Recognition Tags for Tgase-Mediated Conjugation

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This patent describes a method for functionalizing antibodies, especially those lacking an Fc region, using transglutaminase (TGase) and specific peptide recognition tags (such as a modified c-myc tag). The invention enables site-specific conjugation of various functional molecules (such as drugs, imaging agents, or other proteins) to antibodies through engineered recognition tags that are targeted by TGase-mediated chemistry. This results in more predictable, homogeneous, and efficient attachment of payloads to antibody fragments, providing improved tools for making antibody-drug conjugates and multispecific antibodies.

Use CasesContent extracted from patent full text and abstract with AI.

• Developing antibody-drug conjugates (ADCs) for targeted cancer therapy and other diseases.
• Generating bispecific or multispecific antibodies that can bind multiple targets, such as engaging both cancer cells and immune cells for immunotherapy applications.
• Attaching imaging agents or diagnostic molecules to antibodies for better detection and monitoring of diseases.
• High-throughput functional screening of antibody libraries by site-specific conjugation of various functional groups.
• Customization of antibody pharmacokinetics and specificity for advanced biotherapeutic applications.

BenefitsContent extracted from patent full text and abstract with AI.

• Enables site-specific and predictable conjugation, leading to homogeneous antibody conjugates with defined drug-to-antibody ratios and improved therapeutic properties.
• Works with antibodies and antibody fragments lacking Fc domains, expanding the range of formats that can be engineered and utilized.
• Peptide tags (such as c-myc derivatives) are simple to engineer, broadly compatible, and can be added to many polypeptides.
• Reduces the risk of unwanted antibody polymerization and heterogeneous modification, which can compromise function and safety.
• Facilitates efficient, scalable, and cost-effective production of antibody conjugates, including those bearing challenging (e.g., hydrophobic or large) payloads.
• Accelerates antibody and payload screening and development due to modularity and high-throughput compatibility.
• Improves the stability, efficacy, and safety profile of antibody-based therapeutics and diagnostics due to controlled modification.

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Inventors & Applicants

Patent Abstract

The present application relates to methods for the functionalization of antibodies using transglutaminase, in particular antibodies lacking Fc regions. Also disclosed herein are peptide tags for transglutaminase, linking reagents, functionalized antibodies, multi-specific antibodies, pharmaceutical compositions, and method of treating disease and/or conditions.