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The most popular linker is the protease cleavable linker that contains a valine-citrulline-para-aminobenzyl-carbamate moiety (vc-PABC). 10 This is a traceless linker that allows the release of amine containing cytotoxins. Oct 14, 2016 · Cleavable linkers. A major class of ADC linkers is the cleavable linker (Fig. 7). Cleavable linkers are designed to be cleaved by responding to an environmental difference between the extracellular and intracellular environments (pH, redox potential, etc.) or by specific lysosomal enzymes. So, ADCs with noncleavable linkers are more dependent on the biology of the target cell compared to cleavable linkers. Moreover, these ADCs have improved therapeutic index due to their greater stability. The most advantage of using non-cleavable linkers is their increased plasma stability when compared to many cleavable linkers. Owing to its slow and variable release, an alternative is urgently required to improve effectiveness. Herein we describe a PEGylated colistin prodrug whereby the PEG is attached via a cleavable linker (col-aaPEG) introducing an acetic acid terminated poly (ethylene glycol) methyl ether (aaPEG) onto the Thr residue of colistin.
Protein Cross-linkers handbook and selection guide
Releasable conjugation of polymers to proteins 1 Releasable conjugation of polymers to proteins Yuhui Gong1, Jean-Christophe Leroux1, and Marc A. Gauthier2,* 1 Swiss Federal Institute of Technology Zurich (ETHZ), Department of Chemistry and Applied Biosciences, Institute of Pharmaceutical Sciences, Vladimir-Prelog-Weg 1–5/10, 8093 Zurich, Linkers for Antibody Drug Conjugates: Current Role and May 31, 2016
A novel disulfide linker was designed to enable a direct connection between cytotoxic pyrrolobenzodiazepine (PBD) drugs and the cysteine on a targeting antibody for use in antibody–drug conjugates (ADCs). ADCs composed of a cysteine-engineered antibody were armed with a PBD using a self-immolative disulfide linker. Both the chemical linker and the antibody site were optimized for this new
Mar 29, 2020 · The linkers are cell compatible; a cell‐penetrating peptide that contained this linker was efficiently captured and identified after uptake into cells. These findings suggest secondary amino alcohol‐based linkers might be suitable tools for peptide discovery platforms. Apr 18, 2012 · In this paper, we report on the characteristics of a traceless photo-cleavable cross-linker, di 6-(3-succinimidyl carbonyloxymethyl-4-nitro-phenoxy)-hexanoic acid disulfide diethanol ester (SCNE). The traceless feature and the biocompatibility of this photo-cleavable cross-linking reagent were corroborated. Mar 10, 2020 · Traceless linkers are so called because an examination of the final compound reveals no trace of the point of linkage to the solid phase. The first and most widely explored of this traceless linker is the silyl linker. These linkers show non-specific function after cleavage. Traceless linkers are so called because an examination of the final compound reveals no trace of the point of linkage to the solid phase. The oldest definition for „traceless“ traces back to the import of a Hydrogenatom instead of the previous linker. Jun 01, 2004 · A new oxidatively cleavable traceless linker for solid-phase chemistry has been described by Waldmann et al. 25., 26. based on the hydrazide group. The polymer-bound acyl hydrazides 21 were prepared by a hydrazine formation between a carboxy-functionalized resin 19 and different substituted hydrazines 20 . This linker is compatible with several organic synthesis reactions and can be removed selectively in a traceless manner with mild oxidative methods.