Antibodies bearing engineered cysteine residues (termed THIOMAB™ antibodies) enable the site-selective attachment of a drug, label or other payload for specific delivery to certain tissues (e.g., tumors).

2020年7月22日 · THIOMAB antibody technol. utilizes cysteine residues engineered onto an antibody to allow for site-specific conjugation. The technol. has enabled the exploration of different attachment sites on the antibody in combination with small mols., peptides, or proteins to yield antibody conjugates with unique properties.

2024年12月17日 · The site-specific antibody-drug conjugates (ADCs), particularly those utilizing the engineered cysteine in Fc fragments of mAbs (THIOMAB™ antibodies), have emerged as a novel class of biotherapeutics for cancer treatment.

2008年7月20日 · Our THIOMAB technology resolves the issue of conjugate heterogeneity by directing the attachment of drugs at defined sites and with near-uniform stoichiometry.

Herein we demonstrate that conjugation of a next generation maleimide (NGM) to engineered cysteines in a THIOMAB™ antibody delivers a THIOMAB™ antibody-drug conjugate (TDC) with a drug loading of ca. 2. This TDC is highly stable in blood serum conditions, selective and potent towards HER2 expressing cell lines and meets the current criteria ...

Keywords: site-specific conjugation, antibody drug conjugate, THIOMAB, internalization, tumor antigen, linker, cytotoxic drug. Introduction. Monoclonal antibodies (mAbs) have long been an integral tool in basic research due to their high specificity and affinity for target antigens.

Recently, we have engineered THIOMABs (antibodies with engineered reactive cysteine residues) for site-specific conjugation and showed that these antibody conjugates display homogeneous labeling with optimal in vitro and in vivo characteristics.

Herein, we describe the development of a novel bioconjugation platform combining cysteine-engineered (THIOMAB) antibodies and recombinant XTEN polypeptides for the unprecedented generation of homogeneous, stable “TXCs” with DAR of up to 18.

2007年5月1日 · We have developed a novel robust biochemical assay (PHESELECTOR) to screen reactive thiols on antibody surface with an objective of utilizing these thiol groups for site-specific conjugation of cytotoxic drugs.

The THIOMAB™ antibody technology platform uses site-directed mutagenesis to incorporate cysteines into the anti-body. Conjugation to a classical maleimide bearing the drug of choice affords a THIOMAB™ antibody-drug conjugate (TDC) with full control over site reactivity and a precise drug-to-