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EGFR-Directed ADCs for Cancer Treatment
EP39479
Poster Title: EGFR-Directed ADCs for Cancer Treatment
Submitted on 03 Nov 2022
Author(s): Sonia Li
Affiliations: Biopharma PEG Scientific Inc.
Poster Views: 78
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Poster Information
Abstract: Up to now, there are more than 400 antibody-drug conjugates (ADC) in the development stage (including 14 drugs that have been marketed), with more than 150 publicly disclosed targets covering solid tumors and hematological tumors. Among them, the most popular targets is HER2, followed by CLDN18.2, EGFR and TROP2. Here, let's briefly analyze EGFR-directed ADCs.

Epidermal growth factor receptor (EGFR) belongs to the ERBB protein family, also known as ERBB1, which is the classical cell membrane surface tyrosine kinase receptor, and HER2 is also a member of this family.

The EGFR is comprised of an extracellular EGF-binding domain, a short transmembrane sequence, and a cytoplasmic region that incorporates a protein tyrosine kinase domain and a C-terminal phosphorylation domain. Upon ligand binding to EGFR, EGFR can exert its kinase activity to activate phosphorylation modifications on ligand tyrosine residues, which will further activate downstream signaling pathways to perform corresponding physiological functions. It can be said that EGFR is a signal transceiver of cells, which can receive growth signals and further amplify them to the following effector pathways, such as PI3K-AKT pathway, to regulate cell growth, proliferation, migration and other physiological processes.

egfr-structure
Figure 1. Structure of EGFR, sourxe: reference [1]

EGFR plays an important role in the cell cycle and is associated with cell growth, proliferation, and migration. Its coding gene is a proto-oncogene, which is not expressed or only limitedly expressed in the physiological state and is not oncogenic. Mutations in the gene encoding this receptor will result in the production of excess EGFR, which enhances cell signaling and predisposes to tumorigenesis. Excessive activation of EGFR is associated with key processes in tumor growth and grading, including proliferation, angiogenesis, infiltration, and metastasis. According to the American Society of Clinical Oncology (ASCO), EGFR mutations account for 30.6% of the total lung cancer population, far more than other cancers.
Summary: Up to now, there are more than 400 antibody-drug conjugates (ADC) in the development stage. Among them, the most popular targets is HER2, followed by CLDN18.2, EGFR and TROP2. Here, let's briefly analyze EGFR-directed ADCs.References: [1] Cantor, A. J., et al. Deep mutational analysis reveals functional trade-offs in the sequences of EGFR autophosphorylation sites. Proc. Natl Acad. Sci. USA. 115, E7303-E7312(2018)
[2] Yu J, Fang T, Yun C, Liu X, Cai X. Antibody-Drug Conjugates Targeting the Human Epidermal Growth Factor Receptor Family in Cancers. Front Mol Biosci. 2022 Feb 28;9:847835. doi: 10.3389/fmolb.2022.847835. PMID: 35295841; PMCID: PMC8919033.
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