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The Human Benefits Of Peptide Drug Discovery

By Cathy Mercer

Peptides in this context are short chains of amino acids that have a therapeutic biological activity. Many naturally-occurring substances in the body are short chains of peptides, for example, the endorphin and enkephalins in the central nervous system. Peptide drug discovery has led to the development of therapeutic agents that mimic the effects of these naturally-occurring substances.

Endorphins are morphine-like molecules that are made in the body. They are referred to as endogenous opioid peptides; endogenous because they are produced internally and opioid because they are similar to drugs made by the opium poppy. Drugs that actually come from the opium poppy, such as heroin, codeine and morphine, are referred to as opiates. Both opiates and opioids work on systems in the brain responsible for emotion, appetite control, pain and stress.

The tachykinin peptides include Substance P, Neurokinins A and B, Kassinin and Eledoisin. They are so named because of their ability to cause gut tissue to rapidly contract. They consist of only five amino acids. Vasoactive Intestinal Peptide contains 28 amino acid residues so it is much larger than the tachykinins. Other members of this family include Pituitary Adenylate Cyclase Activating Peptide (PACAP), PHI (Peptide Histidine Isoleucine), Growth Hormone Releasing Hormone 1-24 (GHRH 1-24), glucagon and secretin.

Another group of short-chain amino acid molecules are the Calcitonin peptides. These include calcitonin, Amylin and AGG01. In humans, calcitonin is produced by the parafollicular cells of the thyroid gland. It opposes the effects of parathyroid hormone by reducing levels of plasma calcium ions. Salmon calcitonin is used to treat osteoporosis in postmenopausal women, hypercalcemia, Paget’s disease, bone metastases and phantom limb pain.

A fifth major group of these polypeptide substances are the pancreatic polypeptide-related peptides, which include Peptide YY (PYY), pancreatic polypeptide (PPY), avian pancreatic polypeptide (APP) and neuropeptide Y (NPY). The pancreatic polypeptide (PP) molecule is made up of around 36 amino acids with a combined molecular weight of 4200 Daltons. A dalton is a unit of molecular mass. It is equivalent of one gram per mole.

Pancreatic polypeptide controls hepatic glycogen levels, modulates secretions in the digestive tract and controls the secretory functions in the pancreas. These secretions may be endocrine, acting on the pancreas itself, or exocrine, acting on distant organs. PP is secreted by the pancreas in response to a protein meal, fasting, exercising or during a bad attack of hypoglycemia. Ingesting glucose can reverse these effects.

Lactotripeptides are a class of two tiny, three amino acids in length, that naturally occur in milk. There is some evidence that they may be helpful in controlling blood pressure. Basic natriuretic peptide (BNP), or B-type natriuretic peptide, is composed of a chain of 32 amino acids.

Peptide drug discovery is a promising area of medicine because it is relatively simple to manufacture short amino acids in the laboratory. Calcitonin that is used medically is derived from salmon. Because the molecules are so short, they are not long enough to generate an immune response and so it is possible to use animal-derived versions. So far, we have been able to synthesize drugs that operate on the thyroid, pancreas and central nervous system. The lactotripeptides may one day help to control hypertension.

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Article Citation
MLA Style Citation:
Mercer, Cathy "The Human Benefits Of Peptide Drug Discovery." The Human Benefits Of Peptide Drug Discovery. 12 Apr. 2014. 24 Jul 2014 <>.

APA Style Citation:
Mercer, C (2014, April 12). The Human Benefits Of Peptide Drug Discovery. Retrieved July 24, 2014, from

Chicago Style Citation:
Mercer, Cathy "The Human Benefits Of Peptide Drug Discovery"

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