TRANSGLUTAMINASE CONJUGATION METHOD WITH AMINO ACID-BASED LINKERS

TRANSGLUTAMINASE CONJUGATION METHOD WITH AMINO ACID-BASED LINKERS

The present invention relates to a method for generating an antibody-payload conjugate by means of a microbial transglutaminase (MTG). The method comprises a step of conjugating a linker comprising or having the structure (shown in N->C direction) Aax-(Sp1)-B1-(Sp2) via a primary amine in the N-t...

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Hauptverfasser: SPYCHER, Philipp, GRABULOVSKI, Dragan, BERTRAND, Romain, ATTINGER-TOLLER, Isabella
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Sprache:eng ; fre ; ger
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HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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creator SPYCHER, Philipp
GRABULOVSKI, Dragan
BERTRAND, Romain
ATTINGER-TOLLER, Isabella
description The present invention relates to a method for generating an antibody-payload conjugate by means of a microbial transglutaminase (MTG). The method comprises a step of conjugating a linker comprising or having the structure (shown in N->C direction) Aax-(Sp1)-B1-(Sp2) via a primary amine in the N-terminal residue Aax to a glutamine (Gln) residue comprised in the heavy or light chain of an antibody, wherein Aax is an amino acid having the structure NH2-Y-COOH, wherein Y comprises a substituted or unsubstituted alkyl or heteroalkyl chain; (Sp1) is a chemical spacer or is absent; (Sp2) is a chemical spacer or is absent; and B1 is a linking moiety or a payload. Further the present invention relates to antibody-linker conjugates that have been generated with the method of the invention and uses thereof.
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subjects HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
title TRANSGLUTAMINASE CONJUGATION METHOD WITH AMINO ACID-BASED LINKERS
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