How to synthesize RGD cyclopeptide

Integrin, or integrin, is a heterodimer transmembrane glycoprotein receptor that mediates animal cell adhesion and signaling. It is composed of α and β subunits. It is involved in the optimization of various cellular actions including cell migration, cell infiltration, cell and intercellular signaling, cell adhesion, and angiogenesis processes. Integrin αvβ3 is now more widely explored. The appearance of integrin αvβ3 is closely related to tumor migration, angiogenesis, inflammation and osteoporosis. Integrin is highly expressed in all tumor tissues and endothelial cell membranes of neovascularization. The appearance of integrin is closely related to tumor migration and angiogenesis. In recent years, scientific studies have shown that there are 11 integrins that can bind specifically to RGD peptide, which are antagonistic peptides for integrin receptors.

 

RGD peptide is classified into linear RGD peptide and RGD cyclic peptide. Compared with linear RGD peptide, RGD cyclic peptide has stronger receptor compatibility and receptor specificity. The following are the common types and synthesis methods of RGD cyclic peptide.

Common types of RGD cyclic peptides:

1. Cyclic peptides containing RGD sequences formed by disulfide bonds

2. Cyclic peptides containing RGD sequences formed by amide bonds

Synthesis of RGD cyclic peptide:

The utility model relates to a RGD cyclic peptide synthesis process in the field of solid phase polypeptide synthesis technology. The new method is to select 2-chloro-triphenylmethyl chloride resin as the prerequisite carrier, first connect the first side chain carboxyl group with a special protective group of D aspartic acid amino acid, then connect the linear peptide of RGD sequence peptide to the resin, and the last amino acid to remove the protective group FMOC without piperidine. The specified catalyst was added to remove the side chain carboxyl protective group of the first D aspartic acid directly from the resin, followed by the addition of piperidine to remove the amino protective group FMOC of the end amino acid, followed by the addition of binding agent to dehydrate and condense the carboxyl group and amino group exposed from the head and end of the linear peptide directly from the resin in the form of amide bond to produce cyclic peptide. Finally, the cyclic peptide is cut directly from the resin with the cutting solution.


Post time: Apr-24-2023