the absence of a known ligand.
What is ERBB2 positive?
Cancers that may be c-erbB-2 positive include breast, bladder, pancreatic, ovarian, and stomach cancers. Also called HER2 positive and human epidermal growth factor receptor 2 positive.