Cell –Penetrating Peptides (CPPS)2016-07-13
Most of the active small molecular and fluorescent dyes on the market are not well across the cell membrane barrier and into cells, which restricts these chemicals for a wild range of applications in drug research and detection. Cell –Penetrating Peptides (CPPS), are short peptides that facilitate cellular intake/uptake of various molecular equipment. CPPs typically have an amino acid composition that either contains lysine or arginine or has sequences that contain an alternating pattern of polar/charged amino acids and non-polar, hydrophobic amino acids.
Ontores is able to use CPPS modified with the active small molecular and fluorescent dyes, which can get into cells. Take ReACp53 for example. It is a cell-penetrating peptide, designed to inhibit p53 amyloid formation, rescues p53 function in cancer cell lines and in organoids derived from high-grade serous ovarian carcinomas (HGSOC), an aggressive cancer characterized by ubiquitous p53 mutations. Rescued p53 behaves similarly to its wild-type counterpart in regulating target genes, reducing cell proliferation and increasing cell death.
After several years’ research, Ontores has skillfully mastered the technology of modified CPPS. Ontores is able to provide strong technology support for customers’ research.
Data for ReACp53:RRRRRRRRRRPILTRITLE：
Phospho Peptide Synthesis2016-07-06
Peptide is one of the most popular active small molecular on the market. In 2016, the market share of pharmaceutical peptides will probably reach to 10 billion dollars.
Protein phosphorylation and dephosphorylation are ubiquitous reactions involved in many important cell processes, including cell signaling. Accordingly, the preparation of phosphopeptides has received much attention in the chemical literature. Phospho peptides can be prepared either by phosphorylation of an existing peptide (global phosphorylation strategy) or by the use of individual phosphor amino acid building blocks in standard peptide synthesis (prephosphorylation strategy). As with other amino acids, the choice of the side chain protecting group is critical in order to minimize side reactions.
Ontores has already been skillful in both phosphor amino acid building blocks synthesis and single phosphorylation site or multiple phosphorylation sites modification.
Forigerimod (Figure 1) is a phosphor peptide which is developed by ImmuPharma. It is for the treatment of Systemic Lupus Erythematosus, and has already entered Phase III clinical trial stage.
The Application of β-Amino Acids2016-06-29
Currently, lots of pharmaceutical peptides are synthesized by natural amino acids through the condensation reaction of amide bonds. Natural amino acids are also known as α-amino acids. This kind of peptide can form a stable secondary structure by α-helices and β-strands, and it has good regulatory effects on some enzymes in human body. However, there are varieties of proteases which can hydrolyze peptides in human body. It shortens the half-life period of pharmaceutical peptides, which increase the difficulty and cost of giving drugs
After a long time comparative study, scientists found not only the bio-activities of β-peptides are as good as α-peptides, but they also have better tolerance against the hydrolysis of protease and longer half-life than α-peptides. Therefore, the use of β-amino acids will become a research hotspot in pharmaceutical peptide industries.
Synthesis Method of β-amino acid:
Standard Solid Phase Synthesis Method of β-peptide: