Epidermal Growth Factor Receptor (EGFR) Inhibitors as An Efficient Approach in Cancer Targeted Therapy

The epidermal growth factor receptor (EGFR) is one of the most important and attractive targets of clinical and scientific interest in the treatment of most cancers. It is involved in the development and metastasis of relevant cancers, showing a decisive regulatory role in these pathways.

Introduction of EGFR

The epidermal growth factor receptor (EGFR, also known as ErbB1 or HER-1) belongs to the receptor tyrosine kinase (RTK) superfamily, which consists of other three members, ErbB2/Neu/HER-2, ErbB3/HER-3 and ErbB4/HER-4. EGFR is the human epidermal growth factor receptor, a membrane surface sensor with tyrosine kinase activity, commonly expressed in human epidermal and stromal cells and highly expressed in a variety of human malignant tumors, such as pancreatic cancer, nasopharyngeal carcinoma, head and neck tumors. Clinically, EGFR expression or mutation can be determined by auxiliary tests (immunohistochemistry, genetic testing, etc.).

Fig. 1 Representation of the four ErbB receptors and their ligands.

Relationship Between EGFR Families and Cancer

The EGFR family plays an important role in normal tissue development and function, but when their expression or activity is out of control, it leads to cancer-related phenomena such as excessive cell proliferation, resistance to apoptosis, angiogenesis, invasion and metastasis. Therefore, the EGFR family is considered to be an important factor in cancer development and progression and an important target for cancer therapy.

Uncontrolled expression or activity of the EGFR family can be caused by a variety of reasons, including gene mutations, gene amplification, gene rearrangements, epigenetic alterations, ligand overexpression, and abnormal signaling pathways downstream of the receptor. These causes can act individually or in combination, resulting in sustained activation or enhancement of EGFR family signaling pathways. For example, the EGFR gene is frequently mutated or amplified in non-small cell lung cancer (NSCLC), leading to enhanced tyrosine kinase activity or increased dimerization; the HER2 gene is frequently amplified or rearranged in breast cancer, leading to its overexpression or the formation of heterodimers; the HER3 gene is frequently methylated in colorectal cancer, leading to down-regulation of its expression or loss of function; the HER4 genes are frequently sheared or hydrolyzed in breast cancer, resulting in altered isoform ratios or altered signaling pathway selection.

Deregulation of the EGFR family of signaling pathways can affect a variety of cellular functions that contribute to cancer development and progression. These cellular functions include:

Cell proliferation

EGFR family signaling pathway can activate RAS/RAF/MEK/ERK pathway, which can promote cell cycle progression and DNA synthesis, and increase the rate and number of cell division. At the same time, the EGFR family signaling pathway can also activate the PI3K/AKT/mTOR pathway, thus promoting protein synthesis and metabolism, and providing energy and materials for cell growth. In addition, the EGFR family signaling pathway can also activate the JAK/STAT pathway, thus promoting the expression of some genes that promote cell proliferation, such as CYCLIN D1, MYC, BCL-XL, etc.

Anti-apoptosis

EGFR family signaling pathway can inhibit some signals or molecules that induce apoptosis, such as P53, BAX, BAD and so on. Meanwhile, EGFR family signaling pathway can also activate some signals or molecules that inhibit apoptosis, such as BCL-2, BCL-XL, XIAP, etc. In addition, EGFR family signaling pathways can also affect some pathways that mediate apoptosis, such as the mitochondrial pathway, death receptor pathway and so on.

Angiogenesis

EGFR family signaling pathway can promote the proliferation, migration and differentiation of vascular endothelial cells, thus promoting the formation of new blood vessels. Meanwhile, EGFR family signaling pathways can also promote the expression or release of some factors that promote angiogenesis, such as VEGF, FGF, PDGF, etc. In addition, EGFR family signaling pathways can also affect some pathways or mechanisms that regulate angiogenesis, such as HIF-1α, NO, MMP, etc.

Invasion and metastasis

The EGFR family signaling pathway can promote the reduction of adhesion and adhesion of cancer cells to the surrounding stroma or neighboring cells, thereby promoting the detachment and freeing of cancer cells. At the same time, the EGFR family signaling pathway can also promote the enhancement of degradation and penetration of cancer cells to the surrounding stroma or neighboring cells, thus promoting the invasion and traversal of cancer cells. In addition, the EGFR family signaling pathway can also promote the expression or release of some factors that promote invasion and metastasis, such as MMP, uPA, CXCR4 and so on.

EGFR-Related Products & Applications

Creative Biogene provides a comprehensive range of products related to EGFR targets, such as transfected stable cell lines, preformed viral particles, and cell lysates. Our high-quality EGFR product line assists customers in advancing their research on related diseases, drug discovery, and other endeavors.

Transfected stable cell lines

We offer stable cell lines genetically modified to express EGFR or its variants. These cell lines provide consistent and reliable models for studying EGFR-related functions, signaling pathways, and drug responses.

Cat.No.	Product Name	Price
CSC-DC004772	Panoply™ Human EGFR Knockdown Stable Cell Line	Inquiry
CSC-RO0126	Human EGFR Stable Cell Line-Ba/F3	Inquiry
CSC-RO0127	Human EGFR-C797S Stable Cell Line-Ba/F3	Inquiry
CSC-RO0128	Human EGFR-D770_N771insSVD Stable Cell Line-Ba/F3	Inquiry
CSC-RO0129	Human EGFR-DEL19 Stable Cell Line-Ba/F3	Inquiry
CSC-RO0130	Human EGFR-DEL19/C797S Stable Cell Line-Ba/F3	Inquiry
CSC-RO0131	Human EGFR-DEL19/T790M Stable Cell Line-Ba/F3	Inquiry
CSC-RO0132	Human EGFR-DEL19/T790M/C797S Stable Cell Line-Ba/F3	Inquiry
CSC-RO0133	Human EGFR-G719S Stable Cell Line-Ba/F3	Inquiry
CSC-RO0134	Human EGFR-G719S/T263P Stable Cell Line-Ba/F3	Inquiry
CSC-RO0135	Human EGFR-H773_V774insNPH Stable Cell Line-Ba/F3	Inquiry
CSC-RO0136	Human EGFR-L858R Stable Cell Line-Ba/F3	Inquiry
CSC-RO0137	Human EGFR-L858R/C797S Stable Cell Line-Ba/F3	Inquiry
CSC-RO0138	Human EGFR-L858R/T790M Stable Cell Line-Ba/F3	Inquiry
CSC-RO0139	Human EGFR-L858R/T790M/C797S Stable Cell Line-Ba/F3	Inquiry
CSC-RO0140	Human EGFR-L861Q Stable Cell Line-Ba/F3	Inquiry

View more of our transfected stable cell line products.

Preformed viral particles

We offer high quality pre-made viral particle products related to EGFR targets. These viral particles can be used to efficiently deliver EGFR-related genetic material into target cells for functional studies or knockdown experiments.

Cat.No.	Product Name	Price
AD00085Z	Human EGFR adenoviral particles	Inquiry
AD00159Z	Human EGFR adenoviral particles	Inquiry
AD05317Z	Human EGFR adenoviral particles	Inquiry
LV00265Z	Mouse Egfr lentiviral particles	Inquiry
LV00266Z	Human EGFR lentiviral particles	Inquiry
LV00267Z	Human EGFR lentiviral particles	Inquiry
LVG00031Z	scFv(EGFR)-CD3zeta CAR-T Lentivirus	Inquiry
LVG00032Z	scFv(EGFR)-41BB-CD3zeta CAR-T Lentivirus	Inquiry
LVG00033Z	scFv(EGFR)-CD28-CD3zeta CAR-T Lentivirus	Inquiry
LVG00034Z	scFv(EGFR)-OX40-CD3zeta CAR-T Lentivirus	Inquiry
LVG00035Z	scFv(EGFR)-CD28-41BB-CD3zeta CAR-T Lentivirus	Inquiry
LVG00036Z	scFv(EGFR)-CD28-OX40-CD3zeta CAR-T Lentivirus	Inquiry

Cell lysates

Our EGFR cell lysates provide a valuable resource for studying the protein expression, post-translational modifications, and protein-protein interactions involving EGFR. These lysates are derived from cells expressing EGFR, enabling researchers to investigate EGFR-related mechanisms and protein interactions using techniques such as Western blotting, immunoprecipitation, or enzyme activity assays.

Cat.No.	Product Name	Price
CLKO-1660	EGFR KO Cell Lysate-HeLa	Inquiry
CLOE-1813	Human EGFR Insect Cell Lysate	Inquiry
CLOE-1814	Human EGFR HEK293 Cell Lysate	Inquiry
CLOE-1815	Human EGFR(His) Insect Cell Lysate	Inquiry
CLOE-1816	Human EGFR(Fc) HEK293 Cell Lysate	Inquiry
CLOE-2140	Rat Egfr (His) HEK293 Cell Lysate	Inquiry
CLOE-2307	Mouse Egfr HEK293 Cell Lysate	Inquiry
CLOE-2308	Mouse Egfr(Fc) HEK293 Cell Lysate	Inquiry

Reference:

Romano, R.; et al. Role of EGFR in the Nervous System. Cells. 2020, 9(8): 1887.

* For research use only. Not intended for any clinical use.

Quick Inquiry