Peptide Knowledge Center

Development history of peptide synthesizer

Polypeptide synthesis has gone through more than 100 years of glorious course. Emil Fischer first began to focus on peptide synthesis in 1902, when progress was rather slow due to too little knowledge of peptide synthesis, until 1932, when Max Bergmann et al began to use benzyl oxycarbonyl (Z) to protect α- amino groups, peptide synthesis began to develop. By the 1950s, organic chemists had synthesized a large number of bioactive peptides, including oxytocin, insulin and so on, and also made a lot of achievements in the synthesis of peptides and amino acid protective groups, which provided experimental and theoretical basis for the later emergence of solid phase synthesis methods.


 Merrifield won the 1984 Nobel Prize in Chemistry for the first time in 1963, when he first proposed solid-phase peptide synthesis (SPPS), a landmark method for the chemical synthesis of peptides, which became the preferred method for the synthesis of peptides because of their convenience and rapidity, and brought about a revolution in the organic synthesis of peptides and became an independent discipline —— solid-phase organic synthesis (SPOS).


Merrifield have been repeatedly screened, the use of benzyl oxycarbonyl (Z) in solid phase was finally discarded. tert-butyl oxycarbonyl (BOC) was first used to protect α- amino groups and to synthesize solid phase peptides. At the same time, the first fully automatic peptide synthesizer was developed in the late 1960s and the biological protease, ribonuclease (124 amino acids) was first synthesized.


 The Lou Carpino first used 9-methoxycarbonyl (FMOC) in 1972 to protect α- amino groups, which can be removed rapidly under alkaline conditions, can react completely in 10 min, and because of its mild reaction conditions and rapid and widespread use, various peptide automatic synthesizers based on the two methods of BOC and FMOC have emerged and developed one after another, and are still being continuously modified and perfected.


The advent of peptide synthesizer has greatly promoted the development of peptide science. In turn, with the development of peptide science, scientists also put forward higher requirements for synthetic instruments, thus driving the development of synthetic instruments. At present, there are many kinds of peptide synthesizers, which can be divided into microgram, milligram, gram and kilogram; functional, can be divided into research, small test, pilot, ordinary and GMP production; automation, can be divided into automatic, semi-automatic and manual; channel, can be divided into single and multi-channel; from the technical point of view, can be divided into the first generation, second generation, and third generation, and so on;

 peptide synthesizer

First generation peptide synthesizer

The first generation of polypeptide synthesizers was produced in the late 1960s and early 1970s. 

It uses nitrogen bubbles or shocks to stir the reactants and computer program control to achieve limited automatic synthesis. That is, the first generation of polypeptide synthesizer summarized later. With the improvement and development of production process, the first generation polypeptide synthesizer has all withdrawn from the market. The first generation of polypeptide synthesizer is of great significance for the later development and manufacture of synthesizer.


Second generation peptide synthesize

The second generation polypeptide synthesizer was born in the 1980s. The characteristics of the second generation peptide synthesizer is mild reaction can be divided into two types: pure nitrogen bubbling and shaking. The representative product is the PS3Peptide Synthesizer launched by Protein Technologies company,and ACT peptide synthesizer Model 90 launched by Advanced ChemTech companies. The disadvantage is that the reaction may cause the reaction "dead corner ". The dead corner of the reaction will decrease the efficiency and purity of the peptide synthesis, and some will even cause the failure of the synthesis.


Third-generation peptide synthesizer

 The third generation polypeptide synthesizer was born in the 1990s. The representative product is the U.S. Applied Biosystems company's ABI 433peptide synthesizer and C S Bio company's CS336 dead-angle polypeptide synthesizer. ABI433 design principle is that the reactor is relatively fixed above, while the bottom of the cycle 360 degrees of rapid rotation, driving the reactor solid-liquid two-phase from the bottom upward spiral motion, always up to the top of the reactor. It means the solution can reach any point inside the reactor and achieve no dead angle.

 The design principle of the CS336 is make the center of the reactor is the center, the top and bottom are rotated 180 degrees, the stirring speed can reach 180 rpm, at the same time, it adopts the superiority of nitrogen bubbling reaction mode, and integrates nitrogen blowing as an optional reaction mode into the reaction method high coupling rate effect of peptide synthesizer in scientific research field is fully reflected


The fourth generation peptide synthesizer

The fourth generation peptide synthesizer has been recognized by more and more customers because of the 180 degree no dead angle stirring mode. Peptide Scientific Inc company began to use the 180 degree up and down flip mechanical infinity speed regulation stirring mode as the iconic feature of the whole series of products developed by it in 2002. From PSI200、300、400、500 to 600, the whole series polypeptide synthesizer adopts the 180-270 degree up and down flip mechanical stirring mode, PSI adopts the numerical control motor system, the stirring speed is infinitely adjustable, and the stirring intensity and speed play to the extreme physical energy.


The fifth generation peptide Synthesizer

The American CEM Company, known for its manufacturing of protein organic reaction equipment, launched Liberty. The microwave peptide synthesizer .It adopts microwave heating method, which greatly improves the reaction rate and increases the reaction rate to several times or even ten times of the previous polypeptide synthesizer. Its innate characteristics have been recognized by many R & D customers. The drug screening polypeptide synthesizer, such as the 106 channel asynchronous automatic polypeptide synthesizer launched by ACT company, the 96 channel automatic polypeptide synthesizer launched by AAPPTEC company, the 98 channel automatic polypeptide synthesizer launched by PTI company, etc. Unfortunately, the side reactions also increased in the case of heating, and the purity of the polypeptide was not comparable to that of the previous third or even second generation products. In addition, microwave heating method can not be amplified, so it is not suitable for the development of polypeptide drugs

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