Anti-ITGAV+ITGB3 (Etaracizumab)-MC-Vc-PAB-DMEA-(PEG2)-duocarmycin SA ADC
Anti-ITGAV+ITGB3 (Etaracizumab)-MC-Vc-PAB-DMEA-(PEG2)-duocarmycin SA ADC (ADC-W-2131)
This ADC product is comprised of an anti-ITGAV+ITGB3 monoclonal antibody conjugated via a MC-Vc-PAB-DMEA-(PEG2) linker to duocarmycin SA. The duocarmycin SA is targeted to certain cancers by immunerecognition and delivered into cancer cells via receptor mediated endocytosis. Within the cell, duocarmycin SA binds to DNA, causes DNA damage.
ADC Target
Name
ITGAV+ITGB3
Alternative Names
ITGAV+ITGB3
Overview
Integrins are integral cell-surface proteins composed of an alpha chain and a beta chain. They are known to participate in cell adhesion as well as cell-surface mediated signalling. Integrins are heterodimeric integral membrane proteins composed of an alpha chain and a beta chain. CD51 encodes integrin alpha chain V. The I-domain containing integrin alpha V undergoes post-translational cleavage to yield disulfide-linked heavy and light chains, that combine with multiple integrin beta chains to form different integrins. Alpha-V integrins have been implicated in many developmental processes and are therapeutic targets for inhibition of angiogenesis and osteoporosis.
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
duocarmycin SA
Description
Duocarmycins SA belong to the minor-groove-binding DNA-alkylating agents (DNA MGBA). The natural duocarmycins are isolated from the culture broth of Streptmyces sp and a series of derivatives has also been synthesized.