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Misunderstanding of Peptide Synthesis
Since 1963, Merrifield has successfully developed solid phase peptide synthesis (SPPS)
method, and through continuous improvement & perfection, nowadays this method has
become a common technology used in modern peptide and protein synthesis
including Bivalirudin and glycopeptides synthesis. Generally, many common units can
obtain synthetic peptides rely on ready-made peptides synthesis scheme, such as solidphase synthesis, liquid-phase synthesis, as well as large-scale peptide production.
Technically, one usual way to produce such peptides is to buy amino acids from some of
the world’s fine chemical plant production groups as raw materials targeted synthesis of a
single peptide. As pharmaceutical raw materials intermediates, these peptides are
usually used in western medicine formulations to enhance efficacy and improve the
body’s absorption rate of drugs and absorption rate.
In fifties and sixties of last century, peptides are mainly from animal organs. Taking
thymosin as an example, its production method is to cut off the newly born calf’s thymus
and then use the shock separation of biotechnology to separate the calf thymus peptides,
while the final step is to make the thymosin injection. This thymosin is mainly used for
human immunity. At present, such peptide has been out of state due to popular mad cow
disease. This virus can engulf the animal protein in the brain, destroying its brain tissue,
cells and nerves. Therefore, other peptides like Angiotensin II has been payed attention
in recent years.
Once the human body get infected with this virus, it is more terrible than cancer because
such patients will ultimately become vegetative or die very soon. There are also peptides
extracted from human blood, whose side effects are also great. These peptides not only
make the body infected with hepatitis A, hepatitis B, hepatitis C, hepatitis, HIV but also
form rejection of allergic reactions.
For the novice, gaining understanding on the principle of a certain peptide synthesis and
specific process as well as eliminating the problems encountered could be extremely
necessary. In simple terms, the most basic procedure of peptide synthesis process is
nothing more than resin swelling, deprotection, coupling, and then deprotection, and then
Other special synthesis is established on the basis, but there are several errors to note
during the peptide synthesis for mass novice:
1. Omnipotent Peptide Cleavage Reagent
Most of the peptides can be cleaved from the resin by a combination of cleavage
peptides, and this is often necessary for amino acids with specific side chain protection.
For polypeptide sequences without side chain protection, 98% TFA and 2% water
solution can be completed; the flexibility to use a combination of cut peptide reagents
should be payed enough concerns.
2. Amino acid’s side chain protection is the same.
Basic amino acids with active side chains need to be protected in the synthesis, and
depending on the side chain, the protecting groups also have different choices. Selecting
the appropriate protective group can effectively reduce the difficulty of synthesis.
3. Over long Synthesis Process.
The synthesis efficiency of each step in a short time can reach more than 99%, while
long-time reaction on the positive reaction yield is very limited, which could greatly
increase side effects. Therefore, it’s necessary to control the synthesis time as well.
In fact, esterification is a classical organic synthetic reaction; with the development of
peptide synthesis, much research work has been done in this field.