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Small-Molecule Targeted Therapies
Published in David E. Thurston, Ilona Pysz, Chemistry and Pharmacology of Anticancer Drugs, 2021
EGFR, also known as ErbB-1, is one of a sub-family of closely related receptors that includes HER2/neu (ErbB-2), HER3 (ErbB-3), and HER4 (ErbB-4). Up-regulated EGFR-mediated signaling can move cells into a continuous and uncontrolled state of division, thus leading to greater numbers of malignant cells and an increase in tumor size (Figure 6.22).Schematic diagram of the EGFR/HER2 signaling pathway.
Markers of Sensitivity and Resistance to EGFR Inhibitors in Colorectal Cancer
Published in Sherry X. Yang, Janet E. Dancey, Handbook of Therapeutic Biomarkers in Cancer, 2021
Jose G. Monzon, Janet E. Dancey
There are several ways to detect EGFR protein expression, including immunohistochemistry, enzyme-link immunosorbent assay (ELISA), and western blotting [124]. By far, the most commonly used test for EGFR protein expression is IHC. The process of IHC staining exploits the specific interaction between an antibody and a particular antigen. Fixed cells are exposed to, in this case, an anti-EGFR antibody. Visualizing the antibody-antigen interaction can be accomplished in a number of ways, but most commonly an antibody is conjugated to an enzyme that can catalyze a color-producing reaction. The staining results are measured semi-quantitatively on a scale of 0, 1+, 2+, and 3+. The score is based on staining intensity and percentage of tumor cells stained.
Lung Cancer
Published in Pat Price, Karol Sikora, Treatment of Cancer, 2020
EGFR is a member of the human epidermal growth factor receptor 2 (HER2) family of transmembrane receptors and is overexpressed in the majority of lung cancers. EGFR-activating mutations are observed in approximately 15% to 20% of patients with non-small-cell lung cancer.
Nordic 2023 guidelines for the diagnosis and treatment of lung neuroendocrine neoplasms
Published in Acta Oncologica, 2023
Gitte Dam, Henning Grønbæk, Anna Sundlöv, Johan Botling, Anders Sundin, Rene Horsleben Petersen, Staffan Welin, Espen-Thiis Evensen, Halfdan Sorbye, Elizaveta Tabaksblat, Anne Kirstine Arveschoug, Jann Mortensen, Andreas Kjaer, Ulrich Knigge, Eva Tiensuu Janson, Seppo W. Langer
Sequencing-based molecular profiling may identify patients that will benefit from novel targeted therapies. At least one alteration potentially targetable by investigational agents was present in two-thirds of LCNEC. EGFR mutations are rare but may be seen more frequently in peripheral tumors and in tumors with combined histology. ALK, ROS1, BRAF, RET, FGFR1 or ERBB2 alterations are sometimes detected, as are mutations influencing the PI3K/AKT/mTOR pathway [47–51]. Response to immune checkpoint inhibitors has been reported only casuistically [52,53]. Studies of immunotherapy in clinical trials are warranted. Furthermore, DLL-3 has recently been identified as a compelling therapeutic target and is currently under clinical investigation, both with antibody-drug conjugates and T-cell-engaging antibodies.
2-Arylquinolines as novel anticancer agents with dual EGFR/FAK kinase inhibitory activity: synthesis, biological evaluation, and molecular modelling insights
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2022
Mostafa M. Elbadawi, Wagdy M. Eldehna, Amer Ali Abd El-Hafeez, Warda R. Somaa, Amgad Albohy, Sara T. Al-Rashood, Keli K. Agama, Eslam B. Elkaeed, Pradipta Ghosh, Yves Pommier, Manabu Abe
Epidermal growth factor receptor (EGFR) is a member of tyrosine kinase family in which the endogenous ligand binds to the extracellular domain leading to conformational changes and dimerisation of EGFR resulting in its activation which subsequently stimulates its intrinsic intracellular protein-tyrosine kinase activity10. EGFR is over-expressed in many solid tumours and is related to cancer cell proliferation, angiogenesis and metastasis, so it has a critical role in cancer growth. Therefore, EGFR has been validated as an efficient target for anticancer drug discovery. In the last two decades, different 4-anilinoquinazoline-based EFGR inhibitors, such as Gefitinib, Erlotinib, Afatinib, and Dacomitinib (Figure 1), have been FDA-approved for clinical use in treatment of non-small cell lung cancer11,12.
Design, synthesis and biological evaluation of a series of dianilinopyrimidines as EGFR inhibitors
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2022
Longjia Yan, Qin Wang, Li Liu, Yi Le
EGFR is a receptor for an epithelial growth factor (EGF) cell proliferation and signal transduction11. It belongs to a family of ErbB receptors, which includes EGFR (HER1 or ErbB-1), HER2 (ErbB-2), HER3 (ErbB-3) and HER4 (ErbB-4). EGFR plays an essential role in regulating cell growth, proliferation and differentiation and other physiological activities of various cancer cells, which is an important target for anti-cancer drug research12–14. As shown in Figure 1, lots of EGFR inhibitors such as Gefitinib, Afatinib, and Osimertinib have been approved in the market, which significantly improves the clinical treatment of NSCLC patients15–17. However, with the continuously emerging resistance of EGFR inhibitors, the development of new EGFR inhibitors has become a hot topic in drug discovery18–20.