Any updates on the myostatin shot?
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oh, yes. We have enhanced and extended it. Vaccine, version 2, currently waiting for reports about efficiency and usage peculiarities. Its brand name will be PharmaGen. Here is the short description.
PharmaGen 2: myostatin+ somatostatin vaccine, ver.2
The drug is a polyvalent vaccine comprising two fusion proteins making our body to produce antigens blocking the action of endogenous myostatin and somatostatin. Let`s consider both substances in detail.
What is myostatin?
Myostatin (also known as growth differentiation factor 8, abbreviated GDF-8) is a myokine, a protein produced and released by myocytes that acts on muscle cells' autocrine function to inhibit myogenesis: muscle cell growth and differentiation.
Human myostatin consists of two identical subunits, each consisting of 109 amino acid residues. Its total molecular weight is 25.0 kDa.
Myostatin is produced primarily in skeletal muscle cells, circulates in the blood and acts on muscle tissue, by binding a cell-bound receptor called the activin type II receptor.
Myostatin acts in two ways: by inhibiting muscle differentiation, and by inhibiting Akt-induced protein synthesis.
Animals either lacking myostatin or treated with substances that block the activity of myostatin have significantly more muscle mass. Furthermore, individuals who have mutations in both copies of the myostatin gene have significantly more muscle mass and are stronger than normal.
To put it simply, myostatin plays a role in down-regulating or inhibiting the growth and development of skeletal muscle. Inhibition of myostatin leads to muscle hyperplasia and hypertrophy. Myostatin inhibition can improve athletic performance.
What is somatostatin?
Somatostatin, also known as growth hormone-inhibiting hormone (GHIH), is a peptide hormone that inhibits the secretion of several other hormones, including growth hormone, thyroid stimulating hormone and insulin.
Somatostatin has two active forms produced by alternative cleavage of a single preproprotein: one of 14 amino acids, the other of 28 amino acids. Its molecular formula is C76H104N18O19S2, molecular weight - 1637.878 Da.
Somatostatin is secreted primarily in the nervous and digestive systems. Somatostatin released in the pyloric antrum travels via the portal venous system to the heart, then enters the systemic circulation to reach the locations where it will exert its inhibitory effects.
Somatostatin produced in hypothalamus is then carried to the anterior pituitary gland, where it inhibits the secretion of growth hormone from somatotrope cells. The somatostatin neurons in the periventricular nucleus mediate negative feedback effects of growth hormone on its own release; the somatostatin neurons respond to high circulating concentrations of growth hormone and somatomedins by increasing the release of somatostatin, so reducing the rate of secretion of growth hormone.
Pharmagen, ver. 2. What is this?
The vaccine has been developed first of all in order to elicit a highly specific anti-GDF8 immune response. This is not a myostatin inhibitor. There are several ways/drugs to inhibit myostatin (Ace-031, Myo-029, etc), but most of them have significant shortcomings and require high dosages to be really effective.
We offer a modified myostatin, which makes our body to produce its own antibodies to the endogenous myostatin. Moreover, we modernized the vaccine and developed the revised version, which is capable also of somatostatin down-regulation. In fact, this is vaccination followed by immunization; similar to those vaccines, which children are vaccinated by.
The purpose of the development was the preparation of an immunologically active myostatin-containing protein and somatostatin-containing protein inducing an immune response of the body to myostatin and somatostatin, respectively.
The purpose has been achieved by creating a recombinant DNA plasmid pC (Sp) nS coding the fusion protein with the sequence of myostatin (or somatostatin-14), and a spacer (Sp) n ensuring disposition of myostatin (or somatostatin) on the surface of the fusion protein. The number of spacer monomer units (n) can vary from 1 to 8.
The spacer with the values from 1 to 8 ensures disposition of myostatin or somatostatin-14. As carrier for myostatin and somatostatin-14 serve enzymatically inactive water-insoluble chloramphenicol acetyltransferase without 10 terminal amino acids, purified and renatured fusion protein synthesized in a protease-defective strain of Escherichia coli bacteria.
The claimed recombinant DNA plasmid determines constructive synthesis of a fusion protein chloramphenicol acetyltransferase - myostatin (or chloramphenicol acetyltransferase - somatostatin-14) under the control of its own promotor in E. coli cells with a reduced level of degradation of abnormal proteins.
To put it simply, the fusion protein is expressed by a strain of E.coli, transformed by the indicated plasmid pC (Sp) 4S.
In other words, the fusion protein with disposed myostatin (or somatostatin) is an insoluble in water enzymatically inactive chloramphenicol acetyltransferase without 10 terminal amino acid residues, to which via a spacer sequence (RP) n, where n = 1-8, is attached the sequence of myostatin or somatostatin-14.
After vaccination these fusion proteins induce synthesis of myostatin-specific and somatostatin-specific antibodies, which results in the immune response of the body and long-term down-regulating of endogenous GDF8 and somatostatin function.
In practice these processes are expressed in:
- Muscle hypertrophy
- Increase the production of endogenous growth hormone
- Acceleration of metabolism
- Acceleration of fat loss and improved body composition and muscle definition
First results of the vaccine demonstrated good tolerability, with no noted side effects, except high body temperature at the next day or two after vaccination.
Each vial of PharmaGen v.2 comprises:
10 mg of myostatin-containing protein
10 mg of somatostatin-containing protein
The vaccine is readily administered intramuscularly. For an athlete with body-weight no more than 220 lb (100 kg) one vial is enough for the entire cycle. A half of the vial shall be injected deep intramuscularly (preferably into buttock) and another half in 2 weeks.
The vaccine shall be stored refrigerated.
