There are so many payloads, like MMAE, Calicheamicin, MMAF, DM1, SN-38 and Dxd. Microtubule destroying drug 1. Calendula Auristatins is an important payload used in ADC. The most famous family member MMAE exists in two listed drugs, adcetris and Polivy. At present, more than 10 kinds of ADCs with calendula (such as MMAE) or methylcalendula […]
Category Archives: adc
Table2. Chemical triggers Conjugate linker is not only the molecular part forming covalent connection between antibody and small molecule payload, but also the key element with design properties in targeted drug therapy. The addition of linkers should not induce aggregation, and it is necessary to ensure acceptable PK characteristics, limit the premature release (stability) of […]
1. Mylotarg® (gemtuzumab ozogamicin) from Wyeth/Pfizer was the first ADC to reach the market. It is composed of a recombinant humanized anti-CD33 mAb (IgG4κ antibody hP67.6) covalently attached to a calicheamicin derived payload (N-acetyl-γ-calicheamicin 1,2-dimethyl hydrazine dichloride) via a pH-sensitive hydrazone linker. 2. Adcetris® (brentuximab vedotin) from Seagen (formerly Seattle Genetics), containing a CD30-specific mAb conjugated to […]
FDA approved Antibody-drug conjugate (ADC) for clinical use Clinically, most of the ADC drugs approved by FDA are IgG1, and the targets are CD33, CD22, HER2 and so on. The most common payload is MMAE, also contains calicheamicin, DM1. ADC drugs are mainly used in the field of antitumor, which is one of the hot […]
The structure of antibody-drug conjugate (ADC) ADC consists of antibodies and payload, linker connects antibodies and small molecule drugs. After ADC drugs enter the blood, its antibody part will recognize and bind to the surface antigen of target cells. Theninternalizing ADC antigen complex into cells through endocytosis, the complex will be degraded by lysosomes and […]
Product List Case study: Product data of Antibody-drug conjugate (ADC) Antibody Payload QC Ab-001 VCMMAE SDS-PAGE(reducing and non-reducing) Human IgG1 Control DAR Ab-002 Cytotoxity assay First, we used a higher dose of reducing agent (TCEP) and small toxic molecule (vcmmae) to ensure the success of coupling. SDS-PAGE (reducing DTT & non reducing DTT) results showed […]
SDS-PAGE We need run SDS-PAGE(reducing and non-reducing DTT) to see the integrity of antibody and Preliminary observation of the connection of small molecules. In general, we can see that the conjugated antibody will shift upward compared with the naked antibody DAR (methods and standard) ADC drugs are essentially a mixture, which is composed of mAbs […]
In addition to thiomonoclonal antibody technology, the addition of non-standard amino acids (NCAA) provides another possibility for site-specific coupling. The technology uses amino acids with unique chemical structure, which can introduce linker payload complexes in a chemically selective manner. This technique requires the recombination of antibody sequences, using tRNA and aminoacyl tRNA synthetase (AARS) orthogonal […]
Site specific biological coupling of engineered antibodies Advances in bioorthogonal chemistry and protein engineering contribute to the generation of more uniform ADCs. Although there are many attachment methods available on natural monoclonal antibodies, site-specific biological coupling on engineered antibodies can more effectively control Dar and avoid changing the affinity for antigen binding. In this […]
Glycan coupling Because IgG is a glycoprotein, it contains an N-glycan at n297 of CH2 domain of each heavy chain of Fc fragment. This glycosylation can be used as the attachment point of connecting payload. The long-distance localization between polysaccharide and Fab region reduces the risk of damaging the antigen binding ability of antibody after […]
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