K. Arar, M. Monsigny, R. Mayer
Dec 10, 1993
Citations
0
Influential Citations
21
Citations
Journal
Tetrahedron Letters
Abstract
Abstract An improved method of preparation of oligonucleotide-peptide conjugates is described. An oligopeptide containing α and e-aminogroups is mainly substituted at its α-NH 2 end by e-maleimidocaproic acid- N -hydroxysuccinimide ester at pH 6.5 for 1 h. The N α -maleimidocaproyl-peptide derivative, purified by HPLC, reacts with the thiol group of an oligonucleotide in a 82% yield at pH 7.2. The thiol group is generated in situ by the action of tris(carboxyethyl)phosphine on an oligonucleotide bearing a disulfide bridge.