|Topic:||peptide synthesis to obtain therapeutic peptides .|
|Details:|| The production of peptides by automated synthesis on solid support provides a great variety of benefits. Chemical reactions necessary to assemble peptides can be performed simultaneously with plenty of reaction tubes allowing parallel and multiple syntheses. Owing to the simple washing of the resin following coupling or deprotection steps, no intermediate purification is necessary. Furthermore, the possibility to use excess amounts of reagents facilitates high yields of the synthesized peptides. This fast, automated and practicable method has evolved to a major technique to produce chemically synthesized peptide therapeutics, which pushed the market steadily. Automated SPPS is of great importance, especially for structure–activity relationship studies and backbone modification of biologically active peptide hormones. Nevertheless, there are still some issues that have to be addressed. For instance, incorporation of N-methylated amino acids in order to improve their proteolytic stability often is difficult because of steric hindrance . Moreover, the introduction of fatty acids and PEG moieties, especially large sizes, is generally performed manually .
Although remarkable progress has been accomplished since the invention by Merrifield more than 50 years ago , novel technologies in automated peptide synthesis are required. Microwave-assisted SPPS, for instance, has been shown to not only enhance reaction rates but also to enable the synthesis of difficult and rigid peptide sequences . This technique is progressing but needs more improvements, especially in terms of practicability. The ongoing need for peptides as biopharmaceuticals will surely promote these developments in the future.
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