Ontology highlight
ABSTRACT:
SUBMITTER: Anami Y
PROVIDER: S-EPMC6023893 | biostudies-other | 2018 Jun
REPOSITORIES: biostudies-other
Nature communications 20180628 1
Valine-citrulline linkers are commonly used as enzymatically cleavable linkers for antibody-drug conjugates. While stable in human plasma, these linkers are unstable in mouse plasma due to susceptibility to an extracellular carboxylesterase. This instability often triggers premature release of drugs in mouse circulation, presenting a molecular design challenge. Here, we report that an antibody-drug conjugate with glutamic acid-valine-citrulline linkers is responsive to enzymatic drug release but ...[more]