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Stapled Peptide Synthesis2016-08-31
A stapled peptide is a peptide that has a synthetic brace ("staple"). Peptides with multiple, tandem staples are sometimes referred to as stitched peptides. Peptide stapling is used to enhance pharmacologic performance of peptides.
All the natural peptides have bioactive α-helical and β-fold conformation, but the synthetic liner peptides usually lack such bioactive structures. Stapling can greatly improve the pharmacologic performance of peptides, increasing their target affinity, proteolytic resistance, and serum half-life while conferring on them high levels of cell penetration through endocytic vesicle trafficking.
Here, we take R8 and S5 for example to discuss the synthesis method of stapled peptide. An i, i+4 stapled peptide requires one unit of R8 at the i position and one unit of S5 at the i+4 position.
One-pot Reaction for Cyclo-Dipeptide Synthesis2016-08-24
Cyclo-Dipeptides belongs to the diketopiperazine (DKP) family, which is the smallest cyclic organic compound in the nature. Cyclo-Dipeptides have the broad spectrum of bioactivities, and they were found to exist in animals, plants and Microorganism. There are a lot of synthesis methods for the cyclo-dipeptide at present. We will introduce a simple method for cyclo-dipeptides today: The One-pot reaction Method.
We will take the synthesis process of Cyclo (Trp (Boc)-Ala) as an example: