Efficient semisynthesis of a tetraphosphorylated analogue of the type I TGFβ receptor

Robert R. Flavell, Morgan Huse, Mike Goger, Michelle Trester-Zedlitz, John Kuriyan, Tom W. Muir

Research output: Contribution to journalArticle

49 Scopus citations

Abstract

Chemical equation presented Semisynthesis of an active tetraphosphorylated analogue of the Type I TGFβ receptor is reported. An efficient native chemical ligation protocol was developed to link a tetraphosphopeptide and a recombinant receptor fragment. Synthesis of the peptide α-thioester on a 4-sulfamylbutyryl resin was optimized following the characterization of a major side reaction and subsequent substitution of norleucine for methionine in the peptide sequence. These optimized protocols will be applicable to the semisynthesis of related protein kinases.

Original languageEnglish (US)
Pages (from-to)165-168
Number of pages4
JournalOrganic Letters
Volume4
Issue number2
DOIs
StatePublished - Dec 1 2002
Externally publishedYes

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Physical and Theoretical Chemistry
  • Organic Chemistry

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