Solid-phase synthesis of amanitin derivatives and preliminary evaluation of cellular uptake and toxicity

2018 ◽  
Vol 111 (1) ◽  
pp. e24050 ◽  
Author(s):  
Antoine Blanc ◽  
David J. Dietrich ◽  
David M. Perrin
Keyword(s):  
Cellular Uptake ◽  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Preliminary Evaluation ◽  
Phase Synthesis

Synthesis of Asparagusic Acid Modified Lysine and its Application in Solid-Phase Synthesis of Peptides with Enhanced Cellular Uptake

Synlett ◽  
2017 ◽  
Vol 29 (10) ◽  
pp. 1289-1292 ◽  
Author(s):  
Pablo Rivera-Fuentes ◽  
Alina Tirla ◽  
Moritz Hansen
Keyword(s):  
Amino Acid ◽  
Peptide Synthesis ◽  
Cellular Uptake ◽  
Building Block ◽  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Solid Phase Peptide Synthesis ◽  
Live Cells ◽  
Phase Synthesis ◽  
Scalable Synthesis

Cyclic disulfides, such as asparagusic acid, enhance the uptake of a variety of cargoes into live cells. Here, we report a robust and scalable synthesis of an asparagusic acid modified lysine. This amino acid can be used in solid-phase peptide synthesis. We confirmed that incorporation of this building block into the sequence of a peptide increases its cellular uptake substantially.

Concise solid-phase synthesis enables derivatisation of YEATS domain cyclopeptide inhibitors for improved cellular uptake

2021 ◽  
pp. 116342
Author(s):  
Yixiang Jiang ◽  
Sha Liu ◽  
Gaofei Tian ◽  
Hayden Jit Hei Cheung ◽  
Xin Li ◽  
...  
Keyword(s):  
Cellular Uptake ◽  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Phase Synthesis
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