THE DITHIASUCCINOYL METHODOLOGY FOR PEPTIDE SYNTHESIS

AT PRESENT, PROGRESS IN PEPTIDE SYNTHESIS IS LIMITED BY THE RIGOROUS PURIFICATION AND CHARACTERIZATION PROCESSES THAT ARE NECESSARY IN BOTH OF THE TWO CURRENTLY ACCEPTED PEPTIDE SYNTHESIS METHODS. BIOTECHNOLOGY, AS WELL AS BIOCHEMICAL AND PHARMACEUTICAL RESEARCH, WILL BENEFIT FROM THE INTRODUCTION OF A NEW METHOD OF PEPTIDE SYNTHESIS THAT USES MILD REAGENTS. IT IS BELIEVED THAT INTRODUCTION OF A RANGE OF DITHIASUCCINOYL (DTS) AMINO ACIDS, AND ANCILLARY REAGENTS, WILL PROVIDE A HIGH-YIELDING, RACEMIZATION-FREE METHOD OF SYNTHESIZING HIGHLY PURE PEPTIDES, WITH CONSEQUENTDRAMATIC IMPROVEMENTS IN PRODUCTIVITY AND THE COMPLEXITY OF PEPTIDES ACCESSIBLE BY CHEMICAL SYNTHESIS. IN PHASE I OF THE RESEARCH, METHODS SUITABLE FOR LARGE-SCALECOMMERCIAL PREPARATION OF DTS=DERIVATIVES WILL BE DEVELOPED,AND STUDIES WILL BE PERFORMED ON THE AUTOMATIC SYNTHESIS OF A CHALLENGING SEQUENCE TO CONFIRM THE SUITABILITY OF THE PROCEDURE. IN PHASE II, A NOVEL AUTOMATIC PEPTIDE SYNTHESIZER DESIGNED SPECIFICALLY TO EXPLOIT THE MERITS OF THE METHOD WILL BE DEVELOPED, AS WILL BE METHODS TO SYNTHESIZE THESE DERIVATIVES IN MULTIKILOGRAM AMOUNTS.