Optimizing Lysosomal Activation of Antibody–Drug Conjugates (ADCs) by Incorporation of Novel Cleavable Dipeptide Linkers

Volume: 16, Issue: 12, Pages: 4817 - 4825
Published: Oct 14, 2019
Abstract
Although peptide linkers are used in multiple clinical-stage ADCs, there are only few reports on optimizing peptide linkers for efficient lysosomal proteolysis and for stability in circulation. We screened multiple dipeptide linkers for efficiency of proteolysis and compared them to the dipeptide linkers currently being evaluated in the clinic: Val-Cit, Val-Ala, and Ala-Ala. Lead dipeptide linkers selected from the initial screen were...
Paper Details
Title
Optimizing Lysosomal Activation of Antibody–Drug Conjugates (ADCs) by Incorporation of Novel Cleavable Dipeptide Linkers
Published Date
Oct 14, 2019
Volume
16
Issue
12
Pages
4817 - 4825
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