- RGD containing cyclic peptides are highly efficient integrin receptors.
- Solid phase cyclization is the cyclization reaction on the resin, which is cut off from the resin after ring formation.
- Choosing a good reaction strategy, different protection group selection will also affect the subsequent reaction and the yield of the product.
- The solid phase cyclization under the condition of another protective group. DMAB Oh (Fig. Compared with allyl, it has obvious advantages
RGD containing cyclic peptides are highly efficient integrin receptors.
RGD containing cyclopeptides can inhibit the adhesion of swollen Liu Xi cells to the extracellular matrix through competitive binding to integrin receptors, or directly induce apoptosis of swollen Liu Xi cells. Zui can finally inhibit the proliferation, invasion and metastasis of swollen Liu Xi cells.
At present, the cyclization of polypeptides generally adopts the mixed method of solid phase and liquid phase. But its operation process is complicated compared with direct solid-phase cyclization.
Solid phase cyclization is the cyclization reaction on the resin, which is cut off from the resin after ring formation.
The solid-phase cyclization strategy has the advantages of simple separation and purification, and can avoid the formation of dimers or polymers through the “pseudo dilution” effect.
Compared with the coupling reaction of constructing linear peptide, cyclization belongs to intramolecular reaction with low yield, low purity and long reaction time.
However, it is still difficult to avoid the linear ring polymerization in the solution of RGD.
Microwave method is one of the auxiliary technologies to accelerate organic reaction. Microwave assisted reaction can shorten the time, improve the yield and reduce the by-products. It has been widely used in peptide solid-phase Cheng.
Choosing a good reaction strategy, different protection group selection will also affect the subsequent reaction and the yield of the product.
A kind of RGD cyclic peptide solid phase Cheng preparation process, using Fmoc / TBU / allyl orthogonal protection strategy.
The limitation of this method lies in allyl protecting group. Allyl protecting group:
(1) Selective removal of allyl esters requires the use of expensive palladium catalyst [PD (PPh3) 4], and the reaction conditions are complex;
(2) The reaction time of allyl ester removal is longer and the removal of Quan is difficult;
(3) The peptide of Cheng may be contaminated by residual metal catalyst.
The solid phase cyclization under the condition of another protective group. DMAB Oh (Fig. Compared with allyl, it has obvious advantages
(1) The removal conditions are mild and no metal catalyst is involved;
(2) DMAB ester was stable in piperidine and trifluoroacetic acid with good compatibility.
Using Fmoc / TBU / DMAB orthogonal protection strategy, the efficiency of solid-phase cyclization can be improved by microwave-assisted technology. The combined Cheng route is characterized by high efficiency and mild conditions.
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