Journal
ORGANIC LETTERS
Volume 4, Issue 2, Pages 165-168Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ol016859i
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- NCRR NIH HHS [RR00862] Funding Source: Medline
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Semisynthesis of an active tetra phosphorylated analogue of the Type I TGFbeta receptor is reported. An efficient native chemical ligation protocol was developed to link a tetraphosphopeptide and a recombinant receptor fragment. Synthesis of the peptide alpha-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.
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