LINKERS FOR IMPROVING THE STABILITY OF BIOCONJUGATES AND THE SELECTIVITY OF PAYLOAD RELEASE

Disclosed herein are linker architectures for conjugates that do not rely on the SAR of the cleavable trigger or the large steric bulk of a closely positioned antibody to alter payload release. These linkers are expected to reduce off-target payload release facilitated by extracellular cathepsins, a...

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Bibliographic Details
Main Authors DAVIS, Paul D, GIESE, Matthew
Format Patent
LanguageEnglish
Published 25.08.2022
Subjects
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
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Summary:Disclosed herein are linker architectures for conjugates that do not rely on the SAR of the cleavable trigger or the large steric bulk of a closely positioned antibody to alter payload release. These linkers are expected to reduce off-target payload release facilitated by extracellular cathepsins, and may also be applicable to conjugates of antibody fragments that lack the steric protection from a full antibody. In addition, the linkers disclosed herein are expected to provide more selective intracellular payload release. Thus, these linkers can function synergistically with the targeting vector to confer differential payload release rates in vivo that improve the selectivity of intracellular payload release and reduce off target toxicity.
Bibliography:Application Number: US202117554668