Anti-APP (Crenezumab)-MC-Vc-PAB-DMEA-(PEG2)-duocarmycin SA ADC
Anti-APP (Crenezumab)-MC-Vc-PAB-DMEA-(PEG2)-duocarmycin SA ADC (ADC-W-691)
This ADC product is comprised of an anti-APP 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.
This gene encodes a cell surface receptor and transmembrane precursor protein that is cleaved by secretases to form a number of peptides. Some of these peptides are secreted and can bind to the acetyltransferase complex APBB1/TIP60 to promote transcriptiowhile others form the protein basis of the amyloid plaques found in the brains of patients with Alzheimer disease. In addition, two of the peptides are antimicrobial peptides, having been shown to have bacteriocidal and antifungal activities. Mutations in this gene have been implicated in autosomal dominant Alzheimer disease and cerebroarterial amyloidosis (cerebral amyloid angiopathy). Multiple transcript variants encoding several different isoforms have been found for this gene.
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.