Peptide and Bioregulator Science

Peptide and Bioregulator Science

A short history

Introduction

This one may be boring to all but the history buffs out there. Let's take a look at how we got to where we are now with peptide and bioregulator science. Here's a few of the giants in this field and their work.

Peptides were discovered in the early 20th century by the German chemist Hermann Emil Fischer. In 1900, he put forward his hypothesis that peptides consist of chains of amino acids formed by certain bonds, which were later termed peptide bonds, for lack of a better name.

In 1902 he obtained irrefutable proof of the existence of peptide bonds. In 1905 he invented a method of peptide synthesis in the laboratory.

Professor Jean Martinez is also recognized for his work on Organic and Peptide Synthesis methods. He also developed and synthesized selective neuropeptides.

Enter the Russians

Vladimir H. Khavinson, among his many honors, was the Vice President of the Gerontology Association of the Russian Academy of Sciences. This was the cold war era and the Russians were looking for an edge for their military recruits and their cosmonauts. They were also focused on excelling in the world stage of the Olympic Games.

Professor Khavinson's work in these fields focused on the concept of regulation of peptides that might impact aging. His scientific career was focused on prolonging life and increasing the quality of life. Professor Khavinson's innovations were in the field of synthesis research and the use of short peptides. His work was revolutionary.

Russian scientists have played a central role in developing both classical peptide drugs (hormones, neuropeptides, immunomodulators) and the modern peptide bioregulators. One of the discoveries was that fragments of messenger molecules might have a more specific effect and possibly eliminate unwanted effects.

For example, Growth Hormone is a long molecule. They discovered that certain fragments of that long molecule could selectively produce specific effects without the need to use the hormone. We'll cover this topic later, along with the many related peptides that target specific GH effects.

In Russia today, they have an unusually broad peptide pharmacopeia relative to its overall pharmaceutical. They have many peptides used in neurology, immunology, gastroenterology, and so-called anti-aging practice.

Here is a brief look at the timeline of the Russians' research and work. It was a long time before the rest of the world got interested in catching up.

In the 1960s they synthesized and produced key peptide hormones and analogues such as oxytocin, vasopressin, ACTH, and somatostatin.

They developed industrial technology for peptide-drug manufacturing. Work was launched at several pharmaceutical plants, enabling scale-up from lab synthesis to marketed medicines.

Of the 70 peptide drugs marketed, Russian scientists are considered the developers of 20% of those and many of the original drugs. Among those are Thymogen (a dipeptide immunostimulant derived from thymus) and Semax (a heptapeptide neuropeptide for CNS indications).

These agents exploit classic peptide advantages: high receptor selectivity, low toxicity (these are chains of amino acids and molecules ubiquitous in nature).

Khavinson and "peptide bioregulators"

Vladimir Khavinson is strongly associated with the concept of short "peptide bioregulators" aimed at modulating gene expression and slowing aspects of aging.

Over roughly 40 years, his group reported the extraction of more than 20 organ-specific peptide complexes and synthesis of numerous di-, tri- and tetrapeptides (that di, tri and tetra just means a chain of 2,3, or 4 amino acids).

His group is associated with six peptide-based pharmaceuticals and 60+ peptide food supplements introduced into clinical or commercial practice, plus nearly 200 patents and hundreds of publications.

Officially registered peptide drugs in Russia span neurology, gastroenterology, immunology, cardiology, and dentistry, reflecting wide clinical use in mainstream medicine rather than a fringe niche.

Contemporary Russian strategies emphasize next-generation peptide drugs: designing peptides with extended half-life (making the work longer in the body), improved oral or transdermal delivery, and peptidomimetics that retain bioactivity while resisting enzymatic degradation.

Russian Timeline

1960s-1970s: Soviet peptide era begins

Late 1960s: USSR establishes dedicated labs for natural-compound and peptide chemistry. By 1970s: Industrial-scale synthetic production of classic peptide hormones and analogues (oxytocin, vasopressin, ACTH, somatostatin and various depsipeptides) is achieved, giving the USSR a domestic peptide manufacturing base.

1970s-1980s: First original Russian peptide drugs

Thymogen, initially isolated from thymus and then synthesized, is introduced as a natural immunocorrector and becomes one of the earliest Russian immunomodulatory peptide drugs.

1980s-1990s: Expansion and platform building

1980s: Original Soviet/Russian labs refine solid-phase synthesis, analytical methods, and scale-up technologies, enabling wider industrial production of peptide preparations at several pharmaceutical plants.

Late 1980s-1990s: Work intensifies on neuropeptides and immunopeptides, setting up the scientific groundwork for later CNS-active, nootropic, and immunomodulating Russian peptide drugs (e.g., Semax, Selank, Licopid, Immunofan).

1990s-2000s: Clinical peptide portfolio emerges

1990s: Semax (heptapeptide ACTH(4-10) analog) is synthesized and moves into clinical use as a nootropic and neuroprotective peptide for ischemic stroke and CNS indications.

1990s-2000s: A series of original Russian peptides are developed and registered, including Thymogen, Semax, Licopid, Immunofan, Thymodepressin, Gepon, Noopept, Selank, and others, covering immunomodulation, antiviral therapy, nootropics, and stress protection.

2000s-2010s: Recognition and quantitative milestones

By the 2000s-early 2010s: Russia has produced ~5000 chemical drugs total, of which ~15 are Russian-origin small molecules. In contrast, of about 70 peptide drugs worldwide, the Russians were early and now the world labs have poured research dollars into development and this is now a focus world-wide.

14 are Russian-developed, giving Russia ~20% of global peptide-drug innovations.

2010s-2020s: Next-generation targets and AD focus

2010s-2020s: Russian peptide research increasingly focuses on neurodegeneration, inflammation, and cerebral ischemia, including Semax transcriptomic studies showing suppression of ischemia-induced pro-inflammatory gene expression and normalization of mRNA patterns in stroke models.

You can imagine the worldwide attention to this topic now that we have this billion-dollar blockbuster drug category.

There are questions about how you patent molecules that are in every cell of every living organism. Many times a molecule is added to an amino acid chain to delay degradation. Those little changes allow patentability. The drug manufacturers are intent on eliminating any competition.