This ADC product is comprised of an anti-EGFR monoclonal antibody (Trastuzumab) conjugated via a VC linker to Duostatin-3. The Duostatin-3 is targeted to certain cancers by immunerecognition and delivered into cancer cells via receptor mediated endocytosis. Within the cell, Duostatin-3 binds to tubulins, interrupts microtubule dynamics, and subsequently, induces cell death.
The protein encoded by this gene is a transmembrane glycoprotein that is a member of the protein kinase superfamily. This protein is a receptor for members of the epidermal growth factor family. EGFR is a cell surface protein that binds to epidermal growth factor. Binding of the protein to a ligand induces receptor dimerization and tyrosine autophosphorylation and leads to cell proliferation. Mutations in this gene are associated with lung cancer. Multiple alternatively spliced transcript variants that encode different protein isoforms have been found for this gene.
ADC Antibody
Overview
Anti-EGFR lgG1 Antibody, Zalutumumab
Generic name
Zalutumumab
Species Reactivity
Human
ADC Linker
Name
VC (valine-citrulline)
Description
Peptide linkers, belonging to Enzymatically cleavable linkers, combine greater systemic stability with rapid enzymatic release of the drug in the target cell. The scission of peptidic bonds relies on lysosomal proteolytic enzymes, which have very low activities in blood due to endogenous inhibitors and the unfavorably high pH value of blood.
ADC payload drug
Name
Duostatin-3
Description
Duostatin-3 is an antimitotic agent that inhibits cell division by blocking of tubulin polymerization. Unlike vcMMAE, duostatin-3 cannot kill neighboring tumor cells when the drug is released from the antibody.