Third-generation EGFR and ALK inhibitors: mechanisms of
2022年5月9日 · In this Review, we discuss the development of third-generation EGFR and ALK inhibitors, predominant mechanisms of resistance, and approaches to tackling resistance in the clinic, ranging from...
EGFR in Cancer: Signaling Mechanisms, Drugs, and Acquired Resistance
2021年6月1日 · Paracrine loops comprising tumor and stromal cells enable EGFR to fuel invasion across tissue barriers, survival of clusters of circulating tumor cells, as well as colonization of distant organs. We conclude by listing all clinically approved anti-cancer drugs targeting either EGFR or HER2.
Biochemistry, Epidermal Growth Factor Receptor - StatPearls
2023年12月3日 · The most common resistance mechanism is associated with the secondary mutation (T790M) in the EGFR’s kinase domain. Other resistance mechanisms include amplifying various oncogenes such as MET/HGFR, AXL, HER2, and Ras. [8]
Epidermal growth factor receptor: mechanisms of activation …
2003年3月10日 · We review the structure and function of the EGFR, from ligand binding to the initiation of intracellular signalling pathways that lead to changes in the biochemical state of the cell. The recent crystal structures of different domains from several members of the EGFR family have challenged our concepts of these processes.
Targeting the EGFR signaling pathway in cancer therapy - PMC
In this review, the basic mechanism of EGFR activation and the role of EGFR signaling in cancer progression, has been covered. Furthermore, current developments made towards targeting the EGFR signaling pathway for the treatment of epithelial cancers and a summary of the various anti-EGFR therapeutic agents that are currently in use, has also ...
Quantitative analysis reveals how EGFR activation and ... - Nature
2015年8月12日 · Ubiquitination of the epidermal growth factor receptor (EGFR) that occurs when Cbl and Grb2 bind to three phosphotyrosine residues (pY1045, pY1068 and pY1086) on the receptor...
Epidermal Growth Factor Receptor Cell Proliferation Signaling …
Here, we review the molecular mechanisms that regulate EGFR signal transduction, including the EGFR structure and its mutations, ligand binding and EGFR dimerization, as well as the signaling pathways that lead to G1 cell cycle progression.
Activation of the EGF Receptor by Ligand Binding and Oncogenic ...
In this review, we discuss the mechanisms underlying the ligand-induced activation of the preformed EGFR dimer, as well as how oncogenic mutations constitutively activate the receptor dimer, based on the rotation model.
Molecular mechanisms of epidermal growth factor receptor (EGFR ... - PubMed
2006年12月15日 · The epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases, including EGFR, HER2/erbB2, and HER3/erbB3, is an attractive target for antitumor strategies. Aberrant EGFR signaling is correlated with progression of various malignancies, and somatic tyrosine kinase domain mutations …
Structure–function analysis of oncogenic EGFR Kinase Domain …
2021年3月2日 · We provide computational and experimental evidence that EGFR-KDD functions by forming asymmetric EGF-independent intra-molecular and EGF-dependent inter-molecular dimers. Time-resolved...