Peptides And Its Application In Various Therapeutic Segments

By Author: Genosphere Biotechnologies
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Peptides are natural or synthetic compounds consisting of a chain of amino acids building blocks linked by the carboxyl group of one amino acid to the amino group of another: the amide peptide bond. There are 20 natural amino acids (and many rare and unnatural) to choose from to build a linear peptide sequence. They are normally smaller than a protein.

The use of peptides as therapeutics is experiencing renewed enthusiasm owing to advances in delivery, stability and design. In fact peptides are key to modern drug research plans. Pertaining to the completion of many whole genome sequencing projects, millions of peptides are produced in milligram scale for research purposes. The study of their biological activity will enables the identification of new targets. These novel active peptides will help fight diseases and strenghten immuno-resistance.

Moreover, there is a growing emphasis on the use of peptides in vaccine design as insights into tissue-specific processing of the immunogenic epitopes of proteins and the discovery of unusually long cytotoxic T-lymphocyte epitopes broaden the range of targets and ...
... give clues to enhancing peptide immunogenicity. The scientists engaged in medical research have realized the potential of peptide-based vaccines for the treatment of chronic viral diseases and cancer, and more developments in the field of peptide-based vaccines are in process.

While peptides can be very potent molecules, their practical utilization for human and veterinary medicine is hampered by their intrinsic natural origin. All organisms have very efficient pathways for polypeptide and peptide degradation thus lowering in vivo stability and bioavailability of natural peptides. However new molecular design and synthetic approches coupled with modern and sophisticated formulation techniques have led to very encouraging results and significant enhancement of organism bioavailability of active peptides. Peptides can be synthesized with known post-translational modifications and/or deliberately introduced with protease-resistant peptide bonds to regulate their processing independent of tissue-specific proteolysis and to stabilize these compounds in vivo.

Peptides can be used for many therapeutic medicinal purposes, as well as in high-end cosmetic products - like the Dermaxime range of anti-aging skin care cosmetics. Synthetic peptides have been developed, which contain active ingredients that can rival the results of laser treatments or surgical face lifts and there are continuous new developments and advances made in this field.

The list of peptides as potential drugs is huge and hundreds are well advanced on the path of drug development processes; space does not permit discussion of them all. It is beyond the scope of this article to focus on older peptide therapies such as luteinizing-hormone-releasing hormone, growth hormone, arginine vasopressin or the very interesting peptide, cyclosporin. We will instead highlight some exciting new areas of research as well as recent developments in the use of more established peptide therapies.

Insulin was the first peptide to be isolated and administered therapeutically, and is still the most commonly prescribed peptide, having been used for over half a century. We have yet to find a chemical mimic; however, there is still ongoing research into novel analogues and methods of administration. Manipulation of the insulin molecule has allowed the development of shorter-acting insulins, such as Lispro insulin. This is rapidly absorbed, readily dissociates into insulin monomers, and produces plasma levels that more closely mimic the normal postprandial insulin profile. Thus, Lispro can be injected immediately prior to a meal, unlike conventional short-acting insulins that should be injected half an hour earlier.

A recent development is the use of non-injectable forms of insulin. Daily injections up to four times per day, is a major source of distress in the diabetic population, for example children or the elderly. It comes as no surprise that inhaled, intranasal, buccal, rectal and sub-lingual preparations of insulin have all been investigated. Precise insulin dosage is critical for `brittle' type 1 diabetics. However, for some, e.g. people with type 2 diabetes that have significant residual endogenous insulin secretion, less accurate forms of administration may be adequate. Recent results shows that inhaled insulin provided glycemic control equivalent to the subcutaneous route, whilst allowing insulin to be taken immediately before a meal. Thus, the future seems to be more hopeful for the `multiply-punctured diabetic'.

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