Accelerated Multiphosphorylated Peptide Synthesis

[Image: see text] Preparing phosphorylated peptides with multiple adjacent phosphorylations is synthetically difficult, leads to β-elimination, results in low yields, and is extremely slow. We combined synthetic chemical methodologies with computational studies and engineering approaches to develop...

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Detalles Bibliográficos
Autores principales: Grunhaus, Dana, Molina, Estefanía Rossich, Cohen, Roni, Stein, Tamar, Friedler, Assaf, Hurevich, Mattan
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2022
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9397535/
https://www.ncbi.nlm.nih.gov/pubmed/36032360
http://dx.doi.org/10.1021/acs.oprd.2c00164
Descripción
Sumario:[Image: see text] Preparing phosphorylated peptides with multiple adjacent phosphorylations is synthetically difficult, leads to β-elimination, results in low yields, and is extremely slow. We combined synthetic chemical methodologies with computational studies and engineering approaches to develop a strategy that takes advantage of fast stirring, high temperature, and a very low concentration of 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU) to produce multiphosphorylated peptides at an extremely rapid time and high purity.

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