Improving the Stability of Maleimide–Thiol Conjugation for Drug Targeting
Abstract: Maleimides are essential compounds for drug conjugation reactions via thiols to antibodies, peptides and other targeting units. However, one main drawback is the occurrence of thiol exchange reactions with, for example, glutathione resulting in loss of the targeting ability. A new strategy to overcome such retro‐Michael exchange processes of maleimide–thiol conjugates by stabilization of the thiosuccinimide via a transcyclization reaction is presented. This reaction enables the straightforward synthesis of stable maleimide–thiol adducts essential in drug‐conjugation applications.
- Standort
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Deutsche Nationalbibliothek Frankfurt am Main
- Umfang
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Online-Ressource
- Sprache
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Englisch
- Erschienen in
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Improving the Stability of Maleimide–Thiol Conjugation for Drug Targeting ; volume:26 ; number:68 ; year:2020 ; pages:15867-15870 ; extent:4
Chemistry - a European journal ; 26, Heft 68 (2020), 15867-15870 (gesamt 4)
- Urheber
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Lahnsteiner, Marianne
Kastner, Alexander
Mayr, Josef
Roller, Alexander
Keppler, Bernhard K.
Kowol, Christian
- DOI
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10.1002/chem.202003951
- URN
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urn:nbn:de:101:1-2022060611113885322688
- Rechteinformation
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Open Access; Der Zugriff auf das Objekt ist unbeschränkt möglich.
- Letzte Aktualisierung
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15.08.2025, 07:35 MESZ
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Beteiligte
- Lahnsteiner, Marianne
- Kastner, Alexander
- Mayr, Josef
- Roller, Alexander
- Keppler, Bernhard K.
- Kowol, Christian
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