Patent ID: 6326468
Filing Date: 2001-12-04
Classification: C07K

Abstract:
A method of producing an assembled peptide in aqueous solution and on a solid phase comprising:a) binding a partially or completely unprotected first peptide segment to a solid phase via a linker to form a solid phase-bound first peptide segment, wherein said partially or completely unprotected first peptide segment comprises an N-terminus and a thioester of the formula --COSR at its C-terminus, wherein said linker comprises a cleavable moiety and said partially or completely unprotected first peptide segment is bound to said linker at said N-terminus, and wherein R is a straight or branched C.sub.1-15 functionalized alkyl group, a C.sub.1-15 aromatic structure, or 1 to 4 amino acids or derivatives thereof;b) ligating a partially or completely unprotected second peptide segment to said solid phase-bound first peptide segment, wherein said second peptide segment comprises a cysteine at its N-terminus and a thioacid at its C-terminus, and wherein said N-terminal cysteine of said second peptide segment is capable of selectively ligating to said C-terminus of said solid phase-bound first peptide to form a solid phase-bound peptide comprising a thioacid at its C-terminus;c) converting said thioacid of said phase-bound peptide to a thioester of the formula --COSR to form a solid phase-bound peptide comprising a thioester at its C-terminus; andd) ligating an partially or completely unprotected third peptide segment to said solid phase-bound peptide, wherein said third peptide segment comprises a cysteine at its N-terminus, to form a solid phase-bound assembled peptide; ande) optionally repeating steps to b), c) and d) with additional partially or completely unprotected peptide segments, wherein if said steps b) and c) are repeated, the peptide segment of step d) prior to such repetition comprises a thioacid at its C-terminus.