Microwave Assisted Peptide Synthesis of Some Rationally Designed Cell Penetrating Peptides from C-Kit Receptor

Abstract

In the interest of public health, cell-penetrating peptides (CPPs) have proven to be important way for the highly efficient intracellular delivery of bioactive cargos like peptides, proteins, and oligonucliotides. It is feasible to combine one or multiple CPPs with bioactive cargos either by direct chemical conjugation or, more rarely, as non-covalent complexes. The term bioportides was introduced to describe monomeric CPPs that are intrinsically bioactive. One of the consistent problems that may compromise the in vivo applications of CPPs and bioportides, is the stimulation of mast cell (MC) secretion. Therefore, in this study two decapeptides, S6 and S6P, has been designed from the c-kit protein, a mast cells receptor, and synthesized using the technology of microwave assisted solid phase peptide synthesis. In an attempt to find bioportides from the c-Kit protein, and studying their structure- activity relationship, the present work was carried out, investigating the effect of the presence of the phosphotyrosine moiety as an active site in the synthesized peptides.