On August 19, 2020, Lerchen, Hans-Georg; Stelte-Ludwig, Beatrix; Sommer, Anette; Berndt, Sandra; Rebstock, Anne-Sophie; Johannes, Sarah; Mahlert, Christoph; Greven, Simone; Dietz, Lisa; Joerissen, Hannah published an article.Category: esters-buliding-blocks The title of the article was Tailored Linker Chemistries for the Efficient and Selective Activation of ADCs with KSPi Payloads. And the article contained the following:
Several antibody-drug conjugates (ADCs) have failed to achieve a sufficiently large therapeutic window in patients due to toxicity induced by unspecific payload release in the circulation or ADC uptake into healthy organs. Herein, we describe the successful engineering of ADCs consisting of novel linkers, which are efficiently and selectively cleaved by the tumor-associated protease legumain. ADCs generated via this approach demonstrate high potency and a preferential activation in tumors compared to healthy tissue, thus providing an addnl. level of safety. A remarkable tolerance of legumain for different linker peptides, including those with just a single asparagine residue, together with a modifier of the physicochem. metabolite profile, proves the broad applicability of this approach for a tailored design of ADCs. The experimental process involved the reaction of Bis(2,5-dioxopyrrolidin-1-yl) glutarate(cas: 79642-50-5).Category: esters-buliding-blocks
The Article related to linker peptide antibody drug conjugate antitumor targeting tweakr, Pharmaceuticals: Formulation and Compounding and other aspects.Category: esters-buliding-blocks
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