JP2010522693A JP2009544303A JP2009544303A JP2010522693A JP 2010522693 A JP2010522693 A JP 2010522693A JP 2009544303 A JP2009544303 A JP 2009544303A JP 2009544303 A
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 SNAC-tag for sequence-specific chemical protein cleavage Mar 25, 2019
In this report, we describe the synthesis of cancer cell line specific peptide–gossypol conjugates and their cytotoxic effects. The aldehyde group of gossypol was utilized for conjugation, and thiazolidine (1 a ) as well as imine linkages (1 b ) were explored as traceless cleavable linkers (Figure 1).
Traceless linkers Conventional anticancer therapeutics often suffer from lack of speciﬁcity, resulting in poor therapeutic indexes and substantial toxicities to normal healthy tissues. Monoclonal antibodies have demonstrated considerable utility in cancer medicine, but their curative potential is often limited. Antibody–drug conjugates Staben et al. developed a chemoselective ligation approach that targets tertiary and heteroaryl amines coupled through a so-called “traceless” cleavable linker. After proteolytic cleavage of the linker, an adjacent self-immolating unit cyclizes upon itself and releases the payload in an unmodified form. A comparison of three linker types, (1) noncleavable, (2) cleavable but nontraceless, and (3) traceless, reveals up to an 8-fold improvement in T-cell proliferation when the traceless linker is used. Dec 28, 2019 · overcome these issues. Through the introduction of a traceless cleavable linker, the solubilizing tag can be selectively removed to generate native peptide. Here we describe the synthesis of a next-generation amine-reactive linker N-Fmoc-2-(7-amino-1-hydroxyheptylidene)-5,5-dimethylcyclohexane-1,3-dione
A mild chemically cleavable linker system for functional
Traceless | Definition of Traceless at Dictionary.com Traceless definition, having or leaving no trace: a traceless crime. See more. Christopher Shugrue - NIH Postdoctoral Fellow - Bradley L Secondary Amino Alcohols: Traceless Cleavable Linkers for Use in Affinity Capture and Release Angewandte Chemie International Edition March 29, 2020.